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Back Cover: From On‐Target to Off‐Target Activity: Identification and Optimisation of Trypanosoma brucei GSK3 Inhibitors and Their Characterisation as Anti‐ Trypanosoma brucei Drug Discovery Lead Molecules (ChemMedChem 7/2013)
Author(s) -
Woodland Andrew,
Grimaldi Raffaella,
Luksch Torsten,
Cleghorn Laura A. T.,
Ojo Kayode K.,
Van Voorhis Wesley C.,
Brenk Ruth,
Frearson Julie A.,
Gilbert Ian H.,
Wyatt Paul G.
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201390029
Subject(s) - trypanosoma brucei , drug discovery , african trypanosomiasis , trypanocidal agent , computational biology , biology , drug target , drug development , in vitro , identification (biology) , trypanosoma , lead compound , biochemistry , drug , virology , trypanosomiasis , pharmacology , gene , botany
The back cover picture shows the discovery of Trypanosoma brucei protein kinase GSK3 short ( Tb GSK3) inhibitors and their characterization as leads in the development of novel therapeutics against Human African trypanosomiasis (HAT). Hit validation and optimization gave rise to a series of diaminothiazoles with low nanomolar activities against Tb GSK3 that are potent in vitro inhibitors of T. brucei proliferation. For more details, see the Full Paper by Ian H. Gilbert, Paul G. Wyatt et al. on p. 1127 ff.