[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 …

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 …

Identifying purine nucleoside phosphorylase as the target of quinine using cellular thermal shift assay

JM Dziekan, H Yu, D Chen, L Dai, G Wirjanata… - Science translational …, 2019 - science.org
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 …

[HTML][HTML] Drug targets for resistant malaria: historic to future perspectives

S Kumar, TR Bhardwaj, DN Prasad… - Biomedicine & …, 2018 - Elsevier
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 …

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 …

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 …

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 …

Immucillins in infectious diseases

GB Evans, PC Tyler, VL Schramm - ACS infectious diseases, 2018 - ACS Publications
The Immucillins are chemically stable analogues that mimic the ribocation and leaving-
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 …

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 …