Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (−)–Pironetin

Autor:	Gunda I. Georg, Henry L. Wong, Sara K. Coulup, David S. Huang
Rok vydání:	2019
Předmět:	Metabolite 01 natural sciences Mice 03 medical and health sciences chemistry.chemical_compound Tubulin In vivo Cell Line Tumor Drug Discovery medicine Animals Humans Cytotoxic T cell 030304 developmental biology Biological Products 0303 health sciences Natural product Metabolism medicine.disease Streptomyces Tubulin Modulators Rats 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry Biochemistry Pyrones Cell culture Microsomes Liver Microsome Molecular Medicine Ovarian cancer Half-Life
Zdroj:	Journal of Medicinal Chemistry. 62:1684-1689
ISSN:	1520-4804 0022-2623
DOI:	10.1021/acs.jmedchem.8b01774
Popis:	Pironetin, the only crystallographically confirmed natural product to target α-tubulin, displays potent cytotoxic activity against sensitive and resistant A2780 ovarian cancer cell lines but is only marginally active in vivo. We now report that pironetin has a short half-life (
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed6dfd45e73c9e892b2d1c6547d56bf9 https://doi.org/10.1021/acs.jmedchem.8b01774 Zobrazit plný text záznamu