A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain
出版年份 2016 全文链接
标题
A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain
作者
关键词
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出版物
Chemical Science
Volume 7, Issue 3, Pages 2322-2330
出版商
Royal Society of Chemistry (RSC)
发表日期
2015-12-22
DOI
10.1039/c5sc03115j
参考文献
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注意:仅列出部分参考文献,下载原文获取全部文献信息。- LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor
- (2015) Peter G. K. Clark et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B
- (2015) Peiling Chen et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B
- (2015) Ludovic Drouin et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
- (2015) Natalie H. Theodoulou et al. JOURNAL OF MEDICINAL CHEMISTRY
- Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53
- (2015) Andreas C. Joerger et al. STRUCTURE
- Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions
- (2014) Michael Brand et al. ACS Chemical Biology
- The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor
- (2014) Romain Gosmini et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains
- (2014) Duncan A. Hay et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Advantages of crystallographic fragment screening: Functional and mechanistic insights from a powerful platform for efficient drug discovery
- (2014) Disha Patel et al. PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY
- Efficient exploration of chemical space by fragment-based screening
- (2014) Richard J. Hall et al. PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY
- Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
- (2014) Apirat Chaikuad et al. MedChemComm
- 4-Acyl Pyrroles: Mimicking Acetylated Lysines in Histone Code Reading
- (2013) Xavier Lucas et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
- (2013) Fleur M. Ferguson et al. JOURNAL OF MEDICINAL CHEMISTRY
- [1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains
- (2013) Oleg Fedorov et al. JOURNAL OF MEDICINAL CHEMISTRY
- Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands
- (2013) David S. Hewings et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fragment-Based Approaches in Drug Discovery and Chemical Biology
- (2012) Duncan E. Scott et al. BIOCHEMISTRY
- Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family
- (2012) Panagis Filippakopoulos et al. CELL
- Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites
- (2012) Lewis R. Vidler et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
- (2012) Paul V. Fish et al. JOURNAL OF MEDICINAL CHEMISTRY
- Pleckstrin homology domain-interacting protein (PHIP) as a marker and mediator of melanoma metastasis
- (2012) D. De Semir et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Microwave-mediated synthesis and manipulation of a 2-substituted-5-aminooxazole-4-carbonitrile library
- (2012) John Spencer et al. TETRAHEDRON LETTERS
- USRCAT: real-time ultrafast shape recognition with pharmacophoric constraints
- (2012) Adrian M Schreyer et al. Journal of Cheminformatics
- DOGS: Reaction-Driven de novo Design of Bioactive Compounds
- (2012) Markus Hartenfeller et al. PLoS Computational Biology
- A Collection of Robust Organic Synthesis Reactions forIn SilicoMolecule Design
- (2011) Markus Hartenfeller et al. Journal of Chemical Information and Modeling
- The Medicinal Chemist’s Toolbox: An Analysis of Reactions Used in the Pursuit of Drug Candidates
- (2011) Stephen D. Roughley et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery
- (2011) Chun-wa Chung et al. JOURNAL OF MEDICINAL CHEMISTRY
- Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery
- (2011) Martin Philpott et al. Molecular BioSystems
- Suppression of inflammation by a synthetic histone mimic
- (2010) Edwige Nicodeme et al. NATURE
- Selective inhibition of BET bromodomains
- (2010) Panagis Filippakopoulos et al. NATURE
- Lessons for fragment library design: analysis of output from multiple screening campaigns
- (2009) I-Jen Chen et al. JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
- Heteroaromatic Rings of the Future
- (2009) William R. Pitt et al. JOURNAL OF MEDICINAL CHEMISTRY
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