Targeting Solute Carrier Transporters through Functional Mapping

Claire Colas,Elodie Laine

doi:10.1016/j.tips.2020.11.005

Abstract

Solute carrier (SLC) transporters are emerging drug targets. Identifying the molecular determinants responsible for their specific and selective transport activities and describing key interactions with their ligands are crucial steps towards the design of potential new drugs. A general functional mapping across more than 400 human SLC transporters would pave the way to the rational and systematic design of molecules modulating cellular transport.

Highlights

Identifying the molecular determinants responsible for their specific and selective transport activities and describing key interactions with their ligands are crucial steps towards the design of potential new drugs
A Long and Complex Evolutionary History The 456 known human Solute carrier (SLC) transporters are grouped in 65 families based on their sequence and functional similarities
It is believed that learning from beststudied systems can provide insights into how to efficiently tackle drug discovery for SLC transporters

Summary

Introduction

Identifying the molecular determinants responsible for their specific and selective transport activities and describing key interactions with their ligands are crucial steps towards the design of potential new drugs. Understanding these complex biological systems requires the description of many aspects of their functioning (e.g., interactions with ligands and with protein partners, conformational changes and kinetics of transport, response to cofactors, and differential expression in different cell types).

Results

Conclusion