PMID: 9186562Apr 1, 1997Paper

Antimicrobial activities of chemically modified thiazolyl peptide antibiotic MDL 62,879 (GE2270A)

The Journal of Antibiotics
S LociuroR Ciabatti

Abstract

MDL 62,879 (GE2270A) 1 is a new inhibitor of elongation factor-Tu (EF-Tu) and belongs to the class of thiazolyl peptide antibiotics. Controlled acid hydrolysis of 1 followed by treatment with base resulted in the lost of the two terminal amino acids and in the formation of water-soluble MDL 62,935 2. Although less active in vitro than its parent compound, 2 was able to inhibit by 50% an Escherichia coli cell-free protein synthesis system at roughly the same concentration of 1. MDL 62,935 2 was subjected to further modification at the beta-phenylserine residue. Derivatives obtained from 2 were less active in both antimicrobial (MIC) and enzymatic (IC50) assays. This suggests that beta-phenylserine plays an important role for the inhibition of EF-Tu by 1 and 2.

Citations

May 28, 2014·Angewandte Chemie·Xavier Just-BaringoMercedes Álvarez
Jun 5, 2010·The Journal of Biological Chemistry·Christopher T WalshAlbert A Bowers
Jul 6, 2014·The Journal of Antibiotics·Koteppa PariH Sivaramakrishnan
Jul 23, 2020·Cell Chemical Biology·Alexander A Vinogradov, Hiroaki Suga

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