Two-hit wonders: The expanding universe of multitargeting epigenetic agents |
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| Institution: | 1. Departamento de Química Orgánica, Facultade de Química, CINBIO and IIS Galicia Sur, Universidade de Vigo, 36310 Vigo, Spain;2. School of Pharmacy, University of East Anglia, Norwich NR4 7TJ, United Kingdom;1. Department of Cellular and Molecular Pharmacology, University of California San Francisco, 600 16th Street, Genentech Hall, San Francisco, CA 94158, USA;2. Department of Pharmaceutical Chemistry, University of California San Francisco, 600 16th Street, Genentech Hall, San Francisco, CA 94158, USA;3. Quantitative Biosciences Institute, University of California San Francisco, San Francisco, CA 94158, USA;1. Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d’Augusto 237, 47921 Rimini, Italy;2. Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy;3. Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Roma, Italy;1. Department of Medicinal Chemistry, School of Pharmacy, Qingdao University, Qingdao, Shandong, China;2. Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China;3. Department of Pharmacology, College of Basic Medicine, Qingdao University, Qingdao, Shandong, China |
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| Abstract: | Multitargeting involves the application of molecules that are deliberately intended to bind to two or more unrelated cellular targets with high affinity. In epigenetic chemical biology and drug discovery, the rational design of multitargeting agents has evolved to a sophisticated level, and there are now five examples that have reached clinical trials. This review covers recent developments in the field and future prospects. |
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