Design strategies and recent development of bioactive modulators for glutamine transporters.

Zhiyu Li, Xinying Cheng, Yezhi Wang, Guangyue Gong, Pei Shen, Jinlei Bian

Journal: Drug discovery today 2024;29(2):103880

PMID: 38216118

Full Text on Elsevier Science View on PubMed

Abstract

Glutamine transporters are integral to the metabolism of glutamine in both healthy tissues and cancerous cells, playing a pivotal role in maintaining amino acid balance, synthesizing biomolecules, and regulating redox equilibrium. Their critical functions in cellular metabolism make them promising targets for oncological therapies. Recent years have witnessed substantial progress in the field of glutamine transporters, marked by breakthroughs in understanding of their protein structures and the discovery of novel inhibitors, prodrugs, and radiotracers. This review provides a comprehensive update on the latest advancements in modulators targeting the glutamine transporter, with special attention given to LAT1 and ASCT2. It also discusses innovative approaches in drug design aimed at these transporters.

Address: School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.; School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China. Electronic address: [email protected].; School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China. Electronic address: [email protected].

DOI: 10.1016/j.drudis.2024.103880

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MeSH Terms: Glutamine, Amino Acids, Membrane Transport Proteins