title: Antiplasmodial drug targets: a patent review (2000 - 2013).
abstract: BACKGROUND
  New antimalarials with novel modes of action are crucial in countering the challenge of emerging drug-resistant Plasmodium falciparum. Equally significant is the identification and characterization of the targets these compounds inhibit. Biochemical evidence from seminal studies, whole genome clues and high-throughput chemical screening data provide starting points worth exploring in target identification efforts. Several proteins and biochemical processes/pathways critical to parasite survival have since been profiled and patented.
  
  
  METHODS
  In this review, an analysis of patents describing the characterization of different enzymatic and/or biosynthetic targets in P. falciparum over the last fourteen years is presented. The review also details structures, biological evaluation, potential modes of action and therapeutic utilities of small molecule antiplasmodial compounds from ongoing research, designed to inhibit these targets.
  
  
  CONCLUSIONS
  Though various strategies to address antimalarial drug resistance exist, direct inhibition of unrelated targets and non-genome coded processes potentially present the most effective options. Additionally, interest in peptides as antimalarials merits further exploration especially in view of their unique low susceptibility to resistance, wider spectrum of action and faster activity. Finally, target-based optimization and chemical validation of novel targets can be facilitated by routine phenotypic whole-cell screening of antiplasmodial hits against any new target(s).
authors.affiliation: a Department of Chemistry , University of Cape Town , Rondebosch 7701, South Africa.|b South African Medical Research Council Drug Discovery and Development Research Unit , University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: John
authors.initials: J
authors.lastname: Okombo
authors.affiliation: a Department of Chemistry , University of Cape Town , Rondebosch 7701, South Africa.|b South African Medical Research Council Drug Discovery and Development Research Unit , University of Cape Town , Rondebosch 7701, South Africa.|c Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D015195:Drug Design; D004351:Drug Resistance; D057166:High-Throughput Screening Assays / Q000379:methods; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy* / Q000469:parasitology; D058990:Molecular Targeted Therapy; D010330:Patents as Topic; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D000962:Antimalarials
keywords: Plasmodium falciparum; antimalarial peptides; antimalarials; malaria; multiple target inhibition; non-genome coded targets; patent; phenotypic whole cell screening; target identification