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HTR6 Membrane Protein Introduction

Introduction of HTR6

HTR6, encoded by HTR6 gene, is a member of the seven-transmembrane G protein-coupled receptor family, coupled with the Gs alpha subunit. It is found in the central and peripheral nervous systems, involved in the mediation of excitatory and inhibitory neurotransmission. Now most studies are designed to investigate the characters of HTR6 acting as a potential therapeutic target for neurological disorders, such as Alzheimer's disease.

Basic Information of HTR6
Protein Name 5-hydroxytryptamine receptor 6
Gene Name HTR6
Aliases 5-HT6, 5-HT6R
Organism Homo sapiens (Human)
UniProt ID P50406
Transmembrane Times 7
Length (aa) 440
Sequence MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC
RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP
RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG
LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP
RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF
FNIDPAEPELRPHPLGIPTN

Function of HTR6 Membrane Protein

HTR6 is one of the several different receptors for 5-hydroxytryptamine (serotonin) which is a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activated receptor by interacting with serotonin promotes adenylate cyclase, resulting in the activation of cyclic AMP-dependent signaling pathway. It is reported that the receptor functions as a regulator of cholinergic neuronal transmission in the brain and is associated with neurological disorders, such as Alzheimer's disease, depression, schizophrenia, and epilepsy. Moreover, most studies have been identified that inhibition of HTR6 can relieve the impairments of cognitive, working memory and behavioral flexibility which is linked to Alzheimer's disease. Hence HTR6 can be used as a promising therapeutic target for treating neurological disorders. Recently more and more antidepressants and antipsychotic drugs targeting toward to HTR6 have been developed for neurological disorders treatment and they have a high affinity with HTR6.

HTR6 has been proposed as a promising drug target for cognition enhancement in AD. Fig.1 HTR6 has been proposed as a promising drug target for cognition enhancement in AD. (Benhamú B, 2014)

Application of HTR6 Membrane Protein in Literature

  1. Amodeo D.A., et al. 5-HT6 receptor agonist EMD386088 impairs behavioral flexibility and working memory. Behavioural Brain Research. 2018, 349: 8-15. PubMed ID: 29715539

    The study indicates that the inhibition of 5-HT6 receptor may be an effective therapeutic strategy for relieving working memory and behavioral flexibility impairments associated with neuropsychiatric disorders such as Alzheimer's disease and schizophrenia.

  2. Hashemi-Firouzi N., et al. 5-Hydroxytryptamine receptor 6 antagonist, SB258585 exerts neuroprotection in a rat model of Streptozotocin-induced Alzheimer’s disease. Metabolic Brain Disease. 2018. PubMed ID: 29667108

    The research identifies 5-HT6 antagonist SB258585 can relieve cognitive and behavioral impairments associated with Alzheimer's disease (AD) via suppressing the apoptosis of hippocampus.

  3. Hu L., et al. Serotonin 5-HT6 receptors affect cognition in a mouse model of Alzheimer’s disease by regulating cilia function. Alzheimers Research & Therapy. 2017, 9(1):76. PubMed ID: 28931427

    The study suggests that 5-HT6 regulates the morphology and function of neuronal primary cilia which is linked to the axon initial segment (AIS) and axon alterations in Alzheimer's disease (AD) development. Hence 5-HT6 may be involved in the development of AD.

  4. Lalut J., et al. Modulating 5-HT4 and 5-HT6 receptors in Alzheimer's disease treatment. Future Medicinal Chemistry. 2017, 9(8):781-795. PubMed ID: 28504917

    The review reports the recent studies in the understanding of this modulation as well as the medicinal chemistry of 5-HT6R or 5-HT4R ligands from synthesis to ongoing clinical trials.

  5. Ferrero H., et al. Serotonin 5-HT6 receptor antagonists in Alzheimer's disease: therapeutic rationale and current development status. Cns Drugs. 2017, 31(1):19-32. PubMed ID: 27914038

    In this review, authors describe the recent fundamental and clinical investigations about 5-HT6 receptor as a therapeutic target for cognitive and/or behavioral symptoms of Alzheimer's disease (AD). The conclusion is made that 5-HT6 receptor antagonists can reasonably be regarded as potential drug candidates for the treatment of AD.

HTR6 Preparation Options

Based on the versatile Magic™ membrane protein production platform, Creative Biolabs can provide many flexible options for soluble and functional target protein, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-HTR6 antibody development services.


As a forward-looking research institute as well as a leading custom service provider in the field of membrane protein, Creative Biolabs has won good reputation among our worldwide customers for successfully accomplishing numerous challenging projects including generation of many functional membrane proteins. Please feel free to contact us for more information.

Reference

  1. Benhamú B, et al. (2014). Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease. Journal of Medicinal Chemistry, 57(17), 7160-81.

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