Agonist genistein

Phytoestrogens Isoflavones genistein ER/1, ERa" 3 Agonist Induces vitellogenin expression,... 

Adrenergic receptor Quercetin Genistein Rats C2C12 cells Canine ventricular myocardium a2- agonist ot - agonist 3- agonist Kaur et ah, 2007 Jou et ah, 2004 Chu et ah, 2005... 

Genistein has been considered the primary anticancer constituent in soy, based on putative in vitro activities that include its ability to inhibit topoisomerase I and II activity, inhibit protein tyrosine phosphorylation, induce differentiation of cancer cell lines, and act as an estrogen agonist. 

Genistein (GEN Fig. 1.11a) is an isoflavonoid natural product that is an ER- selective partial agonist. The structure of the complex between human ER-y5 and genistein has been reported (PDB entry IGKM) [11]. GEN binds across the ligand-binding cavity in a manner similar to estradiol with ER-a. The A-ring phenol of GEN inter-... 

Tyrosine kinases have been implicated in Ca +-sensitization largely as the result of the inhibitory effects of tyrosine kinase inhibitors, genistein and vanadate, and the correlation between tyrosine phosphorylation and vanadate- or agonist-induced contractions (Di Salvo et al. 1993a,b, 1994, 1997 Steusloff et al. 1995). However, the tyrosine-phosphorylated proteins have yet to be directly linked to a known contractile regulatory mechanism i.e., MLCK, SMPP-IM) and evaluation of the relationships between tyrosine phosphorylation and modulation of Ca +-sensitization of contraction in intact muscle is somewhat complicated by concurrent changes in cytosolic Ca (Di Salvo et al. 1994,1997), possibly as the result of activation of PLC-y (Marrero et al. 1994) or Gaq.n (Umemori et al. 1997). 

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