Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM

SJ Piper, RM Johnson, D Wootten, PM Sexton - Chemical reviews, 2022 - ACS Publications
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …

Structural and functional annotation of solute carrier transporters: implication for drug discovery

V Dvorak, G Superti-Furga - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
ABSTRACT Introduction Solute carriers (SLCs) represent the largest group of membrane
transporters in the human genome. They play a central role in controlling the …

Illumination of serotonin transporter mechanism and role of the allosteric site

D Yang, E Gouaux - Science Advances, 2021 - science.org
The serotonin transporter (SERT) terminates serotonin signaling by using sodium and
chloride gradients to drive reuptake of serotonin into presynaptic neurons and is the target of …

Molecular mechanism for the allosteric inhibition of the human serotonin transporter by antidepressant escitalopram

W Xue, T Fu, S Deng, F Yang, J Yang… - ACS chemical …, 2022 - ACS Publications
Human serotine transporter (hSERT) is one of the most influential drug targets, and its
allosteric modulators (eg, escitalopram) have emerged to be the next-generation medication …

Structure of the human dopamine transporter and mechanisms of inhibition

DK Srivastava, V Navratna, DK Tosh, A Chinn, MF Sk… - Nature, 2024 - nature.com
The neurotransmitter dopamine has central roles in mood, appetite, arousal and movement.
Despite its importance in brain physiology and function, and as a target for illicit and …

Cryo-EM structure of GABA transporter 1 reveals substrate recognition and transport mechanism

SR Nayak, D Joseph, G Höfner, A Dakua… - Nature Structural & …, 2023 - nature.com
The inhibitory neurotransmitter γ-aminobutyric acid (GABA) is cleared from the synaptic cleft
by the sodium-and chloride-coupled GABA transporter GAT1. Inhibition of GAT1 prolongs …

Molecular basis of human noradrenaline transporter reuptake and inhibition

J Tan, Y **ao, F Kong, X Zhang, H Xu, A Zhu, Y Liu… - Nature, 2024 - nature.com
Noradrenaline, also known as norepinephrine, has a wide range of activities and effects on
most brain cell types. Its reuptake from the synaptic cleft heavily relies on the noradrenaline …

Transport and inhibition mechanisms of the human noradrenaline transporter

T Hu, Z Yu, J Zhao, Y Meng, K Salomon, Q Bai, Y Wei… - Nature, 2024 - nature.com
The noradrenaline transporter (also known as norepinephrine transporter)(NET) has a
critical role in terminating noradrenergic transmission by utilizing sodium and chloride …

Ligand coupling mechanism of the human serotonin transporter differentiates substrates from inhibitors

R Gradisch, K Schlögl, E Lazzarin, M Niello… - Nature …, 2024 - nature.com
The presynaptic serotonin transporter (SERT) clears extracellular serotonin following
vesicular release to ensure temporal and spatial regulation of serotonergic signalling and …

Structure of the human dopamine transporter in complex with cocaine

JC Nielsen, K Salomon, IE Kalenderoglou… - Nature, 2024 - nature.com
The dopamine transporter (DAT) is crucial for regulating dopamine signalling and is the
prime mediator for the rewarding and addictive effects of cocaine. As part of the …