While hydrogen sulfide (H2S) is most often known for its distinctive odor and toxicity, this gaseous small molecule also plays important roles in human biology. Though the exact mechanisms are still being investigated, H2S has a wide range of effects depending on its concentration, location, and target and appears to be especially important in the inflammatory, nervous, and cardiovascular systems. Hydrogen sulfide is produced in vivo through many different pathways with two predominant H2S- producing enzymes being cystathionine �-synthase (CBS) and cystathionine ?-lyase (CGL). In particular CBS plays a key role in homocysteine homeostasis, catalyzing the first step in the conversion of toxic homocysteine to cysteine. Aberrant CBS activity has been implicated in a variety of diseases, including Down's Syndrome, hypertension, preeclampsia, and homocystinuria. Our overall goal in this project has been to discover new inhibitors and activators of these H2S-producing enzymes that can be used both to elucidate the roles they play in human health and disease and also as potential therapeutics for those with a CBS-related disorder. To this end, we have developed fluorogenic H2S selective probes and used these probes to screen for potent and selective inhibitors of CBS and CGL.

Novel hydrogen-sulfide selective probes for the study of hydrogen sulfide-producing enzymes

247th National Meeting (2014)

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