[HTML][HTML] Antimalarial drug discovery—approaches and progress towards new medicines
EL Flannery, AK Chatterjee, EA Winzeler - Nature Reviews Microbiology, 2013 - nature.com
Malaria elimination has recently been reinstated as a global health priority but current
therapies seem to be insufficient for the task. Elimination efforts require new drug classes …
therapies seem to be insufficient for the task. Elimination efforts require new drug classes …
Antiviral and antimicrobial nucleoside derivatives: structural features and mechanisms of action
AA Zenchenko, MS Drenichev, IA Il'Icheva… - Molecular biology, 2021 - Springer
The emergence of new viruses and resistant strains of pathogenic microorganisms has
become a powerful stimulus in the search for new drugs. Nucleosides are a promising class …
become a powerful stimulus in the search for new drugs. Nucleosides are a promising class …
Identifying purine nucleoside phosphorylase as the target of quinine using cellular thermal shift assay
Mechanisms of action (MoAs) have been elusive for most antimalarial drugs in clinical use.
Decreasing responsiveness to antimalarial treatments stresses the need for a better …
Decreasing responsiveness to antimalarial treatments stresses the need for a better …
[HTML][HTML] Drug targets for resistant malaria: historic to future perspectives
New antimalarial targets are the prime need for the discovery of potent drug candidates. In
order to fulfill this objective, antimalarial drug researches are focusing on promising targets …
order to fulfill this objective, antimalarial drug researches are focusing on promising targets …
Transition states, analogues, and drug development
VL Schramm - ACS chemical biology, 2013 - ACS Publications
Enzymes achieve their transition states by dynamic conformational searches on the
femtosecond to picosecond time scale. Mimics of reactants at enzymatic transition states …
femtosecond to picosecond time scale. Mimics of reactants at enzymatic transition states …
Enzymatic transition states and drug design
VL Schramm - Chemical reviews, 2018 - ACS Publications
Transition state theory teaches that chemically stable mimics of enzymatic transition states
will bind tightly to their cognate enzymes. Kinetic isotope effects combined with …
will bind tightly to their cognate enzymes. Kinetic isotope effects combined with …
Antiplasmodial activity of coumarins isolated from Polygala boliviensis: in vitro and in silico studies
DF da Silva, JL de Souza, DM da Costa… - Journal of …, 2023 - Taylor & Francis
Polygala boliviensis is found in the Brazilian semiarid region. This specie is little chemically
and biologically studied. Polygala spp. have different metabolites, especially coumarins …
and biologically studied. Polygala spp. have different metabolites, especially coumarins …
Immucillins in infectious diseases
The Immucillins are chemically stable analogues that mimic the ribocation and leaving-
group features of N-ribosyltransferase transition states. Infectious disease agents often rely …
group features of N-ribosyltransferase transition states. Infectious disease agents often rely …
Antimalarials in development in 2014
DS Barnett, RK Guy - Chemical reviews, 2014 - ACS Publications
Malaria continues to be a devastating burden on the world, causing the deaths of an
estimated 627000 people in 2012, with 482 000 of those being children under the age of 5 …
estimated 627000 people in 2012, with 482 000 of those being children under the age of 5 …
Plasmodium purine metabolism and its inhibition by nucleoside and nucleotide analogues
T Cheviet, I Lefebvre-Tournier, S Wein… - Journal of Medicinal …, 2019 - ACS Publications
Malaria still affects around 200 million people and is responsible for more than 400,000
deaths per year, mostly children in subequatorial areas. This disease is caused by parasites …
deaths per year, mostly children in subequatorial areas. This disease is caused by parasites …