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The Natural Product Cyclomarin Kills Mycobacterium Tuberculosis by Targeting the ClpC1 Subunit of the Caseinolytic Protease
Author(s) -
Schmitt Esther K.,
Riwanto Meliana,
Sambandamurthy Vasan,
Roggo Silvio,
Miault Charlotte,
Zwingelstein Christian,
Krastel Philipp,
Noble Christian,
Beer David,
Rao Srinivasa P. S.,
Au Melvin,
Niyomrattanakit Pornwaratt,
Lim Viviam,
Zheng Jun,
Jeffery Douglas,
Pethe Kevin,
Camacho Luis R.
Publication year - 2011
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201101740
Subject(s) - protease , protein subunit , mycobacterium tuberculosis , proteolysis , biology , computational biology , natural product , tuberculosis , drug discovery , microbiology and biotechnology , genetics , bioinformatics , biochemistry , enzyme , medicine , gene , pathology
Target practice : The target of the antibiotic cyclomarin A was identified in Mycobacterium. Cyclomarin A (see structure) binds the regulatory subunit of the Clp protease complex with high affinity resulting in elevated proteolysis and cell death. The property of cyclomarin to kill both growing and nonreplicating mycobacteria makes the Clp protease a promising target for antitubercular drug discovery.