Design, Synthesis, and Biological Application of Novel Photoaffinity Probes of Dihydropyridine Derivatives, BAY R3401

Autor:	Liying Zhang, Zhiwei Yan, Youde Wang, Chengjun Song, Guangxin Miao
Jazyk:	angličtina
Rok vydání:	2019
Předmět:	BAY R3401 molecular mechanism type 2 diabetes photoaffinity probe glycogenolysis photoaffinity labeling target proteins Organic chemistry QD241-441
Zdroj:	Molecules, Vol 24, Iss 13, p 2394 (2019)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules24132394
Popis:	To explore the molecular mechanisms of BAY R3401, four types of novel photoaffinity probes bearing different secondary tags were synthesized. Their potency for glycogenolysis was evaluated in primary human liver HL-7702 cells and HepG2 cells. Probe 2d showed the best activity in primary human liver HL-7702 cells and HepG2 cells, with IC50 values of 4.45 μM and 28.49 μM, respectively. Likewise, probe 5d showed IC50 values of 6.46 μM in primary human liver HL-7702 cells and 15.29 μM in HepG2 cells, respectively. Photoaffinity labeling experiments were also performed and protein bands larger than 170 kDa were specifically tagged by probe 2d. The results suggest that the synthesized probe 2d might be a very promising tool for the isolation of the target proteins of BAY R3401.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/94974a8fca7847e79c6ae1d3376b8a0c Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
Nepřihlášeným uživatelům se plný text nezobrazuje	K zobrazení výsledku je třeba se přihlásit.