Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.
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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.Targeted Protein Degradation: from Chemical Biology to Drug Discovery.Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation.Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-2.Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon.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.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 kinase
P2860
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P2860
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.
description
2017 nî lūn-bûn
@nan
2017年の論文
@ja
2017年学术文章
@wuu
2017年学术文章
@zh-cn
2017年学术文章
@zh-hans
2017年学术文章
@zh-my
2017年学术文章
@zh-sg
2017年學術文章
@yue
2017年學術文章
@zh
2017年學術文章
@zh-hant
name
Discovery of a Small-Molecule ...... of Achieving Tumor Regression.
@en
type
label
Discovery of a Small-Molecule ...... of Achieving Tumor Regression.
@en
prefLabel
Discovery of a Small-Molecule ...... of Achieving Tumor Regression.
@en
P2093
P2860
P50
P1476
Discovery of a Small-Molecule ...... of Achieving Tumor Regression
@en
P2093
Chao-Yie Yang
Donna McEachern
Ester Fernandez-Salas
Jiantao Hu
Longchuan Bai
P2860
P304
P356
10.1021/ACS.JMEDCHEM.6B01816
P407
P577
2017-03-24T00:00:00Z