[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 …

Malaria research in the post-genomic era

EA Winzeler - Nature, 2008 - nature.com
For many pathogens the availability of genome sequence, permitting genome-dependent
methods of research, can partially substitute for powerful forward genetic methods (genome …

Chemical genetics of Plasmodium falciparum

WA Guiguemde, AA Shelat, D Bouck, S Duffy… - Nature, 2010 - nature.com
Malaria caused by Plasmodium falciparum is a disease that is responsible for 880,000
deaths per year worldwide. Vaccine development has proved difficult and resistance has …

In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen

D Plouffe, A Brinker, C McNamara… - Proceedings of the …, 2008 - National Acad Sciences
The growing resistance to current first-line antimalarial drugs represents a major health
challenge. To facilitate the discovery of new antimalarials, we have implemented an efficient …

Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening

JD Johnson, RA Dennull, L Gerena… - Antimicrobial agents …, 2007 - Am Soc Microbiol
Several new fluorescence malaria in vitro drug susceptibility microtiter plate assays that
detect the presence of malarial DNA in infected erythrocytes have recently been reported, in …

Visualisation and quantitative analysis of the rodent malaria liver stage by real time imaging

IHJ Ploemen, M Prudêncio, BG Douradinha… - PloS one, 2009 - journals.plos.org
The quantitative analysis of Plasmodium development in the liver in laboratory animals in
cultured cells is hampered by low parasite infection rates and the complicated methods …

Plasmepsin II–III copy number accounts for bimodal piperaquine resistance among Cambodian Plasmodium falciparum

S Bopp, P Magistrado, W Wong, SF Schaffner… - Nature …, 2018 - nature.com
Multidrug resistant Plasmodium falciparum in Southeast Asia endangers regional malaria
elimination and threatens to spread to other malaria endemic areas. Understanding …

Liver-stage malaria parasites vulnerable to diverse chemical scaffolds

ER Derbyshire, M Prudêncio… - Proceedings of the …, 2012 - National Acad Sciences
Human malaria infection begins with a one-time asymptomatic liver stage followed by a
cyclic symptomatic blood stage. All high-throughput malaria drug discovery efforts have …

The state of the art in anti-malarial drug discovery and development

J N. Burrows, K Chibale… - Current topics in medicinal …, 2011 - benthamdirect.com
Malaria is one of the most prevalent and devastating infectious diseases of our time. Yet,
unfortunately, apart from artemisinin combination therapies there are relatively few effective …

Mycangimycin, a Polyene Peroxide from a Mutualist Streptomyces sp.

DC Oh, JJ Scott, CR Currie, J Clardy - Organic letters, 2009 - ACS Publications
A mutualist actinomycete of the southern pine beetle, Dendroctonus frontalis, produces a
polyene peroxide with pronounced antifungal activity. Its structure, absolute configuration …