Monoamine transporters: structure, intrinsic dynamics and allosteric regulation.
Nat Struct Mol Biol
; 26(7): 545-556, 2019 07.
Article
in En
| MEDLINE
| ID: mdl-31270469
ABSTRACT
Monoamine transporters (MATs) regulate neurotransmission via the reuptake of dopamine, serotonin and norepinephrine from extra-neuronal regions and thus maintain neurotransmitter homeostasis. As targets of a wide range of compounds, including antidepressants, substances of abuse and drugs for neuropsychiatric and neurodegenerative disorders, their mechanism of action and their modulation by small molecules have long been of broad interest. Recent advances in the structural characterization of dopamine and serotonin transporters have opened the way for structure-based modeling and simulations, which, together with experimental data, now provide mechanistic understanding of their transport function and interactions. Here we review recent progress in the elucidation of the structural dynamics of MATs and their conformational landscape and transitions, as well as allosteric regulation mechanisms.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Dopamine Plasma Membrane Transport Proteins
/
Norepinephrine Plasma Membrane Transport Proteins
/
Serotonin Plasma Membrane Transport Proteins
Limits:
Animals
/
Humans
Language:
En
Journal:
Nat Struct Mol Biol
Journal subject:
BIOLOGIA MOLECULAR
Year:
2019
Document type:
Article
Affiliation country:
United States