Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP.
Acetylation
/ drug effects
Antineoplastic Agents
/ chemical synthesis
Cell Line, Tumor
Cell Proliferation
/ drug effects
Drug Discovery
Enzyme Inhibitors
/ chemical synthesis
Gene Expression Regulation, Neoplastic
/ drug effects
Humans
Molecular Docking Simulation
Molecular Structure
Structure-Activity Relationship
Thiophenes
/ chemical synthesis
p300-CBP Transcription Factors
/ antagonists & inhibitors
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
14 05 2020
14 05 2020
Historique:
pubmed:
22
4
2020
medline:
3
11
2020
entrez:
22
4
2020
Statut:
ppublish
Résumé
Histone acetyltransferase (HAT) p300 and its paralog CBP acetylate histone lysine side chains and play critical roles in regulating gene transcription. The HAT domain of p300/CBP is a potential drug target for cancer. Through compound screening and medicinal chemistry, novel inhibitors of p300/CBP HAT with their IC
Identifiants
pubmed: 32314924
doi: 10.1021/acs.jmedchem.9b02164
pmc: PMC7340344
mid: NIHMS1603897
doi:
Substances chimiques
Antineoplastic Agents
0
Enzyme Inhibitors
0
Thiophenes
0
p300-CBP Transcription Factors
EC 2.3.1.48
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
4716-4731Subventions
Organisme : NCI NIH HHS
ID : P30 CA125123
Pays : United States
Organisme : NCI NIH HHS
ID : P50 CA058183
Pays : United States
Organisme : NCI NIH HHS
ID : P50 CA186784
Pays : United States
Organisme : NCI NIH HHS
ID : U54 CA233223
Pays : United States
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