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In silico Guided Drug Repurposing: Discovery of New Competitive and Non-competitive Inhibitors of Falcipain-2
(Frontiers Media S.A., 2019-08-06)
Malaria is among the leading causes of death worldwide. The emergence of Plasmodium falciparum resistant strains with reduced sensitivity to the first line combination therapy and suboptimal responses to insecticides used ...
In silico identification of noncompetitive inhibitors targeting an uncharacterized allosteric site of falcipain-2
(2021-01-01)
Falcipain-2 (FP-2) is a Plasmodium falciparum hemoglobinase widely targeted in the search for antimalarials. FP-2 can be allosterically modulated by various noncompetitive inhibitors that have been serendipitously identified. ...
Predicting binding modes of reversible peptide-based inhibitors of falcipain-2 consistent with structure-activity relationships
(Wiley-Blackwell, 2017-09-01)
Falcipain-2 ( FP-2) is a major hemoglobinase of Plasmodium falciparum, considered an important drug target for the development of antimalarials. A previous study reported a novel series of 20 reversible peptide-based ...
Synthetic compounds from an in house library as inhibitors of falcipain-2 from Plasmodium falciparum
(Taylor & Francis Ltd, 2015-02)
Falcipain-2 (FP-2) is a key cysteine protease from the malaria parasite Plasmodium falciparum. Many previous studies have identified FP-2 inhibitors; however, none has yet met the criteria for an antimalarial drug candidate. ...
Inhibition of Plasmodium falciparum cysteine proteases by the sugarcane cystatin CaneCPI-4
(Elsevier Ireland Ltd, 2018)
Malaria is a disease caused by Plasmodium parasites that affects hundreds of millions of people. Plasmodium proteases are involved in invasion, erythrocyte egress and degradation of host proteins. Falcipains are well studied ...
Identification of (4-(9H-fluoren-9-yl) piperazin-1-yl) methanone derivatives as falcipain 2 inhibitors active against Plasmodium falciparum cultures
(Elsevier Science, 2018-12)
Background: Falcipain 2 (FP-2) is the hemoglobin-degrading cysteine protease of Plasmodium falciparum most extensively targeted to develop novel antimalarials. However, no commercial antimalarial drugs based on FP-2 ...
Identification of (4-(9H-fluoren-9-yl) piperazin-1-yl) methanone derivatives as falcipain 2 inhibitors active against Plasmodium falciparum cultures
(2018-12-01)
Background: Falcipain 2 (FP-2) is the hemoglobin-degrading cysteine protease of Plasmodium falciparum most extensively targeted to develop novel antimalarials. However, no commercial antimalarial drugs based on FP-2 ...
Discovery of novel falcipain 2 inhibitors by in silico guided drug repositioning
(University of Dundee, 2019)
Malaria is a life-threatening condition that continues being one of global leading causes of death worldwide, being themain cause of death globally in the 5-14 year-old population. The disease is caused by parasites from ...