SLC6 transporters: structure, function, regulation, disease association and therapeutics
The SLC6 family of secondary active transporters are integral membrane solute carrier
proteins characterized by the Na+-dependent translocation of small amino acid or amino …
proteins characterized by the Na+-dependent translocation of small amino acid or amino …
Monoamine transporters: insights from molecular dynamics simulations
The human monoamine transporters (MATs) facilitate the reuptake of the neurotransmitters
serotonin, dopamine, and norepinephrine from the synaptic cleft. Imbalance in …
serotonin, dopamine, and norepinephrine from the synaptic cleft. Imbalance in …
Structures of LeuT in bicelles define conformation and substrate binding in a membrane-like context
Neurotransmitter sodium symporters (NSSs) catalyze the uptake of neurotransmitters into
cells, terminating neurotransmission at chemical synapses. Consistent with the role of NSSs …
cells, terminating neurotransmission at chemical synapses. Consistent with the role of NSSs …
Allosteric mechanisms of molecular machines at the membrane: transport by sodium-coupled symporters
MV LeVine, MA Cuendet, G Khelashvili… - Chemical …, 2016 - ACS Publications
Solute transport across cell membranes is ubiquitous in biology as an essential
physiological process. Secondary active transporters couple the unfavorable process of …
physiological process. Secondary active transporters couple the unfavorable process of …
Structural insights into functional lipid–protein interactions in secondary transporters
C Koshy, C Ziegler - Biochimica et Biophysica Acta (BBA)-General …, 2015 - Elsevier
Background Structural evidences with functional corroborations have revealed distinct
features of lipid–protein interactions especially in channels and receptors. Many membrane …
features of lipid–protein interactions especially in channels and receptors. Many membrane …
Identification of the first highly subtype-selective inhibitor of human GABA transporter GAT3
M Damgaard, A Al-Khawaja… - ACS chemical …, 2015 - ACS Publications
Screening a library of small-molecule compounds using a cell line expressing human GABA
transporter 3 (hGAT3) in a [3H] GABA uptake assay identified isatin derivatives as a new …
transporter 3 (hGAT3) in a [3H] GABA uptake assay identified isatin derivatives as a new …
Molecular determinants for substrate interactions with the glycine transporter GlyT2
JE Carland, M Thomas, SN Mostyn… - ACS chemical …, 2017 - ACS Publications
Transporters in the SLC6 family play key roles in regulating neurotransmission and are the
targets for a wide range of therapeutics. Important insights into the transport mechanisms …
targets for a wide range of therapeutics. Important insights into the transport mechanisms …
Toward a systematic structural and functional annotation of solute carriers transporters—example of the SLC6 and SLC7 families
C Colas - Frontiers in Pharmacology, 2020 - frontiersin.org
SLC transporters are emerging key drug targets. One important step for drug development is
the profound understanding of the structural determinants defining the substrate selectivity of …
the profound understanding of the structural determinants defining the substrate selectivity of …
Substrate binds in the S1 site of the F253A mutant of LeuT, a neurotransmitter sodium symporter homologue
LeuT serves as the model protein for understanding the relationships between structure,
mechanism and pharmacology in neurotransmitter sodium symporters (NSSs). At the …
mechanism and pharmacology in neurotransmitter sodium symporters (NSSs). At the …
Identification of a new allosteric binding site for cocaine in dopamine transporter
Dopamine (DA) transporter (DAT) is a major target for psychostimulant drugs of abuse such
as cocaine that competitively binds to DAT, inhibits DA reuptake, and consequently …
as cocaine that competitively binds to DAT, inhibits DA reuptake, and consequently …