Related references
Note: Only part of the references are listed.The emerging role of epigenetic therapeutics in immuno-oncology
Michael J. Topper et al.
NATURE REVIEWS CLINICAL ONCOLOGY (2020)
A Potent Blood-Brain Barrier-Permeable Mutant IDH1 Inhibitor Suppresses the Growth of Glioblastoma with IDH1 Mutation in a Patient-Derived Orthotopic Xenograft Model
Yukino Machida et al.
MOLECULAR CANCER THERAPEUTICS (2020)
ERK Inhibitor LY3214996 Targets ERK Pathway-Driven Cancers: A Therapeutic Approach Toward Precision Medicine
Shripad V. Bhagwat et al.
MOLECULAR CANCER THERAPEUTICS (2020)
The great escape: tumour cell plasticity in resistance to targeted therapy
Soufiane Boumahdi et al.
NATURE REVIEWS DRUG DISCOVERY (2020)
The KRAS(G12C) Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients
Jill Hallin et al.
CANCER DISCOVERY (2020)
Molecular Mechanisms of Acquired Resistance to MET Tyrosine Kinase Inhibitors in Patients with MET Exon 14-Mutant NSCLC
Gonzalo Recondo et al.
CLINICAL CANCER RESEARCH (2020)
Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer
R. K. Murthy et al.
NEW ENGLAND JOURNAL OF MEDICINE (2020)
Novel drugs targeting EGFR and HER2 exon 20 mutations in metastatic NSCLC
Iosune Baraibar et al.
CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2020)
Targeting apoptosis in cancer therapy
Benedito A. Carneiro et al.
NATURE REVIEWS CLINICAL ONCOLOGY (2020)
A phase 1/1b study of LSZ102, an oral selective estrogen receptor degrader (SERD), in combination with ribociclib in patients with estrogen receptor-positive (ER plus ) advanced breast cancer (ABC) who had progressed after endocrine therapy (ET)
Komal Jhaveri et al.
CANCER RESEARCH (2020)
Overcoming CDK4/6 inhibitor resistance in ER-positive breast cancer
Neil Portman et al.
ENDOCRINE-RELATED CANCER (2019)
Phase I study of tirabrutinib (ONO-4059/GS-4059) in patients with relapsed or refractory B-cell malignancies in Japan
Wataru Munakata et al.
CANCER SCIENCE (2019)
A Tumor-Agnostic NTRK (TRK) Inhibitor
Franklin W. Huang et al.
CELL (2019)
The Latest Research and Development into the Antibody-Drug Conjugate, [fam-] Trastuzumab Deruxtecan (DS-8201a), for HER2 Cancer Therapy
Takashi Nakada et al.
CHEMICAL & PHARMACEUTICAL BULLETIN (2019)
The Bruton tyrosine kinase inhibitor zanubrutinib (BGB-3111) demonstrated synergies with other anti-lymphoma targeted agents
Chiara Tarantelli et al.
HAEMATOLOGICA (2019)
HER2 Directed Antibody-Drug-Conjugates beyond T-DM1 in Breast Cancer
Gabriel Rinnerthaler et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2019)
First targeted protein degrader hits the clinic
Asher Mullard
NATURE REVIEWS DRUG DISCOVERY (2019)
Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants
Bryan D. Smith et al.
CANCER CELL (2019)
Targeting EGFR Ex20 mutant lung cancer with the wild type sparing kinase inhibitor PRB001
Martin L. Sos et al.
JOURNAL OF CLINICAL ONCOLOGY (2019)
Molecular profiling of ER plus metastatic breast cancers to reveal association of genomic alterations with acquired resistance to CDK4/6 inhibitors.
Pedram Razavi et al.
JOURNAL OF CLINICAL ONCOLOGY (2019)
Dose-escalation study of SAR439859, an oral selective estrogen receptor (ER) degrader (SERD), in postmenopausal women with ER+/HER2-metastatic breast cancer (mBC).
Aditya Bardia et al.
JOURNAL OF CLINICAL ONCOLOGY (2019)
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants
Tsung-Sheng Wu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of (E)-N1-(3-Fluorophenyl)-N3-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)
Xuesong Liu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes
Lu Zhang et al.
MOLECULAR CANCER THERAPEUTICS (2019)
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor
Ciric To et al.
CANCER DISCOVERY (2019)
An experimentally validated approach to calculate the blood-brain barrier permeability of small molecules
Yukun Wang et al.
SCIENTIFIC REPORTS (2019)
Cancer drug resistance needs urgent attention, says research chief
Rebecca Coombes
BMJ-BRITISH MEDICAL JOURNAL (2019)
Mutant Isocitrate Dehydrogenase Inhibitors as Targeted Cancer Therapeutics
Danielle Golub et al.
FRONTIERS IN ONCOLOGY (2019)
Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation
George M. Burslem et al.
CANCER RESEARCH (2019)
Discovery of 2-(4-chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors
Yun Wu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Structures of BCL-2 in complex with venetoclax reveal the molecular basis of resistance mutations
Richard W. Birkinshaw et al.
NATURE COMMUNICATIONS (2019)
3In-silico Prediction of Synergistic Anti-Cancer Drug Combinations Using Multi-omics Data
Remzi Celebi et al.
SCIENTIFIC REPORTS (2019)
EMERALD: Phase III trial of elacestrant (RAD1901) vs endocrine therapy for previously treated ER plus advanced breast cancer
Aditya Bardia et al.
FUTURE ONCOLOGY (2019)
EGFR-Mutated Lung Cancers Resistant to Osimertinib through EGFR C797S Respond to First-Generation Reversible EGFR Inhibitors but Eventually Acquire EGFR T790M/C797S in Preclinical Models and Clinical Samples
Deepa Rangachari et al.
JOURNAL OF THORACIC ONCOLOGY (2019)
TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations
Hibiki Udagawa et al.
MOLECULAR CANCER RESEARCH (2019)
A reality check of the accelerated approval of immune-checkpoint inhibitors
Jennifer Gill et al.
NATURE REVIEWS CLINICAL ONCOLOGY (2019)
Immuno-oncology drug development goes global
Jia Xin Yu et al.
NATURE REVIEWS DRUG DISCOVERY (2019)
Efficacy and safety of HER2 inhibitors in combination with or without pertuzumab for HER2-positive breast cancer: a systematic review and meta-analysis
Shanshan Chen et al.
BMC CANCER (2019)
The Blood-Brain Barrier (BBB) Score
Mayuri Gupta et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors
Harald Engelhardt et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC)
Richard A. Ward et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Potent in Vitro Activity of Tarloxotinib for HER2 Exon 20 Mutations in Lung Cancer and Mechanism of Acquired Resistance
T. Koga et al.
JOURNAL OF THORACIC ONCOLOGY (2019)
The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity
Jude Canon et al.
NATURE (2019)
A view on drug resistance in cancer
Neil Vasan et al.
NATURE (2019)
Role of Androgen Receptor in Prostate Cancer: A Review
Kazutoshi Fujita et al.
WORLD JOURNAL OF MENS HEALTH (2019)
Dormant, quiescent, tolerant and persister cells: Four synonyms for the same target in cancer
Francois M. Vallette et al.
BIOCHEMICAL PHARMACOLOGY (2019)
The oral selective oestrogen receptor degrader (SERD) AZD9496 is comparable to fulvestrant in antagonising ER and circumventing endocrine resistance
Agostina Nardone et al.
BRITISH JOURNAL OF CANCER (2019)
Advances in HER2-Targeted Therapy: Novel Agents and Opportunities Beyond Breast and Gastric Cancer
Funda Meric-Bernstam et al.
CLINICAL CANCER RESEARCH (2019)
YH25448, an Irreversible EGFR-TKI with Potent Intracranial Activity in EGFR Mutant Non-Small Cell Lung Cancer
Jiyeon Yun et al.
CLINICAL CANCER RESEARCH (2019)
Diverse mechanisms of PARP inhibitor resistance in ovarian cancer
Matthew John Wakefield et al.
BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER (2019)
Efficacy of a Covalent ERK1/2 Inhibitor, CC-90003, in KRAS-Mutant Cancer Models Reveals Novel Mechanisms of Response and Resistance
Ida Aronchik et al.
MOLECULAR CANCER RESEARCH (2019)
RAF inhibitor PLX8394 selectively disrupts BRAF dimers and RAS-independent BRAF-mutant-driven signaling
Zhan Yao et al.
NATURE MEDICINE (2019)
Efficacy, safety, and resistance profile of osimertinib in T790M mutation-positive non-small cell lung cancer in real-world practice
Dong Kyu Oh et al.
PLOS ONE (2019)
Acquisition of the Recurrent Gly101Val Mutation in BCL2 Confers Resistance to Venetoclax in Patients with Progressive Chronic Lymphocytic Leukemia
Piers Blombery et al.
CANCER DISCOVERY (2019)
Comparative activity profiling of tyrosine kinase inhibitors (TKIs) against exon 20 insertions and the wild-type form of epidermal growth factor receptor (EGFR)
Richard A. Ward et al.
CANCER RESEARCH (2019)
GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes
C. Metcalfe et al.
CANCER RESEARCH (2019)
Epidermal growth factor receptor oncogenes expressed in glioblastoma are activated as covalent dimers and exhibit unique pharmacology
Matthew O'Connor et al.
CANCER RESEARCH (2019)
Preclinical evaluation of TQB3804, a potent EGFR C797S inhibitor
Xile Liu et al.
CANCER RESEARCH (2019)
Targeting EGFR exon 20 insertion mutations in non-small cell lung cancer
Simon Vyse et al.
SIGNAL TRANSDUCTION AND TARGETED THERAPY (2019)
Bivalent Ligands for Protein Degradation in Drug Discovery
Marcel Scheepstra et al.
COMPUTATIONAL AND STRUCTURAL BIOTECHNOLOGY JOURNAL (2019)
Mathematical Approach to Differentiate Spontaneous and Induced Evolution to Drug Resistance During Cancer Treatment
James M. Greene et al.
JCO CLINICAL CANCER INFORMATICS (2019)
Next-generation sequencing in liquid biopsy: cancer screening and early detection
Ming Chen et al.
HUMAN GENOMICS (2019)
Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer
Lingfeng Chen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study
Ryan J. Sullivan et al.
CANCER DISCOVERY (2018)
Small Molecules Drive Big Improvements in Immuno-Oncology Therapies
Bayard R. Huck et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2018)
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation
Alexandru D. Buhimschi et al.
BIOCHEMISTRY (2018)
Mechanisms of resistance to immune checkpoint inhibitors
Russell W. Jenkins et al.
BRITISH JOURNAL OF CANCER (2018)
Discovery and pharmacological characterization of a novel series of highly selective inhibitors of cyclin-dependent kinases 4 and 6 as anticancer agents
Solomon Tadesse et al.
BRITISH JOURNAL OF PHARMACOLOGY (2018)
MP0274-CP101: A phase 1, first-in-human, single-arm, multi-center, open-label, dose escalation study to assess safety, tolerability, and pharmacokinetics of MP0274 in patients with advanced HER2-positive solid tumors
Richard Baird et al.
CANCER RESEARCH (2018)
PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
Yonghui Sun et al.
CELL RESEARCH (2018)
Investigating Novel Resistance Mechanisms to Third-Generation EGFR Tyrosine Kinase Inhibitor Osimertinib in Non-Small Cell Lung Cancer Patients
Zhe Yang et al.
CLINICAL CANCER RESEARCH (2018)
Ensartinib (X-396) in ALK-Positive Non-Small Cell Lung Cancer: Results from a First-in-Human Phase I/II, Multicenter Study
Leora Horn et al.
CLINICAL CANCER RESEARCH (2018)
Cytochrome P450 Structure, Function and Clinical Significance: A Review
Palrasu Manikandan et al.
CURRENT DRUG TARGETS (2018)
Brain metastases in non-small-cell lung cancer: are tyrosine kinase inhibitors and checkpoint inhibitors now viable options?
S. Morin-Ben Abdallah et al.
CURRENT ONCOLOGY (2018)
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy
Lei Yin et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)
Ado-Trastuzumab Emtansine for Patients With HER2-Mutant Lung Cancers: Results From a Phase II Basket Trial
Bob T. Li et al.
JOURNAL OF CLINICAL ONCOLOGY (2018)
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer
George S. Tria et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development
James J. y Crawford et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Acquired &ITEGFR&IT L718V mutation mediates resistance to osimertinib in non-small cell lung cancer but retains sensitivity to afatinib
Yutao Liu et al.
LUNG CANCER (2018)
Antitumor Activity of Osimertinib, an Irreversible Mutant-Selective EGFR Tyrosine Kinase Inhibitor, in NSCLC Harboring EGFR Exon 20 Insertions
Nicolas Floc'h et al.
MOLECULAR CANCER THERAPEUTICS (2018)
TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations
Shinichi Hasako et al.
MOLECULAR CANCER THERAPEUTICS (2018)
Mechanisms and clinical activity of an EGFR and HER2 exon 20-selective kinase inhibitor in non-small cell lung cancer
Jacqulyne P. Robichaux et al.
NATURE MEDICINE (2018)
Osimertinib in Untreated EGFR-Mutated Advanced Non-Small-Cell Lung Cancer
J. -C. Soria et al.
NEW ENGLAND JOURNAL OF MEDICINE (2018)
Kinact: a computational approach for predicting activating missense mutations in protein kinases
Carlos H. M. Rodrigues et al.
NUCLEIC ACIDS RESEARCH (2018)
L718Q mutant EGFR escapes covalent inhibition by stabilizing a non-reactive conformation of the lung cancer drug osimertinib
D. Callegari et al.
CHEMICAL SCIENCE (2018)
Are BTK and PLCG2 mutations necessary and sufficient for ibrutinib resistance in chronic lymphocytic leukemia?
Benjamin L. Lampson et al.
EXPERT REVIEW OF HEMATOLOGY (2018)
New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons
Lucia Wang et al.
ACS MEDICINAL CHEMISTRY LETTERS (2018)
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
Janeta Popovici-Muller et al.
ACS MEDICINAL CHEMISTRY LETTERS (2018)
Outcomes of ALK positive lung cancer patients treated with crizotinib or second-generation ALK inhibitor: a monoinstitutional experience
Elisa De Carlo et al.
Oncotarget (2018)
Emerging findings into molecular mechanism of brain metastasis
Wenting Ni et al.
CANCER MEDICINE (2018)
Crystal structures of pan-IDH inhibitor AG-881 in complex with mutant human IDH1 and IDH2
Rui Ma et al.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2018)
The Genomic Landscape of Endocrine-Resistant Advanced Breast Cancers
Pedram Razavi et al.
CANCER CELL (2018)
Pharmacodynamic modelling of resistance to epidermal growth factor receptor inhibition in brain metastasis mouse models
Emma C. Martin et al.
CANCER CHEMOTHERAPY AND PHARMACOLOGY (2018)
Single agent activity of ZW25, a HER2-targeted bispecific antibody, in heavily pretreated HER2-expressing cancers.
Funda Meric-Bernstam et al.
JOURNAL OF CLINICAL ONCOLOGY (2018)
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
Joseph Schoepfer et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors
Jason G. Kettle et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Acquired resistance to IDH inhibition through trans or cis dimer-interface mutations
Andrew M. Intlekofer et al.
NATURE (2018)
Constrained peptides' time to shine?
Chris Morrison
NATURE REVIEWS DRUG DISCOVERY (2018)
Efficacy of ALK inhibitors on NSCLC brain metastases: A systematic review and pooled analysis of 21 studies
Fausto Petrelli et al.
PLOS ONE (2018)
Effective treatment of pulmonary adenocarcinoma harboring triple EGFR mutations of L858R, T790M, and cis-C797S by osimertinib, bevacizumab, and brigatinib combination therapy: a case report
Jing Zhao et al.
ONCOTARGETS AND THERAPY (2018)
C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer?
Tobias Grabe et al.
ACS MEDICINAL CHEMISTRY LETTERS (2018)
The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation
Sean D. Reiff et al.
CANCER DISCOVERY (2018)
The Genetic Landscape and Clonal Evolution of Breast Cancer Resistance to Palbociclib plus Fulvestrant in the PALOMA-3 Trial
Ben O'Leary et al.
CANCER DISCOVERY (2018)
Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibit ROS1/TRK/ALK Solvent-Front Mutations
Alexander Drilon et al.
CANCER DISCOVERY (2018)
Landscape of Acquired Resistance to Osimertinib in EGFR-Mutant NSCLC and Clinical Validation of Combined EGFR and RET Inhibition with Osimertinib and BLU-667 for Acquired RET Fusion
Zofia Piotrowska et al.
CANCER DISCOVERY (2018)
Targeting ROS1 rearrangements in non-small cell lung cancer with crizotinib and other kinase inhibitors
Kartik Sehgal et al.
TRANSLATIONAL CANCER RESEARCH (2018)
Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
Sainan An et al.
EBIOMEDICINE (2018)
NTRK fusion-positive cancers and TRK inhibitor therapy
Emiliano Cocco et al.
NATURE REVIEWS CLINICAL ONCOLOGY (2018)
Hematologic Tumor Cell Resistance to the BCL-2 Inhibitor Venetoclax: A Product of Its Microenvironment?
Joel D. Leverson et al.
FRONTIERS IN ONCOLOGY (2018)
Revisiting the role of ABC transporters in multidrug-resistant cancer
Robert W. Robey et al.
NATURE REVIEWS CANCER (2018)
Alectinib in the treatment of ALK-positive non-small cell lung cancer: an update on its properties, efficacy, safety and place in therapy
Tiziana Vavala et al.
THERAPEUTIC ADVANCES IN MEDICAL ONCOLOGY (2018)
Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors
Stergios J. Moschos et al.
JCI INSIGHT (2018)
Mathematical modeling and computational prediction of cancer drug resistance
Xiaoqiang Sun et al.
BRIEFINGS IN BIOINFORMATICS (2018)
Updated Results of Phase 1 Study of DS-8201a in HER2-Expressing or - Mutated Advanced Non-Small-Cell Lung Cancer
J. Tsurutani et al.
JOURNAL OF THORACIC ONCOLOGY (2018)
New Perspectives, Opportunities, and Challenges in Exploring the Human Protein Kinome
Leah J. Wilson et al.
CANCER RESEARCH (2018)
Combining Mutational Signatures, Clonal Fitness, and Drug Affinity to Define Drug-Specific Resistance Mutations in Cancer
Teresa Kaserer et al.
CELL CHEMICAL BIOLOGY (2018)
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
George M. Burslem et al.
CELL CHEMICAL BIOLOGY (2018)
Predicting resistance of clinical Abl mutations to targeted kinase inhibitors using alchemical free-energy calculations
Kevin Hauser et al.
COMMUNICATIONS BIOLOGY (2018)
Drug-Target Kinetics in Drug Discovery
Peter J. Tonge
ACS CHEMICAL NEUROSCIENCE (2018)
Fc-mediated activity of EGFR x c-Met bispecific antibody JNJ-61186372 enhanced killing of lung cancer cells
Katharine D. Grugan et al.
MABS (2017)
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors
Sourav Kalra et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)
Next-Generation Sequencing in Oncology: Genetic Diagnosis, Risk Prediction and Cancer Classification
Rick Kamps et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2017)
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT
Helena Kaitsiotou et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Phase 1/2 Trial of the Oral EGFR/HER2 Inhibitor AP32788 in Non-Small Cell Lung Cancer (NSCLC)
Robert Doebele et al.
JOURNAL OF THORACIC ONCOLOGY (2017)
Combination Osimertinib and Gefitinib in C797S and T790M EGFR-Mutated Non-Small Cell Lung Cancer
Surein Arulananda et al.
JOURNAL OF THORACIC ONCOLOGY (2017)
Brigatinib effective in ALK-positive non-small-cell lung cancer
Manjulika Das
LANCET ONCOLOGY (2017)
Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo
A. Chaturvedi et al.
LEUKEMIA (2017)
Ability of Bruton's Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling
Andrew T. Bender et al.
MOLECULAR PHARMACOLOGY (2017)
CDK4/6 inhibition triggers anti-tumour immunity
Shom Goel et al.
NATURE (2017)
The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1
Andrew A. Wylie et al.
NATURE (2017)
EMT, CSCs, and drug resistance: the mechanistic link and clinical implications
Tsukasa Shibue et al.
NATURE REVIEWS CLINICAL ONCOLOGY (2017)
RNA-based therapeutics: Increasing efficacy
Sarah Crunkhorn
NATURE REVIEWS DRUG DISCOVERY (2017)
Phase II trial of dacomitinib, a pan-human EGFR tyrosine kinase inhibitor, in recurrent glioblastoma patients with EGFR amplification
Juan Manuel Sepulveda-Sanchez et al.
NEURO-ONCOLOGY (2017)
Determining EGFR-TKI sensitivity of G719X and other uncommon EGFR mutations in non-small cell lung cancer: Perplexity and solution (Review)
Kaidi Li et al.
ONCOLOGY REPORTS (2017)
Targeting EGFR T790M mutation in NSCLC: From biology to evaluation and treatment
Antonio Passaro et al.
PHARMACOLOGICAL RESEARCH (2017)
Inhibitors of cyclin-dependent kinases as cancer therapeutics
Steven R. Whittaker et al.
PHARMACOLOGY & THERAPEUTICS (2017)
CRISPR-Cas9-mediated saturated mutagenesis screen predicts clinical drug resistance with improved accuracy
Leyuan Ma et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2017)
The activity, safety, and evolving role of brigatinib in patients with ALK-rearranged non-small cell lung cancers
Joshua K. Sabari et al.
ONCOTARGETS AND THERAPY (2017)
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor
Young Shin Cho et al.
ACS MEDICINAL CHEMISTRY LETTERS (2017)
Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer
Ken Uchibori et al.
NATURE COMMUNICATIONS (2017)
BLU-285 Targets KIT / PDGFRA Conformation and Activating Loop Mutations
Cancer Discovery (2017)
Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372-001 and STARTRK-1)
Alexander Drilon et al.
CANCER DISCOVERY (2017)
An Acquired HER2T798I Gatekeeper Mutation Induces Resistance to Neratinib in a Patient with HER2 Mutant-Driven Breast Cancer
Ariella B. Hanker et al.
CANCER DISCOVERY (2017)
AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations
Katharine Yen et al.
CANCER DISCOVERY (2017)
Spotlight on ceritinib in the treatment of ALK plus NSCLC: design, development and place in therapy
Mariacarmela Santarpia et al.
DRUG DESIGN DEVELOPMENT AND THERAPY (2017)
BRAF inhibitors: resistance and the promise of combination treatments for melanoma
Merope Griffin et al.
ONCOTARGET (2017)
Alectinib for the management of ALK-positive non-small cell lung cancer brain metastases
Natalie A. Lockney et al.
JOURNAL OF THORACIC DISEASE (2017)
Oncolytic Viruses in Cancer Treatment A Review
Sean E. Lawler et al.
JAMA ONCOLOGY (2017)
Treatment patterns, efficacy and toxicity of regorafenib in gastrointestinal stromal tumour patients
Gustavo Schvartsman et al.
SCIENTIFIC REPORTS (2017)
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays
Daniel J. Urban et al.
SCIENTIFIC REPORTS (2017)
Overcoming resistance to BRAF inhibitors
Imanol Arozarena et al.
ANNALS OF TRANSLATIONAL MEDICINE (2017)
Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands
Norihito Shibata et al.
CANCER SCIENCE (2017)
The Different Mechanisms of Cancer Drug Resistance: A Brief Review
Behzad Mansoori et al.
ADVANCED PHARMACEUTICAL BULLETIN (2017)
Molecular Pathways: Hypoxia-Activated Prodrugs in Cancer Therapy
Natalia Baran et al.
CLINICAL CANCER RESEARCH (2017)
Clinical responses to ERK inhibition in BRAFV600E-mutant colorectal cancer predicted using a computational model
Daniel C. Kirouac et al.
NPJ SYSTEMS BIOLOGY AND APPLICATIONS (2017)
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Ashton C. Lai et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Pharmacokinetic Properties of Anticancer Agents for the Treatment of Central Nervous System Tumors: Update of the Literature
Megan O. Jacus et al.
CLINICAL PHARMACOKINETICS (2016)
Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery
Travis T. Wager et al.
ACS CHEMICAL NEUROSCIENCE (2016)
Antibody-drug conjugates-an emerging class of cancer treatment
Nikolaos Diamantis et al.
BRITISH JOURNAL OF CANCER (2016)
Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor-Positive Breast Cancer
Maria Teresa Herrera-Abreu et al.
CANCER RESEARCH (2016)
Metabolism, Biochemical Actions, and Chemical Synthesis of Anticancer Nucleosides, Nucleotides, and Base Analogs
Jadd Shelton et al.
CHEMICAL REVIEWS (2016)
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity
Peter Ballard et al.
CLINICAL CANCER RESEARCH (2016)
Molecular subtypes of gastrointestinal stromal tumor requiring specific treatments
Michael Pogorzelski et al.
CURRENT OPINION IN ONCOLOGY (2016)
The development of LOXO-195, a second generation TRK kinase inhibitor that overcomes acquired resistance to 1st generation inhibitors observed in patients with TRK-fusion cancers
J. Blake et al.
EUROPEAN JOURNAL OF CANCER (2016)
Development of BT1718, a Bicycle Drug Conjugate (BDC) targeting MT1-MMP for treatment of solid tumours
G. Bennett et al.
EUROPEAN JOURNAL OF CANCER (2016)
The potential of neurotrophic tyrosine kinase (NTRK) inhibitors for treating lung cancer
Francesco Passiglia et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2016)
Resistance Mechanisms to Immune-Checkpoint Blockade in Cancer: Tumor-Intrinsic and -Extrinsic Factors
Jonathan M. Pitt et al.
IMMUNITY (2016)
Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer
Shuhang Wang et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2016)
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor
Bryan K. Chan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers
Gerald Lelais et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
cMET Exon 14 Skipping: From the Structure to the Clinic
Nele Van der Steen et al.
JOURNAL OF THORACIC ONCOLOGY (2016)
AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients
Xiao Xu et al.
MOLECULAR CANCER THERAPEUTICS (2016)
The Effect of F877L and T878A Mutations on Androgen Receptor Response to Enzalutamide
Stefan Prekovic et al.
MOLECULAR CANCER THERAPEUTICS (2016)
Targeting Epithelial-Mesenchymal Transition (EMT) to Overcome Drug Resistance in Cancer
Bowen Du et al.
MOLECULES (2016)
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors
Yong Jia et al.
NATURE (2016)
Preclinical Evaluation of the Novel BTK Inhibitor Acalabrutinib in Canine Models of B-Cell Non-Hodgkin Lymphoma
Bonnie K. Harrington et al.
PLOS ONE (2016)
AZD3759, a BBB-penetrating EGFR inhibitor for the treatment of EGFR mutant NSCLC with CNS metastases
Zhenfan Yang et al.
Science Translational Medicine (2016)
Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer
Magda Bahcall et al.
CANCER DISCOVERY (2016)
Receptor tyrosine kinase (c-Kit) inhibitors: a potential therapeutic target in cancer cells
Maryam Abbaspour Babaei et al.
DRUG DESIGN DEVELOPMENT AND THERAPY (2016)
Approaches to modernize the combination drug development paradigm
Daphne Day et al.
GENOME MEDICINE (2016)
Mathematical Modeling of Therapy-induced Cancer Drug Resistance: Connecting Cancer Mechanisms to Population Survival Rates
Xiaoqiang Sun et al.
SCIENTIFIC REPORTS (2016)
Glioblastoma: Overview of Disease and Treatment
Mary Elizabeth Davis
CLINICAL JOURNAL OF ONCOLOGY NURSING (2016)
Targeted therapies with companion diagnostics in the management of breast cancer: current perspectives
Meagan B. Myers
PHARMACOGENOMICS & PERSONALIZED MEDICINE (2016)
Examining the Uptake of Central Nervous System Drugs and Candidates across the Blood-Brain Barrier
Scott G. Summerfield et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2016)
Massively parallel sequencing fails to detect minor resistant subclones in tissue samples prior to tyrosine kinase inhibitor therapy
Carina Heydt et al.
BMC CANCER (2015)
PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models
Helen Y. Zou et al.
CANCER CELL (2015)
Mapping the Pathways of Resistance to Targeted Therapies
Kris C. Wood
CANCER RESEARCH (2015)
Oncogene addiction: pathways of therapeutic response, resistance, and road maps toward a cure
Raymond Pagliarini et al.
EMBO REPORTS (2015)
Influence of multidrug resistance and drug transport proteins on chemotherapy drug metabolism
Helena Joyce et al.
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2015)
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts
Andiliy Lai et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer
Donald P. McDonnell et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
The Role of Multidrug Resistance Efflux Pumps in Cancer: Revisiting a JNCI Publication Exploring Expression of the MDR1 (P-glycoprotein) Gene
Michael M. Gottesman et al.
JNCI-JOURNAL OF THE NATIONAL CANCER INSTITUTE (2015)
Nivolumab versus chemotherapy in patients with advanced melanoma who progressed after anti-CTLA-4 treatment (CheckMate 037): a randomised, controlled, open-label, phase 3 trial
Jeffrey S. Weber et al.
LANCET ONCOLOGY (2015)
Selective estrogen receptor modulators (SERMs): A review of clinical data
Sebastian Mirkin et al.
MATURITAS (2015)
Prime time for PROTACs
Raymond J. Deshaies
NATURE CHEMICAL BIOLOGY (2015)
Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M
Kenneth S. Thress et al.
NATURE MEDICINE (2015)
Nivolumab in Previously Untreated Melanoma without BRAF Mutation
Caroline Robert et al.
NEW ENGLAND JOURNAL OF MEDICINE (2015)
Nivolumab versus Docetaxel in Advanced Squamous-Cell Non-Small-Cell Lung Cancer
Julie Brahmer et al.
NEW ENGLAND JOURNAL OF MEDICINE (2015)
An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101
Robert C. Doebele et al.
CANCER DISCOVERY (2015)
The Role of Multidrug Resistance Efflux Pumps in Cancer: Revisiting a JNCI Publication Exploring Expression of the MDR1 (P-glycoprotein) Gene
Michael M. Gottesman et al.
JNCI-JOURNAL OF THE NATIONAL CANCER INSTITUTE (2015)
Prediction of Cancer Drug Resistance and implications for Personalized Medicine
Manfred Volm et al.
FRONTIERS IN ONCOLOGY (2015)
TRKing Down an Old Oncogene in a New Era of Targeted Therapy
Aria Vaishnavi et al.
CANCER DISCOVERY (2015)
Brain Exposure of Two Selective Dual CDK4 and CDK6 Inhibitors and the Antitumor Activity of CDK4 and CDK6 Inhibition in Combination with Temozolomide in an Intracranial Glioblastoma Xenograft
Thomas J. Raub et al.
DRUG METABOLISM AND DISPOSITION (2015)
Increased KIT Inhibition Enhances Therapeutic Efficacy in Gastrointestinal Stromal Tumor
Teresa S. Kim et al.
CLINICAL CANCER RESEARCH (2014)
Ponatinib Inhibits Polyclonal Drug-Resistant KIT Oncoproteins and Shows Therapeutic Potential in Heavily Pretreated Gastrointestinal Stromal Tumor (GIST) Patients
Andrew P. Garner et al.
CLINICAL CANCER RESEARCH (2014)
Current Status of Targeted Therapy for Anaplastic Lymphoma Kinase-Rearranged Non-Small Cell Lung Cancer
B. Solomon et al.
CLINICAL PHARMACOLOGY & THERAPEUTICS (2014)
In Vitro and In Vivo Models for Analysis of Resistance to Anticancer Molecular Therapies
Roberta Rosa et al.
CURRENT MEDICINAL CHEMISTRY (2014)
Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor
M. Raymond V. Finlay et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations
Ted W. Johnson et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation
Emily J. Hanan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Anti-programmed-death-receptor-1 treatment with pembrolizumab in ipilimumab-refractory advanced melanoma: a randomised dose-comparison cohort of a phase 1 trial
Caroline Robert et al.
LANCET (2014)
Identification of a new androgen receptor (AR) co-regulator BUD31 and related peptides to suppress wild-type and mutated AR-mediated prostate cancer growth via peptide screening and X-ray structure analysis
Cheng-Lung Hsu et al.
MOLECULAR ONCOLOGY (2014)
mRNA-based therapeutics - developing a new class of drugs
Ugur Sahin et al.
NATURE REVIEWS DRUG DISCOVERY (2014)
Detection of Circulating Tumor DNA in Early- and Late-Stage Human Malignancies
Chetan Bettegowda et al.
SCIENCE TRANSLATIONAL MEDICINE (2014)
The Genetic Landscape of Clinical Resistance to RAF Inhibition in Metastatic Melanoma
Eliezer M. Van Allen et al.
CANCER DISCOVERY (2014)
AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer
Darren A. E. Cross et al.
CANCER DISCOVERY (2014)
The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non-Small Cell Lung Cancer
Luc Friboulet et al.
CANCER DISCOVERY (2014)
Beyond antisepsis: Examining the relevance of the works of Joseph Baron Lister to the contemporary surgeon-scientist
Graeme E. Glass
INDIAN JOURNAL OF PLASTIC SURGERY (2014)
Bruton tyrosine kinase inhibitors: a promising novel targeted treatment for B cell lymphomas
Amin Aalipour et al.
BRITISH JOURNAL OF HAEMATOLOGY (2013)
Allostery in Disease and in Drug Discovery
Ruth Nussinov et al.
CELL (2013)
The Somatic Genomic Landscape of Glioblastoma
Cameron W. Brennan et al.
CELL (2013)
P-glycoprotein Inhibition as a Therapeutic Approach for Overcoming Multidrug Resistance in Cancer: Current Status and Future Perspectives
Ziyad Binkhathlan et al.
CURRENT CANCER DRUG TARGETS (2013)
Lung Cancer That Harbors an HER2 Mutation: Epidemiologic Characteristics and Therapeutic Perspectives
Julien Mazieres et al.
JOURNAL OF CLINICAL ONCOLOGY (2013)
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
Richard A. Ward et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
Synthesis, Structure-Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials
Thomas H. Marsilje et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
EGFR Exon 20 Insertion Mutations in Lung Adenocarcinomas: Prevalence, Molecular Heterogeneity, and Clinicopathologic Characteristics
Maria E. Arcila et al.
MOLECULAR CANCER THERAPEUTICS (2013)
Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trial
George D. Demetri et al.
LANCET (2013)
Through the open door: Preferential binding of dasatinib to the active form of BCR-ABL unveiled by in silico experiments
Erik Laurini et al.
MOLECULAR ONCOLOGY (2013)
K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
Jonathan M. Ostrem et al.
NATURE (2013)
Mutational landscape and significance across 12 major cancer types
Cyriac Kandoth et al.
NATURE (2013)
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets
Andrew J. Souers et al.
NATURE MEDICINE (2013)
Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia
John C. Byrd et al.
NEW ENGLAND JOURNAL OF MEDICINE (2013)
Chimeric Antigen Receptor-Modified T Cells for Acute Lymphoid Leukemia
Stephan A. Grupp et al.
NEW ENGLAND JOURNAL OF MEDICINE (2013)
Effects of oncogenic mutations on the conformational free-energy landscape of EGFR kinase
Ludovico Sutto et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)
Structural, Biochemical, and Clinical Characterization of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations in Lung Cancer
Hiroyuki Yasuda et al.
SCIENCE TRANSLATIONAL MEDICINE (2013)
Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC
Annette O. Walter et al.
CANCER DISCOVERY (2013)
Mechanisms and insights into drug resistance in cancer
Hiba Zahreddine et al.
FRONTIERS IN PHARMACOLOGY (2013)
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802)
Kazutomo Kinoshita et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2012)
Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors
Shaojing Hu et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)
Analysis of Receptor Tyrosine Kinase ROS1-Positive Tumors in Non-Small Cell Lung Cancer: Identification of a FIG-ROS1 Fusion
Victoria M. Rimkunas et al.
CLINICAL CANCER RESEARCH (2012)
Crenolanib Inhibits the Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors
Michael C. Heinrich et al.
CLINICAL CANCER RESEARCH (2012)
Frequent Mutational Activation of the PI3K-AKT Pathway in Trastuzumab-Resistant Breast Cancer
Sarat Chandarlapaty et al.
CLINICAL CANCER RESEARCH (2012)
Strategies for Overcoming EGFR Resistance in the Treatment of Advanced-Stage NSCLC
Christine M. Lovly et al.
CURRENT TREATMENT OPTIONS IN ONCOLOGY (2012)
Amino acids: Chemistry, functionality and selected non-enzymatic post-translational modifications
Rainer Bischoff et al.
JOURNAL OF PROTEOMICS (2012)
The Different Flexibility of c-Src and c-Abl Kinases Regulates the Accessibility of a Druggable Inactive Conformation
Silvia Lovera et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2012)
Dacomitinib (PF-00299804), an Irreversible Pan-HER Inhibitor, Inhibits Proliferation of HER2-Amplified Breast Cancer Cell Lines Resistant to Trastuzumab and Lapatinib
Ondrej Kalous et al.
MOLECULAR CANCER THERAPEUTICS (2012)
Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial
Vincent A. Miller et al.
LANCET ONCOLOGY (2012)
The novel cyclin-dependent kinase inhibitor dinaciclib (SCH727965) promotes apoptosis and abrogates microenvironmental cytokine protection in chronic lymphocytic leukemia cells
A. J. Johnson et al.
LEUKEMIA (2012)
Human Tumor Xenografts: The Good, the Bad, and the Ugly
Richard A. Morgan
MOLECULAR THERAPY (2012)
Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations
Keith T. Flaherty et al.
NEW ENGLAND JOURNAL OF MEDICINE (2012)
Differential Sensitivity of Glioma-versus Lung Cancer-Specific EGFR Mutations to EGFR Kinase Inhibitors
Igor Vivanco et al.
CANCER DISCOVERY (2012)
Epithelial Mesenchymal Transition in Drug Resistance and Metastasis of Lung Cancer
Fariz Nurwidya et al.
CANCER RESEARCH AND TREATMENT (2012)
Personalized Medicine and Cancer
Mukesh Verma
JOURNAL OF PERSONALIZED MEDICINE (2012)
Recent advances in apoptosis, mitochondria and drug resistance in cancer cells
Inthrani R. Indran et al.
BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS (2011)
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors
Kazutomo Kinoshita et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2011)
Hallmarks of Cancer: The Next Generation
Douglas Hanahan et al.
CELL (2011)
Mechanisms of drug resistance in kinases
Rina Barouch-Bentov et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2011)
HER2-amplified breast cancer: mechanisms of trastuzumab resistance and novel targeted therapies
Devika Gajria et al.
EXPERT REVIEW OF ANTICANCER THERAPY (2011)
KRAS and BRAF: drug targets and predictive biomarkers
Efsevia Vakiani et al.
JOURNAL OF PATHOLOGY (2011)
Aromatase, aromatase inhibitors, and breast cancer
Saranya Chumsri et al.
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY (2011)
Pathway Analysis of Glioblastoma Tissue after Preoperative Treatment with the EGFR Tyrosine Kinase Inhibitor Gefitinib-A Phase II Trial
Monika E. Hegi et al.
MOLECULAR CANCER THERAPEUTICS (2011)
The resurgence of covalent drugs
Juswinder Singh et al.
NATURE REVIEWS DRUG DISCOVERY (2011)
Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation
Paul B. Chapman et al.
NEW ENGLAND JOURNAL OF MEDICINE (2011)
Differential Sensitivity of ERBB2 Kinase Domain Mutations towards Lapatinib
Rama Krishna Kancha et al.
PLOS ONE (2011)
The Energy Landscape Analysis of Cancer Mutations in Protein Kinases
Anshuman Dixit et al.
PLOS ONE (2011)
Nilotinib: A Novel, Selective Tyrosine Kinase Inhibitor
Jean-Yves Blay et al.
SEMINARS IN ONCOLOGY (2011)
Lapatinib, a Dual-Targeted Small Molecule Inhibitor of EGFR and HER2, in HER2-Amplified Breast Cancer: From Bench to Bedside
Roger Y. Tsang et al.
CLINICAL MEDICINE INSIGHTS-THERAPEUTICS (2011)
Gastrointestinal stromal tumours: origin and molecular oncology
Christopher L. Corless et al.
NATURE REVIEWS CANCER (2011)
RAS oncogenes: weaving a tumorigenic web
Yuliya Pylayeva-Gupta et al.
NATURE REVIEWS CANCER (2011)
Cyclin D as a therapeutic target in cancer
Elizabeth A. Musgrove et al.
NATURE REVIEWS CANCER (2011)
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site
Doriano Fabbro et al.
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2010)
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
Andrew M. Petros et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)
RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models
Hong Yang et al.
CANCER RESEARCH (2010)
Interleukin-8 Mediates Resistance to Antiangiogenic Agent Sunitinib in Renal Cell Carcinoma
Dan Huang et al.
CANCER RESEARCH (2010)
A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations
Sreenath V. Sharma et al.
CELL (2010)
Molecular Mechanisms of Resistance to Cetuximab and Panitumumab in Colorectal Cancer
Alberto Bardelli et al.
JOURNAL OF CLINICAL ONCOLOGY (2010)
Through the Gatekeeper Door: Exploiting the Active Kinase Conformation
Fabio Zuccotto et al.
JOURNAL OF MEDICINAL CHEMISTRY (2010)
Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant
Wei-Sheng Huang et al.
JOURNAL OF MEDICINAL CHEMISTRY (2010)
A Medicinal Chemist's Guide to Molecular Interactions
Caterina Bissantz et al.
JOURNAL OF MEDICINAL CHEMISTRY (2010)
Oral poly(ADP-ribose) polymerase inhibitor olaparib in patients with BRCA1 or BRCA2 mutations and advanced breast cancer: a proof-of-concept trial
Andrew Tutt et al.
LANCET (2010)
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors
Jianming Zhang et al.
NATURE (2010)
Melanomas acquire resistance toB-RAF(V600E) inhibition by RTK or N-RAS upregulation
Ramin Nazarian et al.
NATURE (2010)
Inhibition of Mutated, Activated BRAF in Metastatic Melanoma
Keith T. Flaherty et al.
NEW ENGLAND JOURNAL OF MEDICINE (2010)
Improved Survival with Ipilimumab in Patients with Metastatic Melanoma
F. Stephen Hodi et al.
NEW ENGLAND JOURNAL OF MEDICINE (2010)
The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy
Lee A. Honigberg et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2010)
Molecular biology of bcr-abl1-positive chronic myeloid leukemia
Alfonso Quintas-Cardama et al.
BLOOD (2009)
Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction
Ji Luo et al.
CELL (2009)
The gatekeeper mutation T315I confers resistance against small molecules by increasing or restoring the ABL-kinase activity accompanied by aberrant transphosphorylation of endogenous BCR, even in loss-of-function mutants of BCR/ABL
A. A. Mian et al.
LEUKEMIA (2009)
Cancer-associated IDH1 mutations produce 2-hydroxyglutarate
Lenny Dang et al.
NATURE (2009)
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
Wenjun Zhou et al.
NATURE (2009)
Gefitinib or Carboplatin-Paclitaxel in Pulmonary Adenocarcinoma.
Tony S. Mok et al.
NEW ENGLAND JOURNAL OF MEDICINE (2009)
Other monuments to inhalation anesthesia
Rafael A. Ortega et al.
ANESTHESIOLOGY (2008)
Comparison of the EGFR resistance mutation profiles generated by EGFR-targeted tyrosine kinase inhibitors and the impact of drug combinations
Egle Avizienyte et al.
BIOCHEMICAL JOURNAL (2008)
Discovery of an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins
Cheol-Min Park et al.
JOURNAL OF MEDICINAL CHEMISTRY (2008)
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
James Tsai et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2008)
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
Cai-Hong Yun et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2008)
Bevacizumab plus interferon alfa-2a for treatment of metastatic renal cell carcinoma: a randomised, double-blind phase III trial
Bernard Escudier et al.
LANCET (2007)
Part I: Mechanisms of resistance to imatinib in chronic myeloid leukaemia
Jane F. Apperley
LANCET ONCOLOGY (2007)
Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer
Manabu Soda et al.
NATURE (2007)
Differential regulation of MAP kinase signalling by dual-specificity protein phosphatases
D. M. Owens et al.
ONCOGENE (2007)
MAP kinase signalling pathways in cancer
A. S. Dhillon et al.
ONCOGENE (2007)
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics
Jimmy A. Blair et al.
NATURE CHEMICAL BIOLOGY (2007)
Approval summary: Sunitinib for the treatment of imatinib refractory or intolerant gastrointestinal stromal tumors and advanced renal cell carcinoma
Vicki L. Goodman et al.
CLINICAL CANCER RESEARCH (2007)
Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase
Zhengying Pan et al.
CHEMMEDCHEM (2007)
Epidermal growth factor receptor mutations in lung cancer
Sreenath V. Sharma et al.
NATURE REVIEWS CANCER (2007)
Contribution of ABL kinase domain mutations to imatinib resistance in different subsets of Philadelphia-positive patients: By the GIMEMA working party on chronic myeloid leukemia
Simona Soverini et al.
CLINICAL CANCER RESEARCH (2006)
2-aminothiazole as a novel kinase inhibitor template.: Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (Dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor
Jagabandhu Das et al.
JOURNAL OF MEDICINAL CHEMISTRY (2006)
Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor - Mutant lung adenocarcinomas with acquired resistance to kinase inhibitors
Marissa N. Balak et al.
CLINICAL CANCER RESEARCH (2006)
A novel Bcr-Abl splice isoform is associated with the L248V mutation in CML patients with acquired resistance to imatinib
F. X. Gruber et al.
LEUKEMIA (2006)
Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial
George D. Demetri et al.
LANCET (2006)
Aromatase inhibitors in breast cancer: An overview
Kadri Altundag et al.
ONCOLOGIST (2006)
Pharmacodynamics of cytarabine alone and in combination with 7-hydroxystaurosporine (UCN-01) in AML blasts in vitro and during a clinical trial
D Sampath et al.
BLOOD (2006)
The extracellular signal-regulated kinase: Multiple substrates regulate diverse cellular functions
S Yoon et al.
GROWTH FACTORS (2006)
Allosteric inhibitors of Bcr-abl-dependent cell proliferation
FJ Adrián et al.
NATURE CHEMICAL BIOLOGY (2006)
BRAF mutation predicts sensitivity to MEK inhibition
DB Solit et al.
NATURE (2006)
Epidermal growth factor receptor (EGFR) signaling in cancer
N Normanno et al.
GENE (2006)
Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy
H Farmer et al.
NATURE (2005)
EGFR mutation and resistance of non-small-cell lung cancer to gefitinib
S Kobayashi et al.
NEW ENGLAND JOURNAL OF MEDICINE (2005)
Evaluation of the MDR-MDCK cell line as a permeability screen for the blood-brain barrier
Q Wang et al.
INTERNATIONAL JOURNAL OF PHARMACEUTICS (2005)
Apoptosis defects and chemotherapy resistance: molecular interaction maps and networks
Y Pommier et al.
ONCOGENE (2004)
Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
TJ Lynch et al.
NEW ENGLAND JOURNAL OF MEDICINE (2004)
Defects in the apoptotic machinery of cancer cells: role in drug resistance
B Zhivotovsky et al.
SEMINARS IN CANCER BIOLOGY (2003)
Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways
WL Xia et al.
ONCOGENE (2002)
Imatinib: a selective tyrosine kinase inhibitor
PW Manley et al.
EUROPEAN JOURNAL OF CANCER (2002)
KIT mutations are common in incidental gastrointestinal stromal tumors one centimeter or less in size
CL Corless et al.
AMERICAN JOURNAL OF PATHOLOGY (2002)
Multidrug resistance in cancer: Role of ATP-dependent transporters
MM Gottesman et al.
NATURE REVIEWS CANCER (2002)
Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia.
BJ Druker et al.
NEW ENGLAND JOURNAL OF MEDICINE (2001)