Lieve van Veggel, Tamara A M Mocking, Hubert J Sijben, Rongfang Liu, Marina Gorostiola González, Majlen A Dilweg, Jeroen Royakkers, Anna Li, Vijay Kumar, Yin Yao Dong, Alex Bullock, David B Sauer, Hanne Diliën, Gerard J P van Westen, Rudy Schreiber, Laura H Heitman, Tim Vanmierlo
Excitatory amino acid transporters (EAATs) are important regulators of amino acid transport and in particular glutamate. Recently, more interest has arisen in these transporters in the context of neurodegenerative diseases. This calls for ways to modulate these targets to drive glutamate transport, EAAT2 and EAAT3 in particular. Several inhibitors (competitive and noncompetitive) exist to block glutamate transport; however, activators remain scarce. Recently, GT949 was proposed as a selective activator of EAAT2, as tested in a radioligand uptake assay...
March 13, 2024: ACS Chemical Neuroscience