Human CYP2C19 Substrate and Inhibitor Characterization of Organophosphate Pesticides.
| Autor: | Vignaux PA; Collaborations Pharmaceuticals, Inc., Raleigh, North Carolina 27606, United States., Shriwas P; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Revnew A; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Agarwal G; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Lane TR; Collaborations Pharmaceuticals, Inc., Raleigh, North Carolina 27606, United States., McElroy CA; Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States., Ekins S; Collaborations Pharmaceuticals, Inc., Raleigh, North Carolina 27606, United States. |
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| Jazyk: | angličtina |
| Zdroj: | Chemical research in toxicology [Chem Res Toxicol] 2023 Sep 18; Vol. 36 (9), pp. 1451-1455. Date of Electronic Publication: 2023 Aug 31. |
| DOI: | 10.1021/acs.chemrestox.3c00188 |
| Abstrakt: | CYP2C19 is an important enzyme for organophosphate pesticide (OPP) metabolism. Because the OPPs can be both substrates and inhibitors of CYP2C19, we screened 45 OPPs for their ability to inhibit the activity of this enzyme and investigated the role of CYP2C19 in the metabolism of 22 of these molecules. We identified several nanomolar inhibitors of CYP2C19 as well as determined that thions, in general, are more potent inhibitors than oxons. We also determined that thions are readily metabolized by CYP2C19, although we saw no relationship between IC |
| Databáze: | MEDLINE |
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