Schaeffer, M., Schroeder, J., Heckeroth, A.R., Noack, S., Gassel, M., Mottram, J.C. , Selzer, P.M. and Coombs, G.H. (2012) Identification of lead compounds targeting the cathepsin B-like enzyme of Eimeria tenella. Antimicrobial Agents and Chemotherapy, 53(3), pp. 1190-1201. (doi: 10.1128/AAC.05528-11)
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Publisher's URL: http://dx.doi.org/10.1128/AAC.05528-11
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: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Selzer, Dr Paul and Coombs, Professor Graham and Mottram, Professor Jeremy |
| Authors: | Schaeffer, M., Schroeder, J., Heckeroth, A.R., Noack, S., Gassel, M., Mottram, J.C., Selzer, P.M., and Coombs, G.H. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Infection & Immunity College of Medical Veterinary and Life Sciences > School of Life Sciences |
| Journal Name: | Antimicrobial Agents and Chemotherapy |
| ISSN: | 0066-4804 |
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