Tsuboi, Katsunori; Bachovchin, Daniel A.; Speers, Anna E.; Spicer, Timothy P.; Fernandez-Vega, Virneliz; Hodder, Peter; Rosen, Hugh; Cravatt, Benjamin F. published the artcile< Potent and Selective Inhibitors of Glutathione S-Transferase Omega 1 That Impair Cancer Drug Resistance>, SDS of cas: 1003-32-3, the main research area is glutathione S transferase omega inhibitor preparation cancer drug resistance; antitumor drug resistance modulator GST omega inhibitor preparation HTS.
Glutathione S-transferases (GSTs) are a superfamily of enzymes that conjugate glutathione to a wide variety of both exogenous and endogenous compounds for biotransformation and/or removal. Glutathione S-transferase omega 1 (GSTO1) is highly expressed in human cancer cells, where it has been suggested to play a role in detoxification of chemotherapeutic agents. Selective inhibitors of GSTO1 are, however, required to test the role that this enzyme plays in cancer and other (patho)physiol. processes. With this goal in mind, we performed a fluorescence polarization activity-based protein profiling (fluopol-ABPP) high-throughput screen (HTS) with GSTO1 and the Mol. Libraries Small Mol. Repository (MLSMR) 300K+ compound library. This screen identified a class of selective and irreversible α-chloroacetamide inhibitors of GSTO1, which were optimized to generate an agent KT53 that inactivates GSTO1 with excellent in vitro (IC50 = 21 nM) and in situ (IC50 = 35 nM) potency. Cancer cells treated with KT53 show heightened sensitivity to the cytotoxic effects of cisplatin, supporting a role for GSTO1 in chemotherapy resistance.
Journal of the American Chemical Society published new progress about Antitumor agent resistance. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, SDS of cas: 1003-32-3.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica