Recent developments in ligands and chemical probes targeting solute carrier transporters.

Andrea Casiraghi, Ariel Bensimon, Giulio Superti-Furga

Journal: Current opinion in chemical biology 2021;62():53-63

PMID: 33689964

Full Text on Elsevier Science View on PubMed

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.

Address: CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, 1090 Vienna, Austria.; CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, 1090 Vienna, Austria; Solgate GmbH, 3400 Klosterneuburg, Austria.; CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, 1090 Vienna, Austria; Center for Physiology and Pharmacology, Medical University of Vienna, 1090 Vienna, Austria. Electronic address: [email protected].

DOI: 10.1016/j.cbpa.2021.01.012

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MeSH Terms: Antineoplastic Agents, Biological Transport, Cell Membrane, Drug Discovery, Humans, Ligands, Metabolic Diseases, Neoplasms, Neurotransmitter Agents, Nutrients, Protein Binding, Protein Conformation, Small Molecule Libraries, Solute Carrier Proteins