Three Decades of Targeting Falcipains to Develop Antiplasmodial Agents: What have we Learned and What can be Done Next?

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniversity of Vienna-
Autor(es): dc.contributorCONICET-
Autor(es): dc.contributorUniversidad de San Martín (UNSAM)-
Autor(es): dc.contributorUniversity of Toronto-
Autor(es): dc.contributorUniversidade Federal do Rio de Janeiro (UFRJ)-
Autor(es): dc.creatorGonzález, Jorge Enrique Hernández-
Autor(es): dc.creatorSalas-Sarduy, Emir-
Autor(es): dc.creatorAlvarez, Lilian Hernández-
Autor(es): dc.creatorValiente, Pedro Alberto-
Autor(es): dc.creatorArni, Raghuvir Krishnaswamy-
Autor(es): dc.creatorPascutti, Pedro Geraldo-
Data de aceite: dc.date.accessioned2025-08-21T16:03:16Z-
Data de disponibilização: dc.date.available2025-08-21T16:03:16Z-
Data de envio: dc.date.issued2025-04-29-
Data de envio: dc.date.issued2023-12-31-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.2174/0929867331666230913165219-
Fonte completa do material: dc.identifierhttps://hdl.handle.net/11449/301370-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/301370-
Descrição: dc.descriptionMalaria is a devastating infectious disease that affects large swathes of human populations across the planet’s tropical regions. It is caused by parasites of the genus Plasmodium, with Plasmodium falciparum being responsible for the most lethal form of the disease. During the intraerythrocytic stage in the human hosts, malaria parasites multiply and degrade hemoglobin (Hb) using a battery of proteases, which include two cysteine proteases, falcipains 2 and 3 (FP-2 and FP-3). Due to their role as major hemoglobinases, FP-2 and FP-3 have been targeted in studies aiming to discover new antimalarials and numerous inhibitors with activity against these enzymes, and parasites in culture have been identified. Nonetheless, cross-inhibition of human cysteine cathepsins remains a serious hurdle to overcome for these compounds to be used clinically. In this article, we have reviewed key functional and structural properties of FP-2/3 and described different compound series reported as inhibitors of these proteases during decades of active research in the field. Special attention is also paid to the wide range of computer-aided drug design (CADD) techniques successfully applied to discover new active compounds. Finally, we provide guidelines that, in our understanding, will help advance the rational discovery of new FP-2/3 inhibitors.-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado do Rio de Janeiro (FAPERJ)-
Descrição: dc.descriptionMultiuser Center for Biomolecular Innovation IBILCE/UNESP, SP-
Descrição: dc.descriptionDepartment of Pharmaceutical Sciences UZA II University of Vienna-
Descrição: dc.descriptionInstituto de Investigaciones Biotecnológicas Dr. Rodolfo Ugalde Universidad Nacional de San Martín CONICET, San Martín-
Descrição: dc.descriptionEscuela de Bio y Nanotecnología (EByN) Universidad de San Martín (UNSAM), San Martín-
Descrição: dc.descriptionDonnelly Centre for Cellular & Biomolecular Research University of Toronto-
Descrição: dc.descriptionLaboratório de Modelagem e Dinâmica Molecular Instituto de Biofísica Carlos Chagas Filho Universidade Federal do Rio de Janeiro, RJ-
Descrição: dc.descriptionMultiuser Center for Biomolecular Innovation IBILCE/UNESP, SP-
Formato: dc.format2234-2263-
Idioma: dc.languageen-
Relação: dc.relationCurrent Medicinal Chemistry-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectdrug discovery-
Palavras-chave: dc.subjectFalcipain 2-
Palavras-chave: dc.subjectfalcipain 3-
Palavras-chave: dc.subjectinhibitors-
Palavras-chave: dc.subjectmalaria-
Palavras-chave: dc.subjectPlasmodium falciparum-
Título: dc.titleThree Decades of Targeting Falcipains to Develop Antiplasmodial Agents: What have we Learned and What can be Done Next?-
Tipo de arquivo: dc.typevídeo-
Aparece nas coleções:Repositório Institucional - Unesp

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