PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
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Selective BET bromodomain inhibition as an antifungal therapeutic strategyExploiting Epigenetic Alterations in Prostate Cancer.Induced protein degradation: an emerging drug discovery paradigm.In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs).Structural basis of PROTAC cooperative recognition for selective protein degradationChemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathwayNew Modalities for Challenging Targets in Drug Discovery.Small molecules and their role in effective preclinical target validation.Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.Waste disposal-An attractive strategy for cancer therapy.Mammalian SWI/SNF complexes in cancer: emerging therapeutic opportunities.Targeted protein knockdown using small molecule degraders.Targeted Protein Degradation: from Chemical Biology to Drug Discovery.Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells.Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer.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-dimethylbutanoyl)-Targeting oncoproteins for degradation by small molecules in myeloid leukemia.Targeting bromodomain and extraterminal proteins in breast cancer.Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders.Synthesis and biological evaluation of indazole-4,7-dione derivatives as novel BRD4 inhibitors.Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands.Destroying the androgen receptor (AR)-potential strategy to treat advanced prostate cancer.Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon.Emerging small molecule approaches to enhance the antimyeloma benefit of proteasome inhibitors.BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells.Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC).Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation.Role of androgen receptor splice variants in prostate cancer metastasis.Recent Advances in Prostate Cancer Treatment and Drug Discovery.Small Molecule Modulators of RING-Type E3 Ligases: MDM and Cullin Families as Targets.Optimization of a "bump-and-hole" approach to allele-selective BET bromodomain inhibition.Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugsPharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinaseInterplay between interferon regulatory factor 1 and BRD4 in the regulation of PD-L1 in pancreatic stellate cells
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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
description
article científic
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article scientifique
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articolo scientifico
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artigo científico
@pt
bilimsel makale
@tr
scientific article published on 06 June 2016
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vedecký článok
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vetenskaplig artikel
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videnskabelig artikel
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vědecký článek
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name
PROTAC-induced BET protein deg ...... ion-resistant prostate cancer.
@en
PROTAC-induced BET protein deg ...... ion-resistant prostate cancer.
@nl
type
label
PROTAC-induced BET protein deg ...... ion-resistant prostate cancer.
@en
PROTAC-induced BET protein deg ...... ion-resistant prostate cancer.
@nl
prefLabel
PROTAC-induced BET protein deg ...... ion-resistant prostate cancer.
@en
PROTAC-induced BET protein deg ...... ion-resistant prostate cancer.
@nl
P2093
P2860
P356
P1476
PROTAC-induced BET protein deg ...... ion-resistant prostate cancer.
@en
P2093
Andrew P Crew
Ann Marie K Rossi
Craig M Crews
Hanqing Dong
James D Winkler
Kanak Raina
Kevin G Coleman
P2860
P304
P356
10.1073/PNAS.1521738113
P407
P577
2016-06-06T00:00:00Z