title: Stability of new carbapenem DA-1131 to renal dipeptidase (dehydropeptidase I).
abstract: The stability of DA-1131 to renal dipeptidase (RDPase) (EC 3.4.13.19) was compared with that of imipenem and meropenem by V(max)/K(m) ratios as an index of the enzyme's preference for substrates. Our results showed a decreasing order of imipenem (6.24), meropenem (2.41), and DA-1131 (1.39). The biochemical evaluation of DA-1131 as the least preferred substrate of RDPase suggests its potential use as a novel beta-lactam antibiotic which may be usable without coadministration of RDPase inhibitors once its clinical suitability is proven.
authors.affiliation: Department of Pharmacy, College of Pharmacy, Chonnam National University, Kwangju, Korea.
authors.forename: Sung Wook
authors.initials: SW
authors.lastname: Park
authors.forename: Jeoung Soon
authors.initials: JS
authors.lastname: We
authors.forename: Gye Won
authors.initials: GW
authors.lastname: Kim
authors.forename: Seong Hak
authors.initials: SH
authors.lastname: Choi
authors.forename: Haeng Soon
authors.initials: HS
authors.lastname: Park
mesh_terms: D000818:Animals; D015780:Carbapenems / Q000494:pharmacology*; D004150:Dipeptidases / Q000187:drug effects / Q000378:metabolism*; D004795:Enzyme Stability / Q000187:drug effects; D015378:Imipenem / Q000494:pharmacology; D000077731:Meropenem; D013379:Substrate Specificity / Q000187:drug effects; D013845:Thienamycins / Q000494:pharmacology
chemical_list: D015780:Carbapenems; C099230:DA 1131; D013845:Thienamycins; D015378:Imipenem; D004150:Dipeptidases; C038937:dipeptidase; D000077731:Meropenem