Cardiff University | Prifysgol Caerdydd ORCA
Online Research @ Cardiff 
WelshClear Cookie - decide language by browser settings

Selectivity profiling of DegP substrates and inhibitors

Hauske, Patrick, Meltzer, Michael, Ottmann, Christian, Krojer, Tobias, Clausen, Tim, Ehrmann, Michael and Kaiser, Markus 2009. Selectivity profiling of DegP substrates and inhibitors. Bioorganic & Medicinal Chemistry 17 (7) , pp. 2920-2924. 10.1016/j.bmc.2009.01.073

Full text not available from this repository.

Abstract

Protein quality control factors are involved in many key physiological processes and severe human diseases that are based on misfolding or amyloid formation. Prokaryotic representatives are often virulence factors of pathogenic bacteria. Therefore, protein quality control factors represent a novel class of drug targets. The bacterial serine protease DegP, belonging to the widely conserved family of HtrA proteases, exhibits unusual structural and functional plasticity that could be exploited by small molecule modulators. However, only one weak synthetic peptide substrate and no inhibitors are available to date. We report the identification of a potent heptameric pNA-substrate and chloromethyl ketone based inhibitors of DegP. In addition, specificity profiling resulted in the identification of one strong inhibitor and a potent substrate for subtilisin as well as a number of specific elastase substrates and inhibitors.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Subjects: Q Science > QH Natural history > QH301 Biology
Publisher: Elsevier
ISSN: 0968-0896
Last Modified: 04 Jun 2017 06:15
URI: http://orca.cf.ac.uk/id/eprint/57790

Citation Data

Cited 33 times in Google Scholar. View in Google Scholar

Cited 31 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item Edit Item