Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors.
Angiotensin-converting enzyme-related carboxypeptidase (ACE2) is a recently identified zinc metalloprotease with carboxypeptidase activity that was identified using our genomics platform. We implemented a rational design approach to identify potent and selective ACE2 inhibitors. To this end, picomolar inhibitors of ACE2 were designed and synthesized.
D000085962:Angiotensin-Converting Enzyme 2; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002268:Carboxypeptidases / Q000037:antagonists & inhibitors*; D002384:Catalysis; D015195:Drug Design; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007703:Peptidyl-Dipeptidase A; D017434:Protein Structure, Tertiary; D013329:Structure-Activity Relationship; D013386:Succinates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000806:Angiotensin-Converting Enzyme Inhibitors; D007093:Imidazoles; D013386:Succinates; C000249:benzylsuccinic acid; D002268:Carboxypeptidases; D007703:Peptidyl-Dipeptidase A; D000085962:Angiotensin-Converting Enzyme 2