Methodology for Identification of Cysteine-Reactive Covalent Inhibitors

Stefan G Kathman; Alexander V Statsyuk

doi:10.1007/978-1-4939-9187-7_15

Methodology for Identification of Cysteine-Reactive Covalent Inhibitors

Methods Mol Biol. 2019:1967:245-262. doi: 10.1007/978-1-4939-9187-7_15.

Authors

Stefan G Kathman¹, Alexander V Statsyuk²

Affiliations

¹ Northwestern University, Department of Chemistry, Silverman Hall, Evanston, IL, USA.
² University of Houston, College of Pharmacy, Houston, TX, USA. alexander.statsyuk@gmail.com.

PMID: 31069775
DOI: 10.1007/978-1-4939-9187-7_15

Abstract

Covalent fragments are an emerging technology to discover covalent ligands in target-based or phenotypic screens. Here we describe screening of cysteine-reactive covalent fragments against a protein of interest using mass spectrometry or enzymatic methods.

Keywords: Covalent fragments; Cysteine.

Publication types

Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

MeSH terms

Cysteine / chemistry*
Humans
Ligands
Mass Spectrometry / methods*
Molecular Structure

Substances

Ligands
Cysteine

Grants and funding

T32 GM105538/GM/NIGMS NIH HHS/United States