Phenotypic Screens, Chemical Genomics, and Antimalarial Lead Discovery
نویسندگان
چکیده
منابع مشابه
Phenotypic Screens, Chemical Genomics, and Antimalarial Lead Discovery
Several extensive small molecule screens against growing Plasmodium falciparum have recently been published [1–3] and thousands of hit structures are now publicly available. This represents a large majority of the drug-like chemical diversity currently available for screening and hence delineates the currently drugable target space of P. falciparum, since the ‘‘drugability’’ term includes an ‘‘...
متن کاملDiscovery and optimisation studies of antimalarial phenotypic hits
There is an urgent need for the development of new antimalarial compounds. As a result of a phenotypic screen, several compounds with potent activity against the parasite Plasmodium falciparum were identified. Characterization of these compounds is discussed, along with approaches to optimise the physicochemical properties. The in vitro antimalarial activity of these compounds against P. falcip...
متن کاملPhenotypic screens as a renewed approach for drug discovery.
The significant reduction in the number of newly approved drugs in the past decade has been partially attributed to failures in discovery and validation of new targets. Evaluation of recently approved new drugs has revealed that the number of approved drugs discovered through phenotypic screens, an original drug screening paradigm, has exceeded those discovered through the molecular target-base...
متن کاملDesigning zebrafish chemical screens.
The zebrafish is proving to be highly amenable to in vivo small molecule screening. With a growing number of screens successfully completed, a rich interface is being created between disciplines that have historically used zebrafish (e.g., embryology and genetics) and disciplines focused on small molecules (e.g., chemistry and pharmacology). Navigating this interface requires consideration of t...
متن کاملChemical genomics as an emerging paradigm for postgenomic drug discovery.
Chemical genomics approaches are evolving to overcome key problems limiting the efficiency of drug discovery in the postgenomic era. Many of these stem from the low success rates in finding drugs for novel genomics targets whose biochemical properties and therapeutic relevance is poorly understood. The fundamental objective of chemical genomics is to find and optimize chemical compounds that ca...
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ژورنال
عنوان ژورنال: PLoS Pathogens
سال: 2011
ISSN: 1553-7374
DOI: 10.1371/journal.ppat.1002156