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Screening and Identification of Inhibitors of Trypanosoma brucei Cathepsin L with Antitrypanosomal Activity
Author(s) -
Jefferson Tierra,
McShan Danielle,
Warfield Jasmine,
Ogungbe Ifedayo Victor
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12628
Subject(s) - trypanosoma brucei , african trypanosomiasis , trypanosomiasis , biology , phenotypic screening , identification (biology) , eflornithine , cathepsin l , virtual screening , trypanosoma , computational biology , pharmacology , cathepsin , drug discovery , phenotype , biochemistry , virology , enzyme , gene , spermidine , botany
Current treatment options for human African trypanosomiasis ( HAT ) are ineffective, and they have several well‐known clinical limitations. In our continued efforts to identify chemotypes that can be developed into clinically useful drugs, we screened a targeted compound library against the major cathepsin L (rhodesain) in T. brucei . We report the antirhodesain activity and antitrypanosomal activity of the compounds in this letter. The identified compounds can serve as starting points for structure‐ and/or phenotype‐based lead optimization strategy against Trypanosoma brucei .