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Open AccessCommentary
Molecules 2016, 21(9), 1170; doi:10.3390/molecules21091170

The Search for Covalently Ligandable Proteins in Biological Systems

1
Department of Chemistry, Islamia College University Peshawar, Peshawar 25120, Pakistan
2
Department of Biochemistry, Abdul Wali Khan University, Mardan, Khyber Pukhtoonkhwa 25120, Pakistan
3
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 27 June 2016 / Revised: 19 August 2016 / Accepted: 31 August 2016 / Published: 2 September 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [161 KB, uploaded 6 September 2016]

Abstract

This commentary highlights the recent article published in Nature, June 2016, titled: “Proteome-wide covalent ligand discovery in native biological systems”. They screened the whole proteome of different human cell lines and cell lysates. Around 700 druggable cysteines in the whole proteome were found to bind the electrophilic fragments in both active and inactive states of the proteins. Their experiment and computational docking results agreed with one another. The usefulness of this study in terms of bringing a change in medicinal chemistry is highlighted here. View Full-Text
Keywords: fragment-based ligand discovery; covalent binding ligands; druggable cysteines; isotopic tandem orthogonal proteolysis‒activity-based protein profiling; methyl transferase; protease caspase enzyme fragment-based ligand discovery; covalent binding ligands; druggable cysteines; isotopic tandem orthogonal proteolysis‒activity-based protein profiling; methyl transferase; protease caspase enzyme
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Badshah, S.L.; Mabkhot, Y.N. The Search for Covalently Ligandable Proteins in Biological Systems. Molecules 2016, 21, 1170.

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