The past, present and future of anti-malarial medicines
Great progress has been made in recent years to reduce the high level of suffering caused
by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria …
by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria …
Strategies to combat multi-drug resistance in tuberculosis
Conspectus “Drug resistance is an unavoidable consequence of the use of drugs; however,
the emergence of multi-drug resistance can be managed by accurate diagnosis and tailor …
the emergence of multi-drug resistance can be managed by accurate diagnosis and tailor …
Malaria medicines: a glass half full?
TNC Wells, RH Van Huijsduijnen… - Nature Reviews Drug …, 2015 - nature.com
Despite substantial scientific progress over the past two decades, malaria remains a
worldwide burden that causes hundreds of thousands of deaths every year. New, affordable …
worldwide burden that causes hundreds of thousands of deaths every year. New, affordable …
[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology
CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …
probes of disease-related targets and potential starting points for drug discovery. In this …
Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase
T Paquet, C Le Manach, DG Cabrera… - Science translational …, 2017 - science.org
As part of the global effort toward malaria eradication, phenotypic whole-cell screening
revealed the 2-aminopyridine class of small molecules as a good starting point to develop …
revealed the 2-aminopyridine class of small molecules as a good starting point to develop …
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors
N Kato, E Comer, T Sakata-Kato, A Sharma, M Sharma… - Nature, 2016 - nature.com
Antimalarial drugs have thus far been chiefly derived from two sources—natural products
and synthetic drug-like compounds. Here we investigate whether antimalarial agents with …
and synthetic drug-like compounds. Here we investigate whether antimalarial agents with …
[HTML][HTML] Antimalarial drug discovery—approaches and progress towards new medicines
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 …
High-level data fusion enables the chemoinformatically guided discovery of chiral disulfonimide catalysts for atropselective iodination of 2-amino-6-arylpyridines
BT Rose, JC Timmerman, SA Bawel… - Journal of the …, 2022 - ACS Publications
The atropselective iodination of 2-amino-6-arylpyridines catalyzed by chiral disulfonimides
(DSIs) is described. Key to the development of this transformation was the use of a …
(DSIs) is described. Key to the development of this transformation was the use of a …
In vitro culture, drug sensitivity, and transcriptome of Plasmodium vivax hypnozoites
The unique relapsing nature of Plasmodium vivax infection is a major barrier to malaria
eradication. Upon infection, dormant liver-stage forms, hypnozoites, linger for weeks to …
eradication. Upon infection, dormant liver-stage forms, hypnozoites, linger for weeks to …
A new class of small molecule inhibitor of BMP signaling
CE Sanvitale, G Kerr, A Chaikuad, MC Ramel… - PloS one, 2013 - journals.plos.org
Growth factor signaling pathways are tightly regulated by phosphorylation and include many
important kinase targets of interest for drug discovery. Small molecule inhibitors of the bone …
important kinase targets of interest for drug discovery. Small molecule inhibitors of the bone …