Advances and Challenges in Rational Drug Design for SLCs.

Rachel-Ann A Garibsingh, Avner Schlessinger

Journal: Trends in pharmacological sciences 2020;40(10):790-800

PMID: 31519459

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Abstract

There are over 420 human solute carrier (SLC) transporters from 65 families that are expressed ubiquitously in the body. The SLCs mediate the movement of ions, drugs, and metabolites across membranes and their dysfunction has been associated with a variety of diseases, such as diabetes, cancer, and central nervous system (CNS) disorders. Thus, SLCs are emerging as important targets for therapeutic intervention. Recent technological advances in experimental and computational biology allow better characterization of SLC pharmacology. Here we describe recent approaches to modulate SLC transporter function, with an emphasis on the use of computational approaches and computer-aided drug design (CADD) to study nutrient transporters. Finally, we discuss future perspectives in the rational design of SLC drugs.

Address: Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.; Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA. Electronic address: [email protected].

DOI: 10.1016/j.tips.2019.08.006

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MeSH Terms: Amino Acid Transport System ASC, Drug Design, Humans, Ligands, Minor Histocompatibility Antigens, Models, Molecular, Receptors, Somatostatin, Solute Carrier Proteins, Structure-Activity Relationship