Article
Structural determinants of RXPA380, a potent and highly selective inhibitor of the angiotensin-converting enzyme C-domain.
Biochemistry - 29 Jun 2004
Georgiadis Dimitris, Cuniasse Philippe, Cotton Jöel, Yiotakis Athanasios, Dive Vincent
Abstract excerpt
RXPA380 (Cbz-PhePsi[PO(2)CH]Pro-Trp-OH) was reported recently as the first highly selective inhibitor of the C-domain of somatic angiotensin-converting enzyme (ACE), able to differentiate the two active sites of somatic ACE by a selectivity factor of more than 3 orders of magnitude. The contribution of each RXPA380 residue toward this remarkable selectivity was evaluated by studying several analogues of RXPA380....
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