Overview of monoamine transporters

S Aggarwal, OV Mortensen - Current protocols in …, 2017 - Wiley Online Library
Abstract The dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters,
which are collectively referred to as monoamine transporters (MATs), play significant roles in …

Allosteric modulation of neurotransmitter transporters as a therapeutic strategy

M Niello, R Gradisch, CJ Loland, T Stockner… - Trends in …, 2020 - cell.com
Neurotransmitter transporters (NTTs) are involved in the fine-tuning of brain neurotransmitter
homeostasis. As such, they are implicated in a plethora of complex behaviors, including …

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-based discovery of a novel allosteric inhibitor against human dopamine transporter

S Deng, H Zhang, R Gou, D Luo, Z Liu… - Journal of chemical …, 2023 - ACS Publications
Human dopamine transporter (hDAT) regulates the reuptake of extracellular dopamine (DA)
and is an essential therapeutic target for central nervous system (CNS) diseases. The …

The binding mode of vilazodone in the human serotonin transporter elucidated by ligand docking and molecular dynamics simulations

Y Zhang, G Zheng, T Fu, J Hong, F Li, X Yao… - Physical Chemistry …, 2020 - pubs.rsc.org
Vilazodone is a novel antidepressant used for the treatment of major depressive disorder
(MDD) with a primary action mechanism of inhibiting the human serotonin reuptake …

The high‐energy transition state of the glutamate transporter homologue GltPh

GHM Huysmans, D Ciftci, X Wang, SC Blanchard… - The EMBO …, 2021 - embopress.org
Membrane transporters mediate cellular uptake of nutrients, signaling molecules, and drugs.
Their overall mechanisms are often well understood, but the structural features setting their …

Investigating the mechanism of sodium binding to SERT using direct simulations

D Szöllősi, T Stockner - Frontiers in Cellular Neuroscience, 2021 - frontiersin.org
The serotonin transporter (SERT) terminates neurotransmission by transporting serotonin
from the synapse into the pre-synaptic nerve terminal. Altered SERT function leads to …

Identification of a novel allosteric modulator of the human dopamine transporter

S Aggarwal, X Liu, C Rice, P Menell… - ACS chemical …, 2019 - ACS Publications
The dopamine transporter (DAT) serves a pivotal role in controlling dopamine (DA)-
mediated neurotransmission by clearing DA from synaptic and perisynaptic spaces and …

A role for fragment-based drug design in developing novel lead compounds for central nervous system targets

MJ Wasko, KA Pellegrene, JD Madura… - Frontiers in …, 2015 - frontiersin.org
Hundreds of millions of US dollars are invested in the research and development of a single
drug. Lead compound development is an area ripe for new design strategies. Therapeutic …

Butyrate acts as a positive allosteric modulator of the 5‐HT transporter to decrease availability of 5‐HT in the ileum

J Cai, J Cheung, SWM Cheung… - British Journal of …, 2024 - Wiley Online Library
Background and Purpose Radiation therapy‐induced gastrointestinal distress is partly
associated with the elimination of gut microbiota. The effectiveness of 5‐HT receptor …