Targeted Covalent Inhibition of <i>Plasmodium</i> FK506 Binding Protein 35
Thomas C. Atack, D.D. Raymond, Christa Blomquist, Charisse Flerida A. Pasaje, Patrick McCarren, Jamie A. Moroco, Henock B. Befekadu, Foxy P. Robinson, Debjani Pal, Lisl Y. Esherick, Alessandra Ianari, Jacquin C. Niles, William R. Sellers
Abstract
FKBP35. Here, we synthesize inhibitors of FKBP35, show that they directly bind FKBP35 in a model cellular setting, selectively covalently modify C106, and exhibit antiplasmodium activity in blood-stage cultured parasites.
Topics & Concepts
Plasmodium falciparumFKBPCovalent bindingCovalent bondCysteinePlasma protein bindingChemistryBiochemistryEnzymeBinding siteBinding affinitiesComputational biologyBiologyMalariaReceptorOrganic chemistryImmunologySignaling Pathways in DiseaseTrypanosoma species research and implicationsResearch on Leishmaniasis Studies