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Discovery of a Flavonoid FM04 as a Potent Inhibitor to Reverse P-Glycoprotein-Mediated Drug Resistance in Xenografts and Improve Oral Bioavailability of Paclitaxel

Biotransformation of flavonoid dimer FD18 resulted in an active metabolite FM04. It was more druggable because of its improved physicochemical properties. FM04 (EC(50) = 83 nM) was 1.8-fold more potent than FD18 in reversing P-glycoprotein (P-gp)-mediated paclitaxel (PTX) resistance in vitro. Simila...

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Detalles Bibliográficos
Autores principales: Kan, Jason W. Y., Yan, Clare S. W., Wong, Iris L. K., Su, Xiaochun, Liu, Zhen, Chan, Tak Hang, Chow, Larry M. C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9739180/
https://www.ncbi.nlm.nih.gov/pubmed/36499627
http://dx.doi.org/10.3390/ijms232315299