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Identification of lead compounds targeting the cathepsin B-like enzyme of Eimeria tenella

Schaeffer, Marie and Schroeder, Joerg and Heckeroth, Anja R and Noack, Sandra and Gassel, Michael and Mottram, Jeremy C and Selzer, Paul M and Coombs, Graham H (2011) Identification of lead compounds targeting the cathepsin B-like enzyme of Eimeria tenella. Antimicrobial Agents and Chemotherapy. ISSN 1098-6596

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Abstract

Cysteine peptidases have been implicated in the development and pathogenesis of Eimeria. We have identified a single copy cathepsin B-like cysteine peptidase (EtCatB) gene in the genome database of Eimeria tenella. Molecular modeling of the predicted protein suggested that it differs significantly from host enzymes and could be a good drug target. EtCatB was expressed and secreted as a soluble, active, glycosylated mature enzyme from Pichia pastoris. Biochemical characterisation of the recombinant enzyme confirmed that it is cathepsin B-like. Screening of a focused library against the enzyme identified three inhibitors (a nitrile, a thiosemicarbazone and an oxazolon) that can be used as leads for novel drug discovery against Eimeria. The oxazolone scaffold is a novel cysteine peptidase inhibitor, it may thus find widespread use.

Item type: Article
ID code: 36360
Keywords: lead compounds , cathepsin B-like enzyme , Eimeria tenella, Therapeutics. Pharmacology, Infectious Diseases, Pharmacology, Pharmacology (medical)
Subjects: Medicine > Therapeutics. Pharmacology
Department: Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
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Depositing user: Pure Administrator
Date Deposited: 08 Dec 2011 09:31
Last modified: 27 Mar 2014 09:53
URI: http://strathprints.strath.ac.uk/id/eprint/36360

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