title: Drugging the Plasmodium kinome: the benefits of academia-industry synergy.
abstract: Malaria remains a major killer in many parts of the world. Recently, the development of nonprofit organisations aimed at fighting this deadly scourge incited academic and industrial scientists to merge their expertise in drug-target validation and lead discovery. Expectations are clear: identification and characterisation of new molecules showing high efficacy, low toxicity and little propensity to induce resistance in the parasite. In this context, protein kinase inhibitors represent an attractive possibility. Here, we compare traditional target-based drug-discovery approaches with innovative exploratory paths (parallel screening, cell-based assays, integrated systems biology and allosteric inhibition) and discuss the benefits of acadaemia-industry cooperation. Early characterisation of distribution, metabolism, pharmacokinetic (DMPK) and toxicology parameters are considered as well.
authors.affiliation: Merck-Serono International S.A., Geneva Research Center, 9, Chemin des Mines, Case postale 54, CH-1211 Genève 20, Switzerland. didier.leroy@merckserono.net
authors.forename: Didier
authors.initials: D
authors.lastname: Leroy
authors.forename: Christian
authors.initials: C
authors.lastname: Doerig
mesh_terms: D000047:Academies and Institutes; D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D035843:Biomedical Research / Q000639:trends; D015195:Drug Design; D004345:Drug Industry; D004351:Drug Resistance; D018503:Genome, Protozoan; D006801:Humans; D007400:Interprofessional Relations; D016778:Malaria, Falciparum / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology / Q000235:genetics; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D011494:Protein Kinases / Q000235:genetics* / Q000378:metabolism
chemical_list: D000962:Antimalarials; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases