Protease Inhibitors
Mostrando 1-12 de 1019 artigos, teses e dissertações.
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1. OTIMIZAÇÃO E VALIDAÇÃO DE MÉTODO ENZIMÁTICO SEMIQUANTITATIVO SIMPLES E DE BAIXO CUSTO PARA A BUSCA DE INIBIDORES DE CISTEINO PROTEASES
Cysteine proteases are an important class of enzymes involved in several essential biological processes. For this reason, these enzymes are important therapeutic targets, and therefore can be used in enzymatic assays for the search of hits. The most widely used methods in the search of enzyme inhibitors are spectrophotometric, however they have relatively hi
Quím. Nova. Publicado em: 2021-04
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2. Identification of Potential Inhibitors of Severe Acute Respiratory Syndrome-Related Coronavirus 2 (SARS-CoV-2) Main Protease from Non-Natural and Natural Sources: A Molecular Docking Study
So far, there is neither a vaccine nor a specific antiviral drug to prevent or treat COVID-19 (coronavirus disease) infection. Recent studies have been done to investigate the capacity of human immunodeficiency virus type 1 (HIV-1) protease inhibitors be used in the treatment of COVID-19 patients. Some of those drugs have shown to be promising. Natural chemi
J. Braz. Chem. Soc.. Publicado em: 2020-12
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3. New Synthetic Quinolines as Cathepsin K Inhibitors
Cathepsin K is a papain-like cysteine protease and is responsible for collagen degradation in bone tissue and thus represents an important target for the development of new therapies for treating diseases such as osteoporosis. Quinolines are an important class of heterocyclic molecular leads with a great pharmacological potential and represent a relevant sca
J. Braz. Chem. Soc.. Publicado em: 2020-08
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4. Inflammatory Biomarkers and Carotid Thickness in HIV Infected Patients under Antiretroviral Therapy, Undetectable HIV-1 Viral Load, and Low Cardiovascular Risk
Resumo Fundamento: As pessoas que vivem com HIV têm um risco aumentado de doença cardiovascular e espessamento da carótida, devido à inflamação causada pelo vírus, à terapia antirretroviral e a outros fatores de risco. No entanto, poucos estudos observaram a ocorrência de doenças cardiovasculares e espessamento carotídeo na população soropositi
Arq. Bras. Cardiol.. Publicado em: 28/10/2019
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5. VDR polymorphisms influence immunological response in HIV-1+ individuals undergoing antiretroviral therapy
Abstract Vitamin D exerts an immuno-modulatory activity on several immune system cells through the vitamin D receptor (VDR). Herein, we verified that age and a therapeutic regimen containing protease inhibitors are associated with failures in antiretroviral therapies (ARVs). In addition, we assessed whether a VDR SNP (rs11568820: C allele and CC genotype) an
Genet. Mol. Biol.. Publicado em: 27/06/2019
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6. Risk factors for cardiovascular disease in HIV/AIDS patients treated with highly active antiretroviral therapy (HAART) in the central-southern region of the state of Paraná – Brazil
Resumo O objetivo deste estudo foi descrever os fatores de risco cardiovascular em pacientes HIV/AIDS de acordo com o esquema terapêutico utilizado. Estudo de Coorte retrospectiva no período de 2002 a 2014. Foram levantadas variáveis clínicas e esquema de tratamento de 538 indivíduos. Utilizaram-se medidas de tendência central, e regressão marginal lo
Ciênc. saúde coletiva. Publicado em: 30/05/2019
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7. Kn-Ba: a novel serine protease isolated from Bitis arietans snake venom with fibrinogenolytic and kinin-releasing activities
Abstract Background: Bitis arietans is a venomous snake found in sub-Saharan Africa and in parts of Morocco and Saudi Arabia. The envenomation is characterized by local and systemic reactions including pain, blistering, edema and tissue damage, besides hemostatic and cardiovascular disturbances, which can cause death or permanent disabilities in its victims
J. Venom. Anim. Toxins incl. Trop. Dis. Publicado em: 24/01/2019
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8. Protease inhibitory, insecticidal and deterrent effects of the trypsin-inhibitor benzamidine on the velvetbean caterpillar in soybean
Abstract The recognition of protease inhibitors with insecticidal activity is important as a basis for the development of mimetic peptides with potential use as biorational insecticides. We sprayed benzamidine on soybean plants and assessed whether this potent synthetic trypsin-inhibitor has protease inhibitory, insecticidal and deterrent effects on the velv
An. Acad. Bras. Ciênc.. Publicado em: 18/10/2018
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9. Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents
ABSTRACT In the search for new anti-schistosomal agents, a series of fifteen ortho-nitrobenzyl derivatives was assayed in vitro against both the schistosomulum (somule) and adult forms of Schistosoma mansoni. Compounds 8 and 12 showed significant activity against somules at low micromolar concentrations, but none was active against adults. The SAR demonstrat
Braz. J. Pharm. Sci.. Publicado em: 26/07/2018
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10. Hepatitis C in Brazil: lessons learned with boceprevir and telaprevir
ABSTRACT In 2012, the first-generation protease inhibitors telaprevir (TVR) and boceprevir (BOC) were introduced in the Brazilian health system for treatment of chronic hepatitis C, after their approval by the National Committee for Health Technology Incorporation (CONITEC). However, these medicines were discontinued in 2015. The short period of use in thera
Rev. Inst. Med. trop. S. Paulo. Publicado em: 28/06/2018
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11. First-wave protease inhibitors for hepatitis C genotype 1 treatment: a real-life experience in Brazilian patients
Abstract INTRODUCTION: Licensed for chronic hepatitis C treatment in 2011, the protease inhibitors (PIs) telaprevir (TVR) and boceprevir (BOC), which have high sustained viral responses (SVR), ushered a new era characterized by the development of direct-action drugs against the hepatitis C virus (HCV). The aim of this study was to analyze the effectiveness
Rev. Soc. Bras. Med. Trop.. Publicado em: 2018-04
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12. An in silico Study of Benzophenone Derivatives as Potential Non-Competitive Inhibitors of Trypanosoma cruzi and Leishmania Amazonensis Cysteine Proteinases
This study investigates the mechanisms of interaction between benzophenone derivatives and cruzain and Llacys1 (the protein expressed by cysteine protease gene isoform 1 of L. amazonensis) by homology modelling, docking and molecular dynamics simulation. The results predict that the same binding site in cruzain and Llacys1 is involved in complexes with benzo
J. Braz. Chem. Soc.. Publicado em: 2018-03