Development of potent dimeric inhibitors of GAS41 YEATS domain

GAS41 is an emerging oncogene overexpressed and implicated in multiple cancers, including non-small cell lung cancer (NSCLC). GAS41 is a dimeric protein that contains the YEATS domain, which is involved in the recognition of lysine-acylated histones. Here, we report the development of GAS41 YEATS in...

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Veröffentlicht in:	Cell chemical biology 2021-12, Vol.28 (12), p.1716-1727.e6
Hauptverfasser:	Listunov, Dymytrii, Linhares, Brian M., Kim, EunGi, Winkler, Alyssa, Simes, Miranda L., Weaver, Sidney, Cho, Hyo Je, Rizo, Alexandrea, Zolov, Sergey, Keshamouni, Venkateshwar G., Grembecka, Jolanta, Cierpicki, Tomasz
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemistry Amides - pharmacology Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Carcinoma, Non-Small-Cell Lung - drug therapy Carcinoma, Non-Small-Cell Lung - metabolism Carcinoma, Non-Small-Cell Lung - pathology Cell Proliferation - drug effects Cells, Cultured chemical probes dimeric inhibitors Drug Screening Assays, Antitumor Female GAS41 Humans lung cancer Lung Neoplasms - drug therapy Lung Neoplasms - metabolism Lung Neoplasms - pathology Male Molecular Structure Protein Interaction Domains and Motifs - drug effects Thiophenes - chemistry Thiophenes - pharmacology Transcription Factors - antagonists & inhibitors Transcription Factors - metabolism YEATS domain
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