Analysing properties of proteasome inhibitors using kinetic and X-ray crystallographic studies

Methods in Molecular Biology
Nerea Gallastegui, Michael Groll

Abstract

The combination of X-ray crystallography and kinetic studies of proteasome:ligand complexes has proven to be an important tool in inhibitor analysis of this crucial protein degradation machinery. Here, we describe in detail the purification protocols, proteolytic activity assays, crystallisation methods, and structure determination for the yeast 20S proteasome (CP) in complex with its inhibitors. The fusion of these advanced techniques offers the opportunity to further optimise drugs which are already tested in different clinical phase studies, as well as to design new promising proteasome lead structures which might be suitable for their application in medicine, plant protection, and antibiotics.

Citations

Jul 21, 2016·Journal of Medicinal Chemistry·Bo-Tao XinHerman S Overkleeft
Mar 12, 2016·Nature Communications·Eva M HuberMichael Groll
May 15, 2015·Angewandte Chemie·Michael GrollAntje Ludwig
Jan 19, 2019·Journal of Medicinal Chemistry·Bo-Tao XinHerman S Overkleeft
Nov 23, 2012·Journal of Medicinal Chemistry·Arwin J BrouwerRob M J Liskamp

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