New Opportunities in the Structure-based Design of Anti-Protozoan Agents

Author(s): James A. Gordon, Colin W.G. Fishwick, Martin J. McPhillie

Journal Name: Current Topics in Medicinal Chemistry

Volume 17 , Issue 1 , 2017

Become EABM
Become Reviewer
Call for Editor

Graphical Abstract:


Since the recent renaissance of phenotypic screening in the field of protozoan drug discovery, is there still an opportunity for the structure-based design of new anti-protozoan agents? Target-based approaches should be used in parallel to phenotypic screening to strengthen the pipeline of anti-protozoan agents. We give an overview of the protozoan drug discovery landscape highlighting four protein targets of interest: cytochrome bc1, dihydroorotate dehydrogenase, dihydrofolate reductase and calcium-dependent protein kinase 1. We discuss recent structurebased design efforts to inhibit these targets, reviewing their crystal structures and their ability to accommodate potent and selective compounds. Finally, we discuss future opportunities to apply structure-based methods to promising molecular targets within protozoan parasites discovered using chemical genomics.

Keywords: Apicomplexan drug discovery, CDPK1, Cytochrome bc1, DHFR, DHODH, Structure-based design.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2017
Page: [79 - 90]
Pages: 12
DOI: 10.2174/1568026616666160719164542
Price: $65

Article Metrics

PDF: 40
PRC: 1