Disease control targeting transporters and drugdiscovery

Abstract

Transporters are membrane proteins responsible for the distribution of substanceswithin the body, acting as interfaces between various compartments, thusdetermining the concentration ratios of substances between these compartments.Consequently, by pharmacologically modulating the function of thesetransporters, we can shift abnormal compound distributions seen in pathologicalstates, restoring homeostasis and thereby promoting recovery from diseases. Forinstance, the SGLT2 (SLC5A2) inhibitors, which suppress the reabsorption ofglucose in the renal tubules, is an exemplary drug that skews glucosedistribution towards the urine, enhancing glucose excretion and rectifyinghyperglycemia, establishing its role in diabetes treatment. From anotherperspective, transporters responsible for nutrient uptake, especially thoseupregulating in pathogenic cells like cancer cells, become potential drugtargets. The amino acid transporter LAT1 (SLC7A5), which is highly expressedwith specificity in cancer cells, presents itself as a potential diagnostic andtherapeutic target. In this lecture, introducing our research on drugdevelopment targeting LAT1 as an example, I would like to discuss theinteractions between transporters and compounds as well as the significance oftransporters as drug targets.