The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Studies on Novel Bacterial Translocase I Inhibitors, A-500359s
II. Biological Activities of A-500359 A, C, D and G
YASUNORI MURAMATSUMICHIKO MIYAZAWA ISHIIMASATOSHI INUKAI
Author information
JOURNALS FREE ACCESS

2003 Volume 56 Issue 3 Pages 253-258

Details
Abstract

A-500359 A, C, D, G and capuramycin inhibited bacterial phospho-N-acetylmuramyl-pentapeptide-translocase (translocase I: EC 2.7.8.13) with IC50 values of 0.017, 0.12, 0.53, 0.14 and 0.018μM, respectively. Consistently, A-500359 A, C and capuramycin inhibited in vitro peptidoglycan biosynthesis. A-500359 A exhibited reversible inhibition, which was mixed type and noncompetitive with respect to UDP-MurNAc-(Nε-Dns)pentapeptide (Ki=0.0079μM) and undecaprenyl-phosphate, respectively. A-500359 A, C, D and G showed antimicrobial activity against Mycobacterium smegmatis. As a single intravenous injection of A-500359 A at a dose of 500mg/kg showed no toxicity in mice, it was suggested that the capuramycin derivatives might become candidates as novel therapeutic agents for various diseases caused by Mycobacteria including tuberculosis.

Information related to the author
© Japan Antibiotics Research Association
Previous article Next article
feedback
Top