Targeting Transcriptional Enhanced Associate Domains (TEADs)

Autor:	Patricia Melnyk, Fabrice Bailly, Manon Sturbaut, Philippe Cotelle, Floriane Gibault
Rok vydání:	2017
Předmět:	0301 basic medicine Hippo signaling pathway Cell growth Effector Chemistry Protein domain Regenerative medicine 3. Good health 03 medical and health sciences 030104 developmental biology Transcription (biology) Drug Discovery Cancer research Molecular Medicine Binding site Stem cell
Zdroj:	Journal of Medicinal Chemistry. 61:5057-5072
ISSN:	1520-4804 0022-2623
DOI:	10.1021/acs.jmedchem.7b00879
Popis:	Transcriptional enhanced associate domain (TEAD) proteins are the downstream effectors of the Hippo signaling pathway that regulate cell proliferation and stem cell functions. TEADs are unable to activate transcription and require the help of coactivators such as YAP, TAZ, VgLL, and p160 proteins. The expression of TEAD family is up-regulated in many cancer types including gastric, colorectal, breast, and prostate cancers, which is correlated with poor survival in patients. Pharmacological modulators of TEADs could therefore find application in cancer treatment and regenerative medicine. In this review, we present the very recent available structures of TEADs with or without coactivators or inhibitors and discuss the potential therapeutic application of their ligands.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::9564609c37885856d272fe8562928586 https://doi.org/10.1021/acs.jmedchem.7b00879 Zobrazit plný text záznamu