Factors influencing the specificity of inhibitor binding to the human and malaria parasite dihydroorotate dehydrogenases

…, GA McConkey, CWG Fishwick…

Index: Davies, Matthew; Heikkilae, Timo; McConkey, Glenn A.; Fishwick, Colin W. G.; Parsons, Mark R.; Johnson, A. Peter Journal of Medicinal Chemistry, 2009 , vol. 52, # 9 p. 2683 - 2693

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Citation Number: 25

Abstract

The de novo pyrimidine biosynthesis enzyme dihydroorotate dehydrogenase is an emerging drug target for the treatment of malaria. In this context a key property of Plasmodium falciparum DHODH (Pf DHODH) is that it can be selectively inhibited over its human homologue (Hs DHODH). However, Hs DHODH is also a validated drug target for autoimmune diseases such as arthritis. Here a series of novel inhibitors is described that ...

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