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Water Bridges Play a Key Role in Affinity and Selectivity for Malarial Protease Falcipain-2
(Amer Chemical Soc, 2020-11-23)
Falcipain-2 (FP-2) is hemoglobinase considered an attractive drug target of Plasmodium falciparum. Recently, it has been shown that peptidomimetic nitriles containing a 3-pyridyl (3Pyr) moiety at P2 display high affinity ...
Prediction of Noncompetitive Inhibitor Binding Mode Reveals Promising Site for Allosteric Modulation of Falcipain-2
(Amer Chemical Soc, 2019-08-29)
Falcipain-2 (FP-2) is a Plasmodium falciparum cysteine protease that has been extensively targeted to identify novel antimalarials. Remarkably, previous reports have shown that FP-2 can be allosterically modulated and, for ...
Tetracycline Derivatives Inhibit Plasmodial Cysteine Protease Falcipain-2 through Binding to a Distal Allosteric Site
(2022-01-10)
Allosteric inhibitors regulate enzyme activity from remote and usually specific pockets. As they promise an avenue for less toxic and safer drugs, the identification and characterization of allosteric inhibitors has gained ...
Computational strategies for selective inhibition of falcipain-2
(Universidade Estadual Paulista (Unesp), 2020-02-14)
A falcipaína-2 (FP-2) é uma hemoglobinase chave do Plasmodium falciparum, frequentemente selecionada como alvo para o planejamento de fármacos antimaláricos. Apesar dos esforços, nenhum inibidor da FP-2 tem entrado em fase ...
Identification of (4-(9H-fluoren-9-yl) piperazin-1-yl) methanone derivatives as falcipain 2 inhibitors active against Plasmodium falciparum cultures
(ElsevierGrupo MalariaAmsterdam, Paises Bajos, 2022)
Characterization of a papain-like cysteine protease essential for the survival of Babesia ovis merozoites
(2016)
Babesia ovis, a tick-transmitted intraerythrocytic protozoan parasite, causes severe infections in small ruminants from Southern Europe, Middle East, and Northern Africa. With the aim of finding potential targets for the ...
In silico-guided drug repurposing: identification of non-competitive inhibitors of Trypanosoma cruzi and Plasmodium falciparum cysteine proteases
(Fundación Revista Medicina, 2020)
Abstract/Resumen: Trypanosoma cruzi and Plasmodium falciparum are the etiologic agents of Chagas disease and Malaria, respectively. Cysteine proteases play key roles in the pathogenesis and survival of these parasites, ...