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。RIPK protein kinase family: Atypical lives of typical kinases
Gregory D. Cuny et al.
SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY (2021)
Chemical-Mediated Targeted Protein Degradation in Neurodegenerative Diseases
Soonsil Hyun et al.
LIFE-BASEL (2021)
Proteolysis targeting chimera (PROTAC) for epidermal growth factor receptor enhances anti-tumor immunity in non-small cell lung cancer
Kai Wang et al.
DRUG DEVELOPMENT RESEARCH (2021)
Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges
Shenxin Zeng et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)
PROTACs to address the challenges facing small molecule inhibitors
Pedro Martin-Acosta et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)
Developments of CRBN-based PROTACs as potential therapeutic agents
Chao Wang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)
Effects of MTX-23, a Novel PROTAC of Androgen Receptor Splice Variant-7 and Androgen Receptor, on CRPC Resistant to Second-Line Antiandrogen Therapy
Geun Taek Lee et al.
MOLECULAR CANCER THERAPEUTICS (2021)
Solution Conformations Shed Light on PROTAC Cell Permeability
Yoseph Atilaw et al.
ACS MEDICINAL CHEMISTRY LETTERS (2021)
Proteolytic Targeting Chimeras with Specificity for Plasma Membrane and Intracellular Estrogen Receptors
Anh S. Lu et al.
MOLECULAR PHARMACEUTICS (2021)
Mutant-selective degradation by BRAF-targeting PROTACs
Shanique Alabi et al.
NATURE COMMUNICATIONS (2021)
Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer
Linrong Chen et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)
Bispecific Estrogen Receptor a Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening
Jeremy S. Disch et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Cancer Selective Target Degradation by Folate-Caged PROTACs
Jing Liu et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)
Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo
Guoshun Luo et al.
ACTA PHARMACEUTICA SINICA B (2021)
PROTACs technology for targeting non-oncoproteins: Advances and perspectives
Chao Wang et al.
BIOORGANIC CHEMISTRY (2021)
Research progress of MEK1/2 inhibitors and degraders in the treatment of cancer
Chao Wang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)
Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma
Yalin Tu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP
Mengzhu Zheng et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
TF-PROTACs Enable Targeted Degradation of Transcription Factors
Jing Liu et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)
Development of Agonist-Based PROTACs Targeting Liver X Receptor
Hanqiao Xu et al.
FRONTIERS IN CHEMISTRY (2021)
E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones
Tasuku Ishida et al.
SLAS DISCOVERY (2021)
A novel small-molecule PROTAC selectively promotes tau clearance to improve cognitive functions in Alzheimer-like models
Weijin Wang et al.
THERANOSTICS (2021)
Development of a PDEδ-Targeting PROTACs that Impair Lipid Metabolism
Michael Winzker et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)
Selective inhibition of Ph-positive ALL cell growth through kinase-dependent and -independent effects by CDK6-specific PROTACs
Marco De Dominici et al.
BLOOD (2020)
Targeted degradation of activating estrogen receptor α ligand-binding domain mutations in human breast cancer
Thomas L. Gonzalez et al.
BREAST CANCER RESEARCH AND TREATMENT (2020)
Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance
Ning Sun et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC)
Hao Zhang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
Estrogen-Related Receptor Alpha: An Under-Appreciated Potential Target for the Treatment of Metabolic Diseases
Madhulika Tripathi et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)
Design, Synthesis, and Biological Evaluation of MEK PROTACs
Stefan Vollmer et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders
Meng Cheng et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
SMAC mimetics and RIPK inhibitors as therapeutics for chronic inflammatory diseases
Simone Jensen et al.
SCIENCE SIGNALING (2020)
Transcription Factor Inhibition: Lessons Learned and Emerging Targets
Andrew Chen et al.
TRENDS IN MOLECULAR MEDICINE (2020)
Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders
Brett L. Roberts et al.
ACS CHEMICAL BIOLOGY (2020)
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs
Niall A. Anderson et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)
Targeted degradation of anaplastic lymphoma kinase by gold nanoparticle-based multi-headed proteolysis targeting chimeras
Yingming Wang et al.
COLLOIDS AND SURFACES B-BIOINTERFACES (2020)
Design and synthesis of selective degraders of EGFRL858R/T790M mutant
Xin Zhang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
Recent advances in FLT3 inhibitors for acute myeloid leukemia
Lexian Tong et al.
FUTURE MEDICINAL CHEMISTRY (2020)
Structure-based drug repositioning explains ibrutinib as VEGFR2 inhibitor
Melissa F. Adasme et al.
PLOS ONE (2020)
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein
Mingliang Wang 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)
Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase
Ka Yang et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
PROTAC Compounds Targeting α-Synuclein Protein for Treating Neurogenerative Disorders: Alzheimer’s and Parkinson’s Diseases
Robert B. Kargbo
ACS Medicinal Chemistry Letters (2020)
A Chemical Switch System to Modulate Chimeric Antigen Receptor T Cell Activity through Proteolysis-Targeting Chimaera Technology
So Myoung Lee et al.
ACS SYNTHETIC BIOLOGY (2020)
Structural Insights into PROTAC-Mediated Degradation of BcI-xL
Chun-wa Chung et al.
ACS CHEMICAL BIOLOGY (2020)
Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs
Michael J. Bond et al.
ACS CENTRAL SCIENCE (2020)
EZH2: a novel target for cancer treatment
Ran Duan et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2020)
A Selective ERRα/γ Inverse Agonist, SLU-PP-1072, Inhibits the Warburg Effect and Induces Apoptosis in Prostate Cancer Cells
Emmalie Schoepke et al.
ACS CHEMICAL BIOLOGY (2020)
Discovery of Novel PDEd Degraders for the Treatment of KRAS Mutant Colorectal Cancer
Junfei Cheng et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight
Terence C. S. Ho et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Small molecule ERK5 kinase inhibitors paradoxically activate ERK5 signalling: be careful what you wish for ...
Simon J. Cook et al.
BIOCHEMICAL SOCIETY TRANSACTIONS (2020)
Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation
Craig Donoghue et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
Systematic Investigation of the Permeability of Androgen Receptor PROTACs
Duncan E. Scott et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK)
Yang Lu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers
Chaoguo Cao et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro tumor growth in vivo
Lijie Zhao et al.
NEOPLASIA (2020)
Discovery of potent small molecule PROTACs targeting mutant EGFR
Hong-Yi Zhao et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics
Hao Chen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders
Jianping Hu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Discovery of novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization
Yuanyuan Shan et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex
Jessie Hao-Ru Hsu et al.
CELL CHEMICAL BIOLOGY (2020)
Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader
Frances Potjewyd et al.
CELL CHEMICAL BIOLOGY (2020)
Exploring Targeted Degradation Strategy for Oncogenic KRASG12C
Mei Zeng et al.
CELL CHEMICAL BIOLOGY (2020)
Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs
Yufeng Xiao et al.
CHEMICAL COMMUNICATIONS (2020)
A caged E3 ligase ligand for PROTAC-mediated protein degradation with light
Cyrille S. Kounde et al.
CHEMICAL COMMUNICATIONS (2020)
PROTACs: An Emerging Therapeutic Modality in Precision Medicine
Dhanusha A. Nalawansha et al.
CELL CHEMICAL BIOLOGY (2020)
PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes
Joshua P. Smalley et al.
CHEMICAL COMMUNICATIONS (2020)
Scaffold hopping enables direct access to more potent PROTACs within vivoactivity
George M. Burslem et al.
CHEMICAL COMMUNICATIONS (2020)
Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders
Christian Steinebach et al.
CHEMICAL SCIENCE (2020)
Inhibitors of ER Aminopeptidase 1 and 2: From Design to Clinical Application
Dimitris Georgiadis et al.
CURRENT MEDICINAL CHEMISTRY (2019)
In Silico Modeling of PROTAC-Mediated Ternary Complexes: Validation and Application
Michael L. Drummond et al.
JOURNAL OF CHEMICAL INFORMATION AND MODELING (2019)
Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions
Johannes Popow et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Treatment of Alzheimer’s by PROTAC-Tau Protein Degradation
Robert B. Kargbo
ACS Medicinal Chemistry Letters (2019)
Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor
Douglas W. Thomson et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Identification of New Small Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation
Lijie Peng et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation
George M. Burslem et al.
CANCER RESEARCH (2019)
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
William Farnaby et al.
NATURE CHEMICAL BIOLOGY (2019)
Targeting IRAK4 for Degradation with PROTACs
Joao Nunes et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader
Hannah Tovell et al.
ACS CHEMICAL BIOLOGY (2019)
Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders
Jiuling Yang et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs
Patrick Pfaff et al.
ACS CENTRAL SCIENCE (2019)
Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader
Jieli Wei et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
EGFR and c-MET Cooperate to Enhance Resistance to PARP Inhibitors in Hepatocellular Carcinoma
Qiongzhu Dong et al.
CANCER RESEARCH (2019)
Optimization techniques for novel c-Met kinase inhibitors
Zhi-Gang Sun et al.
EXPERT OPINION ON DRUG DISCOVERY (2019)
Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)
Jiantao Hu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
Vittoria Zoppi et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer
Xin Han et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands
Xin Han et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
Sajid Khan et al.
NATURE MEDICINE (2019)
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Blake E. Smith et al.
NATURE COMMUNICATIONS (2019)
Targeting transcription factors in cancer - from undruggable to reality
John H. Bushweller
NATURE REVIEWS CANCER (2019)
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyI)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyppyrrolidine-2-carboxamide (VH298)
Pedro Soares et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Andrew P. Crew et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation
Alexandru D. Buhimschi et al.
BIOCHEMISTRY (2018)
PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery
Shanshan Gu et al.
BIOESSAYS (2018)
Emerging Role of Precision Medicine in Cardiovascular Disease
Jane A. Leopold et al.
CIRCULATION RESEARCH (2018)
C-MET inhibitors for advanced non-small cell lung cancer
Giulia Pasquini et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2018)
Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)
Chelsea E. Powell et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Selective inhibition of leukemia-associated SHP2(E69K) mutant by the allosteric SHP2 inhibitor SHP099
X. Sun et al.
LEUKEMIA (2018)
Plasticity in binding confers selectivity in ligand-induced protein degradation
Radoslaw P. Nowak et al.
NATURE CHEMICAL BIOLOGY (2018)
Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands
Lara N. Gechijian et al.
NATURE CHEMICAL BIOLOGY (2018)
Delineating the role of cooperativity in the design of potent PROTACs for BTK
Adelajda Zorba et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2018)
Exercise and prostate cancer: From basic science to clinical applications
Christian Campos et al.
PROSTATE (2018)
Identification, structure modification, and characterization of potential small-molecule SGK3 inhibitors with novel scaffolds
Grace Qun Gong et al.
ACTA PHARMACOLOGICA SINICA (2018)
Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)
Chung Hyo Kang et al.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2018)
Emerging EZH2 Inhibitors and Their Application in Lymphoma
Jennifer K. Lue et al.
CURRENT HEMATOLOGIC MALIGNANCY REPORTS (2018)
Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
Sainan An et al.
EBIOMEDICINE (2018)
Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
George M. Burslem et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2018)
Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation
Philipp M. Cromm et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2018)
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Daniel P. Bondeson 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)
Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance
Jemilat Salami et al.
COMMUNICATIONS BIOLOGY (2018)
Synthesis of piperazine-based thiazolidinones as VEGFR2 tyrosine kinase inhibitors inducing apoptosis
Mostafa M. M. El-Miligy et al.
FUTURE MEDICINAL CHEMISTRY (2017)
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
Wei Qi et al.
NATURE CHEMICAL BIOLOGY (2017)
Structural basis of PROTAC cooperative recognition for selective protein degradation
Morgan S. Gadd et al.
NATURE CHEMICAL BIOLOGY (2017)
Poly (ADP-Ribosyl) Polymerase 1 Inhibitors: A Patent Review
Mengda Cao et al.
RECENT PATENTS ON ANTI-CANCER DRUG DISCOVERY (2017)
Targeting ALK: Precision Medicine Takes on Drug Resistance
Jessica J. Lin et al.
CANCER DISCOVERY (2017)
Design, Synthesis, and Characterization of Brequinar Conjugates as Probes to Study DHODH Inhibition
Joseph T. Madak et al.
CHEMISTRY-A EUROPEAN JOURNAL (2017)
Identification of Breast Cancer Inhibitors Specific for G Protein-Coupled Estrogen Receptor (GPER)-Expressing Cells
Francesca Aiello et al.
CHEMMEDCHEM (2017)
RAS Proteins and Their Regulators in Human Disease
Dhirendra K. Simanshu et al.
CELL (2017)
Structure-based development of PDEδ inhibitors
Pablo Martin-Gago et al.
BIOLOGICAL CHEMISTRY (2017)
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Ashton C. Lai et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Targeting CDK4 and CDK6: From Discovery to Therapy
Charles J. Sherr et al.
CANCER DISCOVERY (2016)
Small-Molecule PROTACS: New Approaches to Protein Degradation
Momar Toure et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
FDA Approval of Palbociclib in Combination with Fulvestrant for the Treatment of Hormone Receptor-Positive, HER2-Negative Metastatic Breast Cancer
Amanda J. Walker et al.
CLINICAL CANCER RESEARCH (2016)
Second- and third-generation ALK inhibitors for non-small cell lung cancer
Jingjing Wu et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2016)
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
Kanak Raina et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition
Julianty Frost et al.
NATURE COMMUNICATIONS (2016)
The Many Roles of BAF (mSWI/SNF) and PBAF Complexes in Cancer
Courtney Hodges et al.
COLD SPRING HARBOR PERSPECTIVES IN MEDICINE (2016)
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
Michael Zengerle et al.
ACS CHEMICAL BIOLOGY (2015)
LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor
Peter G. K. Clark et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2015)
Targeting a Cryptic Allosteric Site for Selective Inhibition of the Oncogenic Protein Tyrosine Phosphatase Shp2
Cynthia M. Chio et al.
BIOCHEMISTRY (2015)
Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription
Yosuke Demizu et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2015)
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination
Philip Jones et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson et al.
NATURE CHEMICAL BIOLOGY (2015)
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-IRK Inhibitors
Ha-Soon Choi et al.
ACS MEDICINAL CHEMISTRY LETTERS (2015)
Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery
Yanai Zhan et al.
EPIGENETICS & CHROMATIN (2015)
Mechanisms of Acquired Resistance to ALK Inhibitors and the Rationale for Treating ALK-positive Lung Cancer
Hideko Isozaki et al.
CANCERS (2015)
RIP kinases: key decision makers in cell death and innate immunity
F. Humphries et al.
CELL DEATH AND DIFFERENTIATION (2015)
Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders
Divya Chaudhary et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
Targeting liver X receptors in cancer therapeutics
Chin-Yo Lin et al.
NATURE REVIEWS CANCER (2015)
Structure-Guided Design and Optimization of Small Molecules Targeting the Protein Protein Interaction between the von Hippel- Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities
Carles Galdeano et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Therapeutic Potential of Targeting the Oncogenic SHP2 Phosphatase
Li-Fan Zeng et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer
Irfan A. Asangani et al.
NATURE (2014)
Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy
Peter E. Czabotar et al.
NATURE REVIEWS MOLECULAR CELL BIOLOGY (2014)
Chimeric Antigen Receptor T Cells for Sustained Remissions in Leukemia
Shannon L. Maude et al.
NEW ENGLAND JOURNAL OF MEDICINE (2014)
Knockdown of Tripartite Motif Containing 24 by Lentivirus Suppresses Cell Growth and Induces Apoptosis in Human Colorectal Cancer Cells
Jianwei Wang et al.
ONCOLOGY RESEARCH (2014)
INPP4B overexpression enhances the antitumor efficacy of PARP inhibitor AG014699 in MDA-MB-231 triple-negative breast cancer cells
Ying Sun et al.
TUMOR BIOLOGY (2014)
Cancer cell death induced by novel small molecules degrading the TACC3 protein via the ubiquitin-proteasome pathway
N. Ohoka et al.
CELL DEATH & DISEASE (2014)
Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond
Matthew Holderfield et al.
NATURE REVIEWS CANCER (2014)
Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells
Keiichiro Okuhira et al.
CANCER SCIENCE (2013)
Histone deacetylase inhibitors down-regulate G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells
Patrick Imesch et al.
FERTILITY AND STERILITY (2013)
Identification of Cryptotanshinone as an Inhibitor of Oncogenic Protein Tyrosine Phosphatase SHP2 (PTPN11)
Wei Liu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer
Anastasia Wyce et al.
ONCOTARGET (2013)
Mechanistic insight into ALK receptor tyrosine kinase in human cancer biology
Bengt Hallberg et al.
NATURE REVIEWS CANCER (2013)
Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy
Yosuke Demizu et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)
Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface
Inge Van Molle et al.
CHEMISTRY & BIOLOGY (2012)
Targeting the von Hippel-Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction
Dennis L. Buckley et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2012)
EMD638683, a Novel SGK Inhibitor with Antihypertensive Potency
Teresa F. Ackermann et al.
CELLULAR PHYSIOLOGY AND BIOCHEMISTRY (2011)
Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein
Keiichiro Okuhira et al.
FEBS LETTERS (2011)
Recent Developments in the Medicinal Chemistry and Therapeutic Potential of Dihydroorotate Dehydrogenase (DHODH) Inhibitors
V. K. Vyas et al.
MINI-REVIEWS IN MEDICINAL CHEMISTRY (2011)
From basic research to clinical development of MEK1/2 inhibitors for cancer therapy
Christophe Fremin et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2010)
Protein Knockdown Using Methyl Bestatin-Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins
Yukihiro Itoh et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2010)
Use of the Pharmacological Inhibitor BX795 to Study the Regulation and Physiological Roles of TBK1 and IκB Kinase ε A DISTINCT UPSTREAM KINASE MEDIATES SER-172 PHOSPHORYLATION AND ACTIVATION
Kristopher Clark et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2009)
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics
Ashley R. Schneekloth et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
ABT-263: A potent and orally bioavailable Bcl-2 family inhibitor
Christin Tse et al.
CANCER RESEARCH (2008)
4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1
Keith A. Menear et al.
JOURNAL OF MEDICINAL CHEMISTRY (2008)
Epidermal growth factor receptor mutations in lung cancer
Sreenath V. Sharma et al.
NATURE REVIEWS CANCER (2007)
ERBB receptors and cancer: The complexity of targeted inhibitors
NE Hynes et al.
NATURE REVIEWS CANCER (2005)
Mechanisms of BCR-ABL in the pathogenesis of chronic myelogenous leukaemia
R Ren
NATURE REVIEWS CANCER (2005)
Androgen receptor in prostate cancer
CA Heinlein et al.
ENDOCRINE REVIEWS (2004)
Chemical genetic control of protein levels: Selective in vivo targeted degradation
JS Schneekloth et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2004)
Characteristics of Photoreceptor PDE (PDE6): similarities and differences to PDE5
RH Cote
INTERNATIONAL JOURNAL OF IMPOTENCE RESEARCH (2004)
Development of protacs to target cancer-promoting proteins for ubiquitination and degradation
KM Sakamoto et al.
MOLECULAR & CELLULAR PROTEOMICS (2003)
Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation
KM Sakamoto et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2001)
Structural mechanism for statin inhibition of HMG-CoA reductase
ES Istvan et al.
SCIENCE (2001)
Ubiquitination of hypoxia-inducible factor requires direct binding to the β-domain of the von Hippel-Lindau protein
M Ohh et al.
NATURE CELL BIOLOGY (2000)
分享论文
