Discovery and refinement of a new structural class of potent peptide deformylase inhibitors

…, R Alves de Sousa, V Larue, T Cresteil…

Index: Boularot, Adrien; Giglione, Carmela; Petit, Sylvain; Duroc, Yann; De Sousa, Rodolphe Alves; Larue, Valery; Cresteil, Thierry; Dardel, Frederic; Artaud, Isabelle; Meinnel, Thierry Journal of Medicinal Chemistry, 2007 , vol. 50, # 1 p. 10 - 20

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Citation Number: 61

Abstract

New classes of antibiotics are urgently needed to counter increasing levels of pathogen resistance. Peptide deformylase (PDF) was originally selected as a specific bacterial target, but a human homologue, the inhibition of which causes cell death, was recently discovered. We developed a dual-screening strategy for selecting highly effective compounds with low inhibition effect against human PDF. We selected a new scaffold in vitro that discriminated ...