Pharmacology of human trace amine‐associated receptors: Therapeutic opportunities and challenges☆

@article{Berry2017PharmacologyOH,
  title={Pharmacology of human trace amine‐associated receptors: Therapeutic opportunities and challenges☆},
  author={Mark D. Berry and Raul R. Gainetdinov and Marius C. Hoener and Mohammed Shahid},
  journal={Pharmacology \& Therapeutics},
  year={2017},
  volume={180},
  pages={161–180}
}
&NA; 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 amines. Initial optimism quickly faded, however, as the TAAR family presented a series of challenges preventing the use of standard medicinal chemistry and pharmacology technologies. Consequently the development of basic tools for probing TAAR and translating findings from model systems to humans has been… Expand
Trace amine-associated receptor 1: a multimodal therapeutic target for neuropsychiatric diseases
TLDR
A combination of preclinical and translationally driven studies has solidified TAAR1 as a key node in the regulation of dopaminergic signaling and holds great promise as a therapeutic target for mental illness, addiction, and sleep disorders. Expand
Trace Amine-Associated Receptors as Novel Therapeutic Targets for Immunomodulatory Disorders
TLDR
A model whereby TAARs may be considered as a novel therapeutic target for disorders associated with dysregulated immune responses to environmental factors is developed, hypothesizing that altered trace amine homeostasis results in hyperactivity of the immune system. Expand
Trace Amine-Associated Receptor 1 (TAAR1): A new drug target for psychiatry?
TLDR
There is evidence to suggest that TAAR1 may be a promising therapeutic target for the treatment of schizophrenia, psychosis in Parkinson's disease, substance use disorders, and the metabolic syndrome and obesity. Expand
Trace amine associated receptor 1 (TAAR1) modulators: a patent review (2010-present)
  • M. Tonelli, Elena Cichero
  • Chemistry, Medicine
  • Expert opinion on therapeutic patents
  • 2019
TLDR
The discovery of TAAR receptors has allowed better investigation of the role played by TAs, not only as secondary neuromodulators, but also as neurotransmitters, even if it should still be completely clarified. Expand
Biochemical and Functional Characterization of the Trace Amine-Associated Receptor 1 (TAAR1) Agonist RO5263397
TLDR
RO5263397 not only increases cAMP levels at very low concentrations but also can induce the phosphorylation of ERK and CREB in a concentration- and time-dependent manner, which provides new insight on intracellular signaling pathway and other neurotransmitter receptors modulated by TAAR1 receptor activation. Expand
Molecular Variants in Human Trace Amine-Associated Receptors and Their Implications in Mental and Metabolic Disorders
TLDR
A comprehensive review of the available evidence on the pathophysiological implications of genetic variants in the human trace amine-associated receptor (TAAR) superfamily finds dysregulations of TAARs have been identified in brain disorders characterized by cognitive impairment. Expand
Validation of a High-Throughput Calcium Mobilization Assay for the Human Trace Amine-Associated Receptor 1
TLDR
A robust, 3-addition high-throughput screening (HTS) calcium mobilization assay using stable CHO-Gαq16-hTAAR1 cells, which functionally couple hTAar1 to the promiscuous G αq16 protein and thus allow signal transduction to occur through mobilization of internal calcium. Expand
Trace Amine-Associated Receptor 1 Contributes to Diverse Functional Actions of O-Phenyl-Iodotyramine in Mice but Not to the Effects of Monoamine-Based Antidepressants
  • I. Mantas, M. Millan, +7 authors Xiaoqun Zhang
  • Medicine
  • International journal of molecular sciences
  • 2021
Trace Amine-Associated Receptor 1 (TAAR1) is a potential target for the treatment of depression and other CNS disorders. However, the precise functional roles of TAAR1 to the actions of clinicallyExpand
Actions of Trace Amines in the Brain-Gut-Microbiome Axis via Trace Amine-Associated Receptor-1 (TAAR1)
TLDR
It is hypothesized that a therapeutic benefit of TAAR1 specific compounds in clinical trials in the brain-gut-microbiome axis, as well as a potential for thoughtful manipulation of the brain/gut/microbiomes axis to modulate symptoms of neuropsychiatric disease. Expand
Genetic Deletion of Trace-Amine Associated Receptor 9 (TAAR9) in Rats Leads to Decreased Blood Cholesterol Levels
TLDR
Role of TAAR9 in cholesterol regulation not only brings a new understanding of mechanisms and biological pathways of lipid exchange but also provides a new potential drug target for disorders involving cholesterol-related pathology, such as atherosclerosis. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 237 REFERENCES
Further Insights Into the Pharmacology of the Human Trace Amine‐Associated Receptors: Discovery of Novel Ligands for TAAR1 by a Virtual Screening Approach
TLDR
An homology model for the hTAAR1 was used and several agonists and one antagonist, with activities in the low micromolar range were found, which could represent the starting point for the development of more potent and selective TAAR1 ligands. Expand
Insights into the Structure and Pharmacology of the Human Trace Amine‐Associated Receptor 1 (hTAAR1): Homology Modelling and Docking Studies
TLDR
A homology model for the hTAAR1 receptor was derived and an opportunity to reasonably identify the h TAAR1 key residues involved in ligand recognition and thus define important starting points to design new agonists was provided. Expand
Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.
TLDR
The successful expression of human and mouse TAAR1 and the characterization of their responses to various natural and synthetic agonists raise new possibilities about the mechanism of some of the imidazoline-related agents. Expand
A renaissance in trace amines inspired by a novel GPCR family.
TLDR
The recent discovery of a novel family of G-protein-coupled receptors that includes individual members that are highly specific for TAs indicates a potential role forTAs as vertebrate neurotransmitters or neuromodulators, although the majority of these GPCRs so far have not been demonstrated to be activated by TAs. Expand
The potential of trace amines and their receptors for treating neurological and psychiatric diseases.
  • M. D. Berry
  • Biology, Medicine
  • Reviews on recent clinical trials
  • 2007
TLDR
The aim of the current article is to review the previous studies linking trace amines to human pathology in the context of the recently discovered trace amine receptors and evidence of the existence of Trace amine receptor polymorphisms and mutations associated with such disorders. Expand
International Union of Pharmacology. LXXII. Recommendations for Trace Amine Receptor Nomenclature
TLDR
This review proposes an official nomenclature designating TAAR1 as the trace amine 1 receptor following the convention of naming receptors after the endogenous agonist, abbreviated to TA1 where necessary. Expand
Trace Amine-Associated Receptor 1 Partial Agonism Reveals Novel Paradigm for Neuropsychiatric Therapeutics
TLDR
With the first potent and selective TAAR1 partial agonist, RO5203648, it is shown that TAar1 is implicated in a broad range of relevant physiological, behavioral, and cognitive neuropsychiatric dimensions and suggest that agonists at this receptor might have therapeutic potential in one or more Neuropsychiatric domains. Expand
Trace Amines and the Trace Amine-Associated Receptor 1: Pharmacology, Neurochemistry, and Clinical Implications
TLDR
TAAR1 is uniquely positioned to exert direct control over DA and 5-HT neuronal firing and release, which has profound implications for understanding the pathophysiology of, and therefore designing more efficacious therapeutic interventions for, a range of neuropsychiatric disorders that involve aminergic dysregulation. Expand
Trace amine-associated receptors form structurally and functionally distinct subfamilies of novel G protein-coupled receptors.
TLDR
A uniform nomenclature is proposed describing this novel GPCR family in all mammalian species as trace-amine-associated receptors (TAARs), which resolves the ambiguities and contradictions of the previous naming. Expand
The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia
Trace amines have been implicated in a number of neuropsychiatric disorders including depression and schizophrenia. Although long known to modulate neurotransmission indirectly through the release ofExpand
...
1
2
3
4
5
...