Design, synthesis and in vitro biological evaluation of oligopeptides targeting E. coli type I signal peptidase (LepB).

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De Rosa M, Lu L, Zamaratski E, Szałaj N, Cao S, Wadensten H, Lenhammar L, Gising J, Roos AK, Huseby DL, Larsson R, Andrén PE, Hughes D, Brandt P, Mowbray SL, Karlén A

Bioorg. Med. Chem. 25 (3) 897-911 [2017-02-01; online 2016-12-07]

Type I signal peptidases are potential targets for the development of new antibacterial agents. Here we report finding potent inhibitors of E. coli type I signal peptidase (LepB), by optimizing a previously reported hit compound, decanoyl-PTANA-CHO, through modifications at the N- and C-termini. Good improvements of inhibitory potency were obtained, with IC

Affiliated researcher

PubMed 28038943

DOI 10.1016/j.bmc.2016.12.003

Crossref 10.1016/j.bmc.2016.12.003

pii: S0968-0896(16)31360-8