The Search for Covalently Ligandable Proteins in Biological Systems
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 fou...
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| Format: | Article |
| Language: | English |
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MDPI AG
2016-09-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1420-3049/21/9/1170 |
| _version_ | 1811192771046801408 |
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| author | Syed Lal Badshah Yahia Nasser Mabkhot |
| author_facet | Syed Lal Badshah Yahia Nasser Mabkhot |
| author_sort | Syed Lal Badshah |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-11T23:58:04Z |
| format | Article |
| id | doaj.art-0fbbb9e835d8430393d6ddbd25afdb08 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-04-11T23:58:04Z |
| publishDate | 2016-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-0fbbb9e835d8430393d6ddbd25afdb082022-12-22T03:56:19ZengMDPI AGMolecules1420-30492016-09-01219117010.3390/molecules21091170molecules21091170The Search for Covalently Ligandable Proteins in Biological SystemsSyed Lal Badshah0Yahia Nasser Mabkhot1Department of Chemistry, Islamia College University Peshawar, Peshawar 25120, PakistanDepartment of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaThis 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.http://www.mdpi.com/1420-3049/21/9/1170fragment-based ligand discoverycovalent binding ligandsdruggable cysteinesisotopic tandem orthogonal proteolysis‒activity-based protein profilingmethyl transferaseprotease caspase enzyme |
| spellingShingle | Syed Lal Badshah Yahia Nasser Mabkhot The Search for Covalently Ligandable Proteins in Biological Systems Molecules fragment-based ligand discovery covalent binding ligands druggable cysteines isotopic tandem orthogonal proteolysis‒activity-based protein profiling methyl transferase protease caspase enzyme |
| title | The Search for Covalently Ligandable Proteins in Biological Systems |
| title_full | The Search for Covalently Ligandable Proteins in Biological Systems |
| title_fullStr | The Search for Covalently Ligandable Proteins in Biological Systems |
| title_full_unstemmed | The Search for Covalently Ligandable Proteins in Biological Systems |
| title_short | The Search for Covalently Ligandable Proteins in Biological Systems |
| title_sort | search for covalently ligandable proteins in biological systems |
| topic | fragment-based ligand discovery covalent binding ligands druggable cysteines isotopic tandem orthogonal proteolysis‒activity-based protein profiling methyl transferase protease caspase enzyme |
| url | http://www.mdpi.com/1420-3049/21/9/1170 |
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