Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines

Many cancers have the tumor suppressor p53 inactivated by mutation, making reactivation of mutant p53 with small molecules a promising strategy for the development of novel anticancer therapeutics. The oncogenic p53 mutation Y220C, which accounts for approximately 100,000 cancer cases per year, crea...

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Bibliographic Details
Published in:	European journal of medicinal chemistry Vol. 152; pp. 101 - 114
Main Authors:	Baud, Matthias G.J., Bauer, Matthias R., Verduci, Lorena, Dingler, Felix A., Patel, Ketan J., Horil Roy, Deeptee, Joerger, Andreas C., Fersht, Alan R.
Format:	Journal Article
Language:	English
Published:	ISSY-LES-MOULINEAUX Elsevier Masson SAS 25.05.2018 Elsevier Editions Scientifiques Elsevier
Subjects:	Anticancer therapy Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Benzothiazoles - chemical synthesis Benzothiazoles - chemistry Benzothiazoles - pharmacology Cell Proliferation - drug effects Cell Survival - drug effects Chemistry, Medicinal Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Life Sciences & Biomedicine Molecular Structure Mutant p53 Pharmacology & Pharmacy Real-Time Polymerase Chain Reaction Science & Technology Signal Transduction - drug effects Signal Transduction - genetics Structure-Activity Relationship Structure-based drug discovery Tumor Cells, Cultured Tumor Suppressor Protein p53 - genetics Tumor Suppressor Protein p53 - metabolism Anticancer therapy Structure-based drug discovery Mutant p53 WILD-TYPE DNA-BINDING DESIGN PROTEIN TP53 MUTATION GLIDE CORE DOMAIN RESCUE ACCURATE DOCKING REACTIVATION
ISSN:	0223-5234, 1768-3254, 1768-3254
Online Access:	Get full text
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