Fragment-based screening in tandem with phenotypic screening provides novel antiparasitic hits

Autor:	Anitha Shanmugham, Iwan J. P. de Esch, Ewald Edink, Louis Maes, A.R. Blaazer, Rob Leurs, David M. Bailey, Geert Jan Sterk, Paul England, Chimed Jansen, Marco Siderius, Kristina M. Orrling
Přispěvatelé:	Medicinal chemistry, AIMMS
Jazyk:	angličtina
Rok vydání:	2015
Předmět:	Drug Evaluation Preclinical Protozoan Proteins Pharmacology 01 natural sciences Biochemistry Analytical Chemistry Parasitic Sensitivity Tests Drug Discovery Enzyme Inhibitors Non-U.S. Gov't 0303 health sciences biology Antiparasitic Agents Drug discovery Research Support Non-U.S. Gov't Neglected Diseases Preclinical 3. Good health Chemistry Molecular Medicine Leishmania infantum 5'-Cyclic-AMP Phosphodiesterases Type 4 Engineering sciences. Technology Biotechnology Cyclic Nucleotide Phosphodiesterases Antiparasitic medicine.drug_class Phenotypic screening Trypanosoma cruzi Computational biology Trypanosoma brucei Research Support 03 medical and health sciences Inhibitory Concentration 50 SDG 3 - Good Health and Well-being parasitic diseases medicine Journal Article 3' Humans Chagas Disease Biology 030304 developmental biology Plasmodium falciparum biology.organism_classification Antiparasitic agent 0104 chemical sciences Cyclic Nucleotide Phosphodiesterases Type 4 010404 medicinal & biomolecular chemistry 3' 5'-Cyclic-AMP Phosphodiesterases Drug Evaluation Human medicine
Zdroj:	Journal of Biomolecular Screening, 20(1), 131-140. SAGE Publications Inc. Journal of biomolecular screening Blaazer, A R, Orrling, K M, Shanmugham, A, Jansen, C, Maes, L, Edink, E, Sterk, G J, Siderius, M, England, P, Bailey, D, de Esch, I J P & Leurs, R 2015, ' Fragment-based screening in tandem with phenotypic screening provides novel antiparasitic hits ', Journal of Biomolecular Screening, vol. 20, no. 1, pp. 131-140 . https://doi.org/10.1177/1087057114549735
ISSN:	1087-0571
DOI:	10.1177/1087057114549735
Popis:	Methods to discover biologically active small molecules include target-based and phenotypic screening approaches. One of the main difficulties in drug discovery is elucidating and exploiting the relationship between drug activity at the protein target and disease modification, a phenotypic endpoint. Fragment-based drug discovery is a target-based approach that typically involves the screening of a relatively small number of fragment-like (molecular weight
Databáze:	OpenAIRE
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