Small-molecule inhibitor: MK351A

Summary Literature

Name

Common name: MK351A
Other names: 351A

Inhibition

History: MK135A is a p-hydroxybenzamidine derivative of N-(1-carboxy-3-phenylpropyl)-L-lysyl-L-proline (lisinopril). It is easily labeled with radioiodine, and because of this has been much used in laboratory studies of angiotensin-converting enzyme compound peptidase.
Peptidases inhibited: Angiotensin-converting enzyme compound peptidase
Mechanism: Reversible.

Chemistry

CID at PubChem: 122144
Structure
Formula weight: 525

General

Inhibitor class: This is a compound in the carboxylate class of reversible metallopeptidase inhibitors. In these, the active site zinc of the enzyme is generally coordinated by a carboxylate of the inhibitor, and this interaction contributes to inhibitory potency. Reviewed by Patchett & Cordes (1985) and Powers & Harper (1986), pp. 268 - 277 (who provide a table of K_i values).