Gustavo Capatti Cassiano
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View article: Evaluation of the Activity of 4-Quinolones against Multi-Life Stages of <i>Plasmodium</i> spp.
Evaluation of the Activity of 4-Quinolones against Multi-Life Stages of <i>Plasmodium</i> spp. Open
Malaria is a critical global health problem, with high mortality and morbidity rates, which ultimately hinder socioeconomic development in endemic areas. The evolution of drug resistance in malaria parasites, particularly in the case of
View article: Fluorescent Marinoquinoline Derivative as Inhibitors of <i>Plasmodium falciparum</i> : SAR Analysis, Mode of Action and In Vivo Studies
Fluorescent Marinoquinoline Derivative as Inhibitors of <i>Plasmodium falciparum</i> : SAR Analysis, Mode of Action and In Vivo Studies Open
We present insights into the mechanism of action of marinoquinolines (MQ), a novel class of lead candidates. Using a divergent synthetic approach, we developed a series of 20 new analogues with fluorescence properties. Structure-activity r…
View article: A novel 4-aminoquinoline chemotype with multistage antimalarial activity and lack of cross-resistance with PfCRT and PfMDR1 mutants
A novel 4-aminoquinoline chemotype with multistage antimalarial activity and lack of cross-resistance with PfCRT and PfMDR1 mutants Open
Artemisinin-based combination therapy (ACT) is the mainstay of effective treatment of Plasmodium falciparum malaria. However, the long-term utility of ACTs is imperiled by widespread partial artemisinin resistance in Southeast Asia and its…
View article: Deep Learning-driven research for drug discovery: Tackling Malaria
Deep Learning-driven research for drug discovery: Tackling Malaria Open
Malaria is an infectious disease that affects over 216 million people worldwide, killing over 445,000 patients annually. Due to the constant emergence of parasitic resistance to the current antimalarial drugs, the discovery of new drug can…
View article: QSAR-Driven Design and Discovery of Novel Compounds With Antiplasmodial and Transmission Blocking Activities
QSAR-Driven Design and Discovery of Novel Compounds With Antiplasmodial and Transmission Blocking Activities Open
Malaria is a life-threatening infectious disease caused by parasites of the genus Plasmodium, affecting more than 200 million people worldwide every year and leading to about a half million deaths. Malaria parasites of humans have evolved …
View article: Chalcones as a basis for computer-aided drug design: innovative approaches to tackle malaria
Chalcones as a basis for computer-aided drug design: innovative approaches to tackle malaria Open
Aim: Computer-aided drug design approaches were applied to identify chalcones with antiplasmodial activity. Methodology: The virtual screening was performed as follows: structural standardization of in-house database of chalcones; identifi…
View article: Innovative Multistage ML-QSAR Models for Malaria: From Data to Discovery
Innovative Multistage ML-QSAR Models for Malaria: From Data to Discovery Open
Malaria presents a significant challenge to global public health, with around 247 million cases estimated to occur annually worldwide. The growing resistance of Plasmodium parasites to existing therapies underscores the urgent need …
View article: Whole genome sequencing identifies novel mutations in malaria parasites resistant to artesunate (ATN) and to ATN + mefloquine combination
Whole genome sequencing identifies novel mutations in malaria parasites resistant to artesunate (ATN) and to ATN + mefloquine combination Open
Introduction The global evolution of resistance to Artemisinin-based Combination Therapies (ACTs) by malaria parasites, will severely undermine our ability to control this devastating disease. Methods Here, we have used whole genome sequen…
View article: Mutation in the 26S proteasome regulatory subunit rpn2 gene in Plasmodium falciparum confers resistance to artemisinin
Mutation in the 26S proteasome regulatory subunit rpn2 gene in Plasmodium falciparum confers resistance to artemisinin Open
Introduction Malaria parasites increasingly develop resistance to all drugs available in the market, hampering the goal of reducing malaria burden. Methods Herein, we evaluated the impact of a single-nucleotide variant, E738K, present in t…
View article: Identification of potential inhibitors of casein kinase 2 alpha of <i>Plasmodium falciparum</i> with potent <i>in vitro</i> activity
Identification of potential inhibitors of casein kinase 2 alpha of <i>Plasmodium falciparum</i> with potent <i>in vitro</i> activity Open
Drug resistance to commercially available antimalarials is a major obstacle in malaria control and elimination, creating the need to find new antiparasitic compounds with novel mechanisms of action. The success of kinase inhibitors for onc…
View article: Antimalarial and Cytotoxic Activity of Native Plants Used in Cabo Verde Traditional Medicine
Antimalarial and Cytotoxic Activity of Native Plants Used in Cabo Verde Traditional Medicine Open
Medicinal plants have historically been a source of drugs in multiple applications, including the treatment of malaria infections. The Cabo Verde archipelago harbors a rich diversity of native plants, most of which are used for medicinal p…
View article: Antiplasmodial activity of aurora kinase-2 inhibitor compounds from Plasmodium spp.
Antiplasmodial activity of aurora kinase-2 inhibitor compounds from Plasmodium spp. Open
Anais do GBMeeting: Encontro Anual da Pós Graduação em Genética e Biologia Molecular da UNICAMP (978-85-5722-785-9) - Antiplasmodial Activity Of Aurora Kinase-2 Inhibitor Compounds From Plasmodium Spp.
View article: Studies on the in vitro antiplasmodial activity of endemic and native plants from Cabo Verde
Studies on the in vitro antiplasmodial activity of endemic and native plants from Cabo Verde Open
Background Traditional medicinal plants and other remedies are one of the many potential sources of new antimalarial drugs, there being an increasing interest in studying their potential for the treatment of malaria and other illnesses. Th…
View article: Circumsporozoite Protein from <i>Plasmodium vivax</i> and Its Relationship to Human Malaria
Circumsporozoite Protein from <i>Plasmodium vivax</i> and Its Relationship to Human Malaria Open
The circumsporozoite surface protein (CSP) is the most abundant polypeptide in the sporozoite covering. This protein is involved in the motility and invasion of the sporozoite during its entrance in the hepatocyte. Plasmodium vivax CSP seq…
View article: CYP2D6 Allele Frequency in Five Malaria Vivax Endemic Areas From Brazilian Amazon Region
CYP2D6 Allele Frequency in Five Malaria Vivax Endemic Areas From Brazilian Amazon Region Open
Genetic variability was linked with individual responses to treatment and susceptibility to malaria by Plasmodium vivax . Polymorphisms in the CYP 2D6 gene may modulate enzyme level and activity, thereby affecting individual responses to p…
View article: Violacein-Induced Chaperone System Collapse Underlies Multistage Antiplasmodial Activity
Violacein-Induced Chaperone System Collapse Underlies Multistage Antiplasmodial Activity Open
Antimalarial drugs with novel modes of action and wide therapeutic potential are needed to pave the way for malaria eradication. Violacein is a natural compound known for its biological activity against cancer cells and several pathogens, …
View article: THE POLYMORPHISM RS2234767 (-1377 G>A) IN THE FAS GENE MAY BE ASSOCIATED WITH PLASMODIUM VIVAX INFECTION IN THE BRAZILIAN AMAZON / O POLIMORFISMO RS2234767 (-1377 G>A) NO GENE FAS PODE ESTAR ASSOCIADO À INFECÇÃO POR PLASMODIUM VIVAX NA AMAZÔNIA BRASILEIRA
THE POLYMORPHISM RS2234767 (-1377 G>A) IN THE FAS GENE MAY BE ASSOCIATED WITH PLASMODIUM VIVAX INFECTION IN THE BRAZILIAN AMAZON / O POLIMORFISMO RS2234767 (-1377 G>A) NO GENE FAS PODE ESTAR ASSOCIADO À INFECÇÃO POR PLASMODIUM VIVAX NA AMAZÔNIA BRASILEIRA Open
View article: Correction for Ferreira et al., “Computational Chemogenomics Drug Repositioning Strategy Enables the Discovery of Epirubicin as a New Repurposed Hit for Plasmodium falciparum and P. vivax”
Correction for Ferreira et al., “Computational Chemogenomics Drug Repositioning Strategy Enables the Discovery of Epirubicin as a New Repurposed Hit for Plasmodium falciparum and P. vivax” Open
Volume 64, no. 9, e02041-19, 2020, https://doi.org/10.1128/AAC.02041-19. Page 1: This article was published on 20 August 2020 with a standard copyright line (“© 2020 American Society for Microbiology. All Rights Reserved.”). The authors el…
View article: Polymorphism in the IL-1β promoter is associated with IgG antibody response to circumsporozoite protein repeats of Plasmodium vivax
Polymorphism in the IL-1β promoter is associated with IgG antibody response to circumsporozoite protein repeats of Plasmodium vivax Open
Background It is well established that infection by Plasmodium vivax is a result of host-parasite interactions. In the present study, association with the IL1/IL2 cytokine profiles, anticircumsporozoite protein antibody levels and parasiti…
View article: Computational Chemogenomics Drug Repositioning Strategy Enables the Discovery of Epirubicin as a New Repurposed Hit for Plasmodium falciparum and P. vivax
Computational Chemogenomics Drug Repositioning Strategy Enables the Discovery of Epirubicin as a New Repurposed Hit for Plasmodium falciparum and P. vivax Open
Widespread resistance against antimalarial drugs thwarts current efforts for controlling the disease and urges the discovery of new effective treatments. Drug repositioning is increasingly becoming an attractive strategy since it can reduc…
View article: Deep Learning-driven research for drug discovery: Tackling Malaria
Deep Learning-driven research for drug discovery: Tackling Malaria Open
Malaria is an infectious disease that affects over 216 million people worldwide, killing over 445,000 patients annually. Due to the constant emergence of parasitic resistance to the current antimalarial drugs, the discovery of new drug can…
View article: A new heparan sulfate from the mollusk Nodipecten nodosus inhibits merozoite invasion and disrupts rosetting and cytoadherence of Plasmodium falciparum
A new heparan sulfate from the mollusk Nodipecten nodosus inhibits merozoite invasion and disrupts rosetting and cytoadherence of Plasmodium falciparum Open
BACKGROUND Despite treatment with effective antimalarial drugs, the mortality rate is still high in severe cases of the disease, highlighting the need to find adjunct therapies that can inhibit the adhesion of Plasmodium falciparum-infecte…
View article: Chloroquine and mefloquine resistance profiles are not related to the circumsporozoite protein (CSP) VK210 subtypes in field isolates of Plasmodium vivax from Manaus, Brazilian Amazon
Chloroquine and mefloquine resistance profiles are not related to the circumsporozoite protein (CSP) VK210 subtypes in field isolates of Plasmodium vivax from Manaus, Brazilian Amazon Open
The VK210 variant is the most frequently observed in the studied region and there is significant genetic variability in the CRR of the P. vivax CSP. Moreover, the antimalarial drug sensitivity profiles of the isolates does not seem to be r…
View article: A new heparan sulfate from the mollusk Nodipecten nodosus inhibits merozoite invasion and disrupts rosetting and cytoadherence of Plasmodium falciparum
A new heparan sulfate from the mollusk Nodipecten nodosus inhibits merozoite invasion and disrupts rosetting and cytoadherence of Plasmodium falciparum Open
These findings support a potential use for mollusk HS as adjunct therapy for severe malaria.
View article: Chloroquine and mefloquine resistance profiles are not related to the circumsporozoite protein (CSP) VK210 subtypes in field isolates of Plasmodium vivax from Manaus, Brazilian Amazon
Chloroquine and mefloquine resistance profiles are not related to the circumsporozoite protein (CSP) VK210 subtypes in field isolates of Plasmodium vivax from Manaus, Brazilian Amazon Open
BACKGROUND The central repetitive region (CRR) of the Plasmodium vivax circumsporozoite surface protein (CSP) is composed of a repetitive sequence that is characterised by three variants: VK210, VK247 and P. vivax-like. The most important …
View article: Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies
Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies Open
View article: Genetic sequence characterization and naturally acquired immune response to Plasmodium vivax Rhoptry Neck Protein 2 (PvRON2)
Genetic sequence characterization and naturally acquired immune response to Plasmodium vivax Rhoptry Neck Protein 2 (PvRON2) Open
View article: QSAR-Driven Design and Discovery of Novel Compounds With Antiplasmodial and Transmission Blocking Activities
QSAR-Driven Design and Discovery of Novel Compounds With Antiplasmodial and Transmission Blocking Activities Open
Malaria is a life-threatening infectious disease caused by parasites of the genus Plasmodium, affecting more than 200 million people worldwide every year and leading to about a half million deaths. Malaria parasites of humans have e…
View article: Plasmodium vivax Cell Traversal Protein for Ookinetes and Sporozoites (PvCelTOS) gene sequence and potential epitopes are highly conserved among isolates from different regions of Brazilian Amazon
Plasmodium vivax Cell Traversal Protein for Ookinetes and Sporozoites (PvCelTOS) gene sequence and potential epitopes are highly conserved among isolates from different regions of Brazilian Amazon Open
The Plasmodium vivax Cell-traversal protein for ookinetes and sporozoites (PvCelTOS) plays an important role in the traversal of host cells. Although essential to PvCelTOS progress as a vaccine candidate, its genetic diversity remains unch…
View article: Frequency of Plasmodium vivax circumsporozoite protein genotypes in humans and anopheline mosquitoes in an endemic area of southeastern Pará State, Brazil
Frequency of Plasmodium vivax circumsporozoite protein genotypes in humans and anopheline mosquitoes in an endemic area of southeastern Pará State, Brazil Open
The objective of this study was therefore to investigate the frequency of circumsporozoite protein (CSP) genotypes in human blood and their correlation with parasitemia, as well as to evaluate the presence of these genotypes in Anopheles i…