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Recent developments in ligands and chemical probes targeting solute carrier transporters |
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| Affiliation: | 1. Department DiBEST (Biologia, Ecologia, Scienze della Terra) Unit of Biochemistry and Molecular Biotechnology, University of Calabria, Via P. Bucci 4C, 87036 Arcavacata di Rende, Italy;2. Dipartimento di Scienze Farmacologiche e Biomolecolari, Università degli Studi di Milano, Italy;3. Dipartimento di Scienze Farmacologiche e Biomolecolari e Dipartimento di Scienze Biomediche e Cliniche “L. Sacco”, Università degli Studi di Milano, Italy;1. Faculty of Pharmacy, University of Sydney, NSW 2006, Australia;2. Save Sight Institute, the University of Sydney, Sydney, NSW 2000, Australia;3. Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, 214063, Jiangsu Province, China;4. Pharmacogenomics and Drug Development Group, Discipline of Pharmacology, School of Medical Sciences, The University of Sydney, NSW 2006, Australia |
| Abstract: | Solute carrier (SLC) membrane transporters remain a largely unexploited target class, despite their central roles in cell identity and metabolism. This gap is reflected in the lack of high-quality chemical ligands or probes and in the small number of compounds that have progressed toward clinical development. In this review, we discuss recent advancements in SLC ligand discovery as well as new candidates that have been added to the investigational toolkit, with a particular focus on first-in-class ligands and the cognate discovery strategies. The availability of new probes expands the opportunity to elucidate the functions of SLCs and their relevance in physiology and explores any future potential of SLC druggability. |
| Keywords: | Ligand discovery Solute carrier (SLC) transporters Small-molecule probes First-in-class ligands Drug discovery PET tracers Cancer Modulators of neurotransmission |
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