[HTML][HTML] Pharmacology of human trace amine-associated receptors: Therapeutic opportunities and challenges

MD Berry, RR Gainetdinov, MC Hoener… - Pharmacology & …, 2017 - Elsevier
The discovery in 2001 of a G protein-coupled receptor family, subsequently termed trace
amine-associated receptors (TAAR), triggered a resurgence of interest in so-called trace …

Trace amine-associated receptor 1 (TAAR1): Potential application in mood disorders: A systematic review

Y Alnefeesi, JK Tamura, LMW Lui, MY Jawad… - Neuroscience & …, 2021 - Elsevier
There is a need for innovation with respect to therapeutics in psychiatry. Available evidence
indicates that the trace amine-associated receptor 1 (TAAR1) agonist SEP-363856 is …

Ulotaront: a TAAR1 agonist for the treatment of schizophrenia

MLR Heffernan, LW Herman, S Brown… - ACS medicinal …, 2021 - ACS Publications
Ulotaront (SEP-363856) is a trace-amine associated receptor 1 (TAAR1) agonist with 5-
HT1A receptor agonist activity in Phase 3 clinical development, with FDA Breakthrough …

[HTML][HTML] Pharmacophore modeling, 3D-QSAR, docking study and ADME prediction of acyl 1, 3, 4-thiadiazole amides and sulfonamides as antitubulin agents

MF Khan, G Verma, W Akhtar… - Arabian Journal of …, 2019 - Elsevier
Pharmacophore modeling, molecular docking, and in silico ADME studies have been
carried out to determine the binding mode and drug likeliness profile of acyl 1, 3, 4 …

Different Circulating Trace Amine Profiles in De Novo and Treated Parkinson's Disease Patients

G D'Andrea, G Pizzolato, A Gucciardi, M Stocchero… - Scientific Reports, 2019 - nature.com
Early diagnosis of Parkinson's disease (PD) remains a challenge to date. New evidence
highlights the potential clinical value of circulating trace amines (TAs) in early-stage PD and …

Identification of a potent human trace amine-associated receptor 1 antagonist

AM Decker, MF Brackeen… - ACS chemical …, 2022 - ACS Publications
Human trace amine-associated receptor subtype 1 (hTAAR1) is a G protein-coupled
receptor that has therapeutic potential for multiple diseases, including schizophrenia, drug …

Discovery of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 2-(5-(4′-Chloro-[1,1′-biphenyl]-4-yl)-4H-1,2,4-triazol-3-yl)ethan-1-amine (LK00764) for the …

M Krasavin, A Lukin, I Sukhanov, AS Gerasimov… - Biomolecules, 2022 - mdpi.com
A focused in-house library of about 1000 compounds comprising various heterocyclic motifs
in combination with structural fragments similar to β-phenylethylamine or tyramine was …

Finding a potential dipeptidyl peptidase-4 (DPP-4) inhibitor for type-2 diabetes treatment based on molecular docking, pharmacophore generation, and molecular …

H Meduru, YT Wang, JJP Tsai, YC Chen - International journal of …, 2016 - mdpi.com
Dipeptidyl peptidase-4 (DPP-4) is the vital enzyme that is responsible for inactivating
intestinal peptides glucagon like peptide-1 (GLP-1) and Gastric inhibitory polypeptide (GIP) …

Novel biguanide-based derivatives scouted as TAAR1 agonists: Synthesis, biological evaluation, ADME prediction and molecular docking studies

M Tonelli, S Espinoza, RR Gainetdinov… - European Journal of …, 2017 - Elsevier
Trace amines (TAs) are endogenous neuromodulators that play a functional role in the
synaptic transmission within central nervous system (CNS), targeting trace amine …

Overlap and specificity in the substrate spectra of human monoamine transporters and organic cation transporters 1, 2, and 3

L Gebauer, O Jensen, M Neif, J Brockmöller… - International Journal of …, 2021 - mdpi.com
Human monoamine transporters (MATs) are cation transporters critically involved in
neuronal signal transmission. While inhibitors of MATs have been intensively studied, their …