Expanding chemogenomic space using chemoproteomics |
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| Institution: | 1. School of Pharmacy, Health Science Center, Xi’an Jiaotong University, Xi’an, 710061, China;2. Affiliated Dongfeng Hospital, Hubei University of Medicine, Shiyan, 442008, China;3. Department of Pharmacy, The First Affiliated Hospital of Xi’an Jiaotong University, Xi’an, 710061, China;1. Synthetic and Functional Biomolecules Center, Peking University, Beijing, China;2. Beijing National Laboratory for Molecular Sciences, Peking University, Beijing, China;3. Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Peking University, Beijing, China;4. Peking-Tsinghua Center for Life Sciences, Peking University, Beijing, China;5. College of Chemistry and Molecular Engineering, Peking University, Beijing, China;1. Division of Chemistry & Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore, 637371, Singapore;2. Department of Chemistry and Materials Science, College of Science, Nanjing Forestry University, Nanjing, 210037, PR China;3. Department of Chemistry and Biochemistry, Queens College of the City University of New York, New York, 11367, United States;4. The Graduate Center of the City University of New York, New York, 10016, United States;1. School of Pharmacy, Anhui Province Key Laboratory of Major Autoimmune Diseases, Anhui Medical University, Hefei, 230032, China;2. School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan, 430070, China;3. Department of Mathematics, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah, 21589, Saudi Arabia;1. Department of Radiology, School of Medicine, Washington University in Saint Louis, Saint Louis, MO 63110, United States;2. Department of Chemistry and Cancer Center at Illinois, University of Illinois at Urbana-Champaign, IL 61801, United States |
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| Abstract: | Chemogenomics expedites the discovery of therapeutically-relevant targets from phenotypic screens. However, the vast majority of proteins in the proteome lack selective pharmacological modulators, necessitating the development of new technologies that significantly expand chemogenomic space. Chemoproteomics has emerged as a robust platform to map small molecule-protein interactions in cells using functionalized chemical probes in conjunction with mass spectrometry analysis. Exploration of the ligandable proteome in this manner has led to the development of new pharmacological modulators of diverse proteins. Opportunities to further enhance the impact of chemoproteomics using medicinal chemical biology are described. |
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| Keywords: | Chemogenomics Chemoproteomics Chemical probes |
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