Orthosteric and Allosteric Activation of Human 5-HT3A Receptors.
Sign Up to like & getrecommendations! Published in 2020 at "Biophysical journal"
DOI: 10.1016/j.bpj.2020.08.029
Abstract: The serotonin type 3 receptor (5-HT3) is a ligand-gated ion channel that converts the binding of the neurotransmitter serotonin (5-HT) into a transient cation current that mediates fast excitatory responses in peripheral and central nervous… read more here.
Keywords: orthosteric allosteric; human ht3a; activation; allosteric activation ... See more keywords
Orthosteric and Allosteric Dual Targeting of the Nuclear Receptor RORγt with a Bitopic Ligand
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DOI: 10.1021/acschembio.0c00941
Abstract: The RORγt nuclear receptor (NR) is of critical importance for the differentiation and proliferation of T helper 17 (Th17) cells and their production of the pro-inflammatory cytokine IL-17a. Dysregulation of RORγt has been linked to… read more here.
Keywords: orthosteric allosteric; bit; ror; bitopic ... See more keywords
Orthosteric–allosteric dual inhibitors of PfHT1 as selective antimalarial agents
Sign Up to like & getrecommendations! Published in 2021 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2017749118
Abstract: Significance There is an urgent need for alternative antimalarials with the emergence of artemisinin-resistant malaria parasites. Blocking sugar uptake in Plasmodium falciparum by selectively inhibiting the hexose transporter P. falciparum hexose transporter 1 (PfHT1) kills… read more here.
Keywords: orthosteric allosteric; resistant malaria; falciparum; hexose transporter ... See more keywords
Makaluvamine G from the Marine Sponge Zyzzia fuliginosa Inhibits Muscle nAChR by Binding at the Orthosteric and Allosteric Sites
Sign Up to like & getrecommendations! Published in 2018 at "Marine Drugs"
DOI: 10.3390/md16040109
Abstract: Diverse ligands of the muscle nicotinic acetylcholine receptor (nAChR) are used as muscle relaxants during surgery. Although a plethora of such molecules exists in the market, there is still a need for new drugs with… read more here.
Keywords: orthosteric allosteric; muscle nachr; allosteric sites; muscle ... See more keywords