Transforming targeted cancer therapy with PROTACs: A forward-looking perspective |
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| Affiliation: | 1. Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, UK;2. Boehringer Ingelheim RCV GmbH & Co KG, Dr. Boehringer Gasse 5-11, A-1121, Vienna, Austria;1. Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Institute of Materia Medica, Hangzhou Medical College, Hangzhou, 310013, PR China;2. School of Pharmacy, Hangzhou Medical College, Hangzhou, 310013, PR China;3. Center for Molecular Medicine, Hangzhou Medical College, Hangzhou, 310013, PR China;4. Department of Drug Platform of Small Molecules, HangZhou ZhongMei HuaDong Pharmaceutical CO, LTD, 866 Moganshan Road, Hangzhou, 310011, PR China;1. Department of Pathology, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA;2. Department of Biochemistry and Molecular Biology, Research Center of Laboratory Medicine, School of Laboratory Medicine, Bengbu Medical College, Anhui, 233030, China;3. Department of Obstetrics and Gynecology, the Second Affiliated Hospital of Wenzhou Medical University, Wenzhou, 325027, China;4. Department of Clinical Laboratory Diagnostics, School of Laboratory Medicine, Bengbu Medical College, Anhui, 233030, China |
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| Abstract: | Small-molecule targeted protein degraders have in recent years made a great impact on the strategies of many industry and academic cancer research endeavours. We seek here to provide a concise perspective on the opportunities and challenges that lie ahead for bifunctional degrader molecules, so-called ‘Proteolysis Targeting Chimeras (PROTACs),’ in the context of cancer therapy. We highlight high-profile studies that support the potential for PROTAC approaches to broaden drug target scope, address drug resistance, enhance target selectivity and provide tissue specificity, but also assess where the modality is yet to fully deliver in these contexts. Future opportunities presented by the unique bifunctional nature of these molecules are also discussed. |
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| Keywords: | Targeted protein degradation PROTACs Cancer Bifunctional molecules Drug discovery Target selectivity Drug resistance |
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