Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:2.3.1.107 (DAT)
 1,471 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The successful generation and functional expression of a series of recombinant chimeric transporters, in which distinct functional properties of NET and DAT are exchanged, have allowed the assignment of a number of important functional properties of MPP+ and antidepressant-sensitive catecholamine transporters to specific domains within their primary structure. These studies are the first comprehensive structure-function analysis of members of the rapidly growing superfamily of Na+/Cl- carriers using chimeric transporters. This represents the first step in identifying the specific structural or regulatory determinants that differentiate NET and DAT. An appreciation of the potentially distinct sites for substrate recognition, translocation, and transport inhibition of NET and DAT may facilitate the development of more selective drugs for the treatment of stimulant addiction, human depression, and other affective disorders.
NIDA Res Monogr 1996
PMID:Discrete structural domains and cell-specific expression determine functional selectivity of the dopamine and norepinephrine transporters. 878 50

The study reported here concerns the preparation of a novel graphene-diaminotriazine (G-DAT) nanocomposite hydrogel for application in the drug delivery field. The hybrid nature of this material is founded on two key elements: the presence of the DAT backbone induced the formation of hydrophobic regions that allowed efficient loading of a series of drugs of increasing hydrophobicity (Metronidazole, Benzocaine, Ibuprofen, Naproxen and Imipramine), while simultaneously endowing swelling-induced pH-responsiveness to the hydrogel. Additionally, the incorporation of graphene was found to interfere with these hydrophobic domains through favourable non-covalent interactions, thus leading to the partial disruption of these aggregates. As a consequence, graphene facilitated and enhanced the release of model hydrophobic drug Imipramine in a synergistic manner with the pH trigger, and increased the swelling capacities and improved mechanical performance. This hybrid hydrogel can therefore be envisaged as a proof-of-concept system for the release of hydrophobic compounds in the field of drug delivery.
 ...
PMID:Stimuli-responsive graphene-based hydrogel driven by disruption of triazine hydrophobic interactions. 3218 62