相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。Allosteric SHP2 inhibitors in cancer: Targeting the intersection of RAS, resistance, and the immune microenvironment
D. Lucas Kerr et al.
CURRENT OPINION IN CHEMICAL BIOLOGY (2021)
Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRASG12C Inhibition
Meagan B. Ryan et al.
CLINICAL CANCER RESEARCH (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)
Rapid non-uniform adaptation to conformation-specific KRAS(G12C) inhibition
Jenny Y. Xue et al.
NATURE (2020)
Pan-cancer analysis of whole genomes
Peter J. Campbell et al.
NATURE (2020)
Negative regulation of RAF kinase activity by ATP is overcome by 14-3-3-induced dimerization
Nicholas P. D. Liau et al.
NATURE STRUCTURAL & MOLECULAR BIOLOGY (2020)
REPLY TO TRAN ET AL.: Dimeric KRAS protein-protein interaction stabilizers
Dirk Kessler et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2020)
The small molecule BI-2852 induces a nonfunctional dimer of KRAS
Timothy H. Tran et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2020)
Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors
David E. Heppner et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application
Xinrui Yuan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Selumetinib in Children with Inoperable Plexiform Neurofibromas
Andrea M. Gross et al.
NEW ENGLAND JOURNAL OF MEDICINE (2020)
Structural Basis of AZD9291 Selectivity for EGFR T790M
Xiao-E Yan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Dimerization Induced by C-Terminal 14-3-3 Binding Is Sufficient for BRAF Kinase Activation
Nicholas P. D. Liau et al.
BIOCHEMISTRY (2020)
Targeting KRAS(G12C): From Inhibitory Mechanism to Modulation of Antitumor Effects in Patients
Dongsung Kim et al.
CELL (2020)
RAS-targeted therapies: is the undruggable drugged?
Amanda R. Moore et al.
NATURE REVIEWS DRUG DISCOVERY (2020)
Structural basis for the action of the drug trametinib at KSR-bound MEK
Zaigham M. Khan et al.
NATURE (2020)
Cryo-EM as a powerful tool for drug discovery
John H. Van Drie et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands
Janina Niggenaber et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001-2020)
Liling Huang et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2020)
Clinical Development of BRAF plus MEK Inhibitor Combinations
Vivek Subbiah et al.
TRENDS IN CANCER (2020)
Targeting Alterations in the RAF-MEK Pathway
Rona Yaeger et al.
CANCER DISCOVERY (2019)
A phase I/II multiple expansion cohort trial of MRTX849 in patients with advanced solid tumors with KRAS G12C mutation.
Kyriakos P. Papadopoulos et al.
JOURNAL OF CLINICAL ONCOLOGY (2019)
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor
Ciric To et al.
CANCER DISCOVERY (2019)
Drugging an undruggable pocket on KRAS
Dirk Kessler et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)
Dacomitinib in non-small-cell lung cancer: a comprehensive review for clinical application
Hao Sun et al.
FUTURE ONCOLOGY (2019)
Cryo-EM structure of a dimeric B-Raf:14-3-3 complex reveals asymmetry in the active sites of B-Raf kinases
Yasushi Kondo et al.
SCIENCE (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)
Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes
Eunyoung Park et al.
NATURE (2019)
The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity
Jude Canon et al.
NATURE (2019)
Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors
Dries J. H. De Clercq et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Sorafenib: key lessons from over 10 years of experience
Bernard Escudier et al.
EXPERT REVIEW OF ANTICANCER THERAPY (2019)
RAF inhibitor PLX8394 selectively disrupts BRAF dimers and RAS-independent BRAF-mutant-driven signaling
Zhan Yao et al.
NATURE MEDICINE (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)
Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor
Matthew R. Janes et al.
CELL (2018)
Oncogenic Signaling Pathways in The Cancer Genome Atlas
Francisco Sanchez-Vega et al.
CELL (2018)
Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase
Dietrich A. Ruess et al.
NATURE MEDICINE (2018)
Cryo-EM in drug discovery: achievements, limitations and prospects
Jean-Paul Renaud et al.
NATURE REVIEWS DRUG DISCOVERY (2018)
Osimertinib in Untreated EGFR-Mutated Advanced Non-Small-Cell Lung Cancer
J. -C. Soria et al.
NEW ENGLAND JOURNAL OF MEDICINE (2018)
ERK1/2 inhibitors: New weapons to inhibit the RAS-regulated RAF-MEK1/2-ERK1/2 pathway
Andrew M. Kidger et al.
PHARMACOLOGY & THERAPEUTICS (2018)
Allele-Specific Mechanisms of Activation of MEK1 Mutants Determine Their Properties
Yijun Gao et al.
CANCER DISCOVERY (2018)
Type II RAF inhibitor causes superior ERK pathway suppression compared to type I RAF inhibitor in cells expressing different BRAF mutant types recurrently found in lung cancer
Noeparast Amir et al.
Oncotarget (2018)
Targeting the MAPK Pathway in RAS Mutant Cancers
Sarah G. Hymowitz et al.
COLD SPRING HARBOR PERSPECTIVES IN MEDICINE (2018)
RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1-and RAS-driven cancers
Robert J. Nichols et al.
NATURE CELL BIOLOGY (2018)
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping
Michael Juchum et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site
Marcel Gunther et al.
JOURNAL OF MEDICINAL CHEMISTRY (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)
New perspectives for targeting RAF kinase in human cancer
Zoi Karoulia et al.
NATURE REVIEWS CANCER (2017)
RAS Proteins and Their Regulators in Human Disease
Dhirendra K. Simanshu et al.
CELL (2017)
Lung Cancer: EGFR Inhibitors with Low Nanomolar Activity against a Therapy-Resistant L858R/T790M/C797S Mutant
Marcel Guenther et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
B-Raf Inhibition in the Clinic: Present and Future
Warren Fiskus et al.
ANNUAL REVIEW OF MEDICINE, VOL 67 (2016)
Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2
Scott A. Foster et al.
CANCER CELL (2016)
An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling
Zoi Karoulia et al.
CANCER CELL (2016)
Association Between Plasma Genotyping and Outcomes of Treatment With Osimertinib (AZD9291) in Advanced Non-Small-Cell Lung Cancer
Geoffrey R. Oxnard et al.
JOURNAL OF CLINICAL ONCOLOGY (2016)
Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases
Ying-Nan P. Chen et al.
NATURE (2016)
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors
Yong Jia et al.
NATURE (2016)
Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design
Jonathan M. L. Ostrem et al.
NATURE REVIEWS DRUG DISCOVERY (2016)
Twenty years on: the impact of fragments on drug discovery
Daniel A. Erlanson et al.
NATURE REVIEWS DRUG DISCOVERY (2016)
BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition
Zhan Yao et al.
CANCER CELL (2015)
The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies
Matthew J. Niederst et al.
CLINICAL CANCER RESEARCH (2015)
Use of the epidermal growth factor receptor inhibitors gefitinib, erlotinib, afatinib, dacomitinib, and icotinib in the treatment of non-small-cell lung cancer: a systematic review
P. M. Ellis et al.
CURRENT ONCOLOGY (2015)
RAF inhibitors that evade paradoxical MAPK pathway activation
Chao Zhang et al.
NATURE (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)
Regulation of RAF protein kinases in ERK signalling
Hugo Lavoie et al.
NATURE REVIEWS MOLECULAR CELL BIOLOGY (2015)
Inhibition of Shp2 suppresses mutant EGFR-induced lung tumors in transgenic mouse model of lung adenocarcinoma
Valentina E. Schneeberger et al.
ONCOTARGET (2015)
PTPN11 Is a Central Node in Intrinsic and Acquired Resistance to Targeted Cancer Drugs
Anirudh Prahallad et al.
CELL REPORTS (2015)
MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road
Christopher J. Caunt et al.
NATURE REVIEWS CANCER (2015)
Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?
Zheng Zhao et al.
ACS CHEMICAL BIOLOGY (2014)
Structure of the BRAF-MEK Complex Reveals a Kinase Activity Independent Role for BRAF in MAPK Signaling
Jacob R. Haling et al.
CANCER CELL (2014)
Disruption of CRAF-Mediated MEK Activation Is Required for Effective MEK Inhibition in KRAS Mutant Tumors
Piro Lito et al.
CANCER CELL (2014)
Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond
Matthew Holderfield et al.
NATURE REVIEWS CANCER (2014)
Enhanced Inhibition of ERK Signaling by a Novel Allosteric MEK Inhibitor, CH5126766, That Suppresses Feedback Reactivation of RAF Activity
Nobuya Ishii et al.
CANCER RESEARCH (2013)
Developing Irreversible Inhibitors of the Protein Kinase Cysteinome
Qingsong Liu et al.
CHEMISTRY & BIOLOGY (2013)
Afatinib: First Global Approval
Rosselle T. Dungo et al.
DRUGS (2013)
K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
Jonathan M. Ostrem et al.
NATURE (2013)
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Georgia Hatzivassiliou et al.
NATURE (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)
A Comprehensive Survey of Ras Mutations in Cancer
Ian A. Prior et al.
CANCER RESEARCH (2012)
Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker
Flavio Solca et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2012)
The ERBB network: at last, cancer therapy meets systems biology
Yosef Yarden et al.
NATURE REVIEWS CANCER (2012)
GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition
Aidan G. Gilmartin et al.
CLINICAL CANCER RESEARCH (2011)
RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
Poulikos I. Poulikakos et al.
NATURE (2011)
Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate)
Hiroyuki Abe et al.
ACS MEDICINAL CHEMISTRY LETTERS (2011)
Structural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancer
Michael J. Eck et al.
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2010)
Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF
Sonja J. Heidorn et al.
CELL (2010)
Cell Signaling by Receptor Tyrosine Kinases
Mark A. Lemmon et al.
CELL (2010)
RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF
Poulikos I. Poulikakos et al.
NATURE (2010)
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
Georgia Hatzivassiliou et al.
NATURE (2010)
Crystal Structures of MEK1 Binary and Ternary Complexes with Nucleotides and Inhibitors
Thierry O. Fischmann et al.
BIOCHEMISTRY (2009)
ErbB receptors and signaling pathways in cancer
Nancy E. Hynes et al.
CURRENT OPINION IN CELL BIOLOGY (2009)
Ligand-induced ErbB receptor dimerization
Mark A. Lemmon
EXPERIMENTAL CELL RESEARCH (2009)
Neratinib: an oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer
Prithviraj Bose et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2009)
A dimerization-dependent mechanism drives RAF catalytic activation
Thanashan Rajakulendran et al.
NATURE (2009)
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
Wenjun Zhou et al.
NATURE (2009)
Structure-based design of molecular cancer therapeutics
Rob L. M. van Montfort et al.
TRENDS IN BIOTECHNOLOGY (2009)
Tandem Duplication Producing a Novel Oncogenic BRAF Fusion Gene Defines the Majority of Pilocytic Astrocytomas
David T. W. Jones et al.
CANCER RESEARCH (2008)
The molecular functions of Shp2 in the Ras/Mitogen-activated protein kinase (ERK1/2) pathway
Marie Dance et al.
CELLULAR SIGNALLING (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)
Identification of JTP-70902, a p15INK4b-inductive compound, as a novel MEK1/2 inhibitor
Takayuki Yamaguchi et al.
CANCER SCIENCE (2007)
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: Mechanism of activation and insights into differential inhibitor sensitivity
Cai-Hong Yun et al.
CANCER CELL (2007)
Discovery and development of sorafenib: a multikinase inhibitor for treating cancer
Scott Wilhelm et al.
NATURE REVIEWS DRUG DISCOVERY (2006)
Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib
Kendall D. Carey et al.
CANCER RESEARCH (2006)
An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor
Xuewu Zhang et al.
CELL (2006)
Structural determinants of 14-3-3 binding specificities and regulation of subcellular localization of 14-3-3-ligand complexes: A comparison of the X-ray crystal structures of all human 14-3-3 isoforms
Alexandra K. Gardino et al.
SEMINARS IN CANCER BIOLOGY (2006)
EGFR mutation and resistance of non-small-cell lung cancer to gefitinib
S Kobayashi et al.
NEW ENGLAND JOURNAL OF MEDICINE (2005)
Protein kinase inhibitors: Insights into drug design from structure
MEM Noble et al.
SCIENCE (2004)
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF
PTC Wan et al.
CELL (2004)
A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): Relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells
ER Wood et al.
CANCER RESEARCH (2004)
EGF receptor gene mutations are common in lung cancers from never smokers and are associated with sensitivity of tumors to gefitinib and erlotinib
W Pao et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2004)
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
JF Ohren et al.
NATURE STRUCTURAL & MOLECULAR BIOLOGY (2004)
EGFR mutations in lung cancer:: Correlation with clinical response to gefitinib therapy
JG Paez et al.
SCIENCE (2004)
Mechanisms and implications of imatinib resistance mutations in BCR-ABL
V Nardi et al.
CURRENT OPINION IN HEMATOLOGY (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)
Mutations of the BRAF gene in human cancer
H Davies et al.
NATURE (2002)