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From Proteopedia
Revision as of 02:30, 7 August 2014 by OCA (Talk | contribs)
A limited therapeutic arsenal against increasing clinical disease due to Aspergillus spp. necessitates urgent characterisation of new antifungal targets. Here we describe the discovery of novel, low micromolar chemical inhibitors of Aspergillus fumigatus family 18 plant-type chitinase A1 (AfChiA1) by high-throughput screening (HTS). Analysis of the binding mode by X-ray crystallography confirmed competitive inhibition and kinetic studies revealed two compounds with selectivity towards fungal plant-type chitinases. These inhibitors provide new chemical tools to probe the effects of chitinase inhibition on A. fumigatus growth and virulence, presenting attractive starting points for the development of further potent drug-like molecules.
Screening-based discovery of Aspergillus fumigatus plant-type chitinase inhibitors.,Lockhart DE, Schuettelkopf A, Blair DE, van Aalten DM FEBS Lett. 2014 Jul 22. pii: S0014-5793(14)00564-X. doi:, 10.1016/j.febslet.2014.07.015. PMID:25063338[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
↑ Lockhart DE, Schuettelkopf A, Blair DE, van Aalten DM. Screening-based discovery of Aspergillus fumigatus plant-type chitinase inhibitors. FEBS Lett. 2014 Jul 22. pii: S0014-5793(14)00564-X. doi:, 10.1016/j.febslet.2014.07.015. PMID:25063338 doi:http://dx.doi.org/10.1016/j.febslet.2014.07.015
