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Chapter 4

Human Targets Repositioning and Cell-based Approaches for Antimalarial Discovery

This chapter consists of two major areas highlighting successes and opportunities for improvement: first, the use of targeted human therapeutics against malaria parasite proliferation and second, the use of cell-based assays to find novel antimalarials. The first part of the chapter will describe the use of compounds from major human therapeutic targets, namely farnasyltranferase, histone deacetylase, protein kinase, and protease inhibitors. Compounds from the highly successful human target classes have been investigated as treatment methods for plasmodium infections and some interesting leads from medicinal chemistry optimization will be described. As a complimentary approach, the second part of this chapter describes cell-based screening as a method to generate novel antimalarial drugs. Traditionally demonstrated as a highly successful approach to anti-infectives, this part of the chapter outline new methods for high-throughput screening, hit triaging and subsequent methods available to determine mechanism of action, including recent examples in the literature.

Print publication date: 04 Nov 2011
Copyright year: 2012
Print ISBN: 978-1-84973-192-8
PDF eISBN: 978-1-84973-349-6
From the book series:
RSC Drug Discovery