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The Potent Antiplasmodial Calmodulin-Antagonist Trifluoperazine Inhibits Plasmodium falciparum Calcium-Dependent Protein Kinase 4

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Due to their critical involvement in the execution of the malaria parasite developmental pattern both in the mosquito vector and in the human host, Plasmodium calcium-dependent protein kinases (CDPKs) are considered promising candidates for the development of new tools to block malaria transmission. We report here that the phenothiazine trifluoperazine non-competitively inhibits Plasmodium falciparum CDPK4 in the micromolar range while other calmodulin antagonists only marginally affect the enzyme activity, and we propose the inhibition mechanism. Our results demonstrate that selective enzyme inhibition is achievable by targeting its calmodulin-like domain. This observation could be exploited for the discovery of innovative phenothiazine-based CDPK inhibitors of potential medical interest.

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Keywords: AMP; CDPKs; CaM-LD; EDTA; FPLC; Pf-HisCDPK4; Plasmodium falciparum; RFU; Subcloning; TFP; Thermal melt/thermal shift assays; antimalaria drug discovery; calmodulin antagonists; malaria; protein kinases

Document Type: Research Article

Publication date: 2011-12-01

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  • Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.
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