Introduction of HTR7
HTR7 belongs to the G protein-coupled serotonin receptor family which has seven transmembrane domains. It is encoded by HTR7 gene and exists three different splice variants with different carboxy terminals. The receptor couples with Gs subunit of cell surface involving in regulating the production of intracellular signaling molecule cAMP and multiple signaling pathway transductions. Recently, a lot of studies indicate that the receptor can be used as a drug development target for the treatment of several clinical disorders, such as neuromodulation disorder, mental disorders.
|Basic Information of HTR7|
|Protein Name||5-hydroxytryptamine receptor 7|
|Organism||Homo sapiens (Human)|
Function of HTR7 Membrane Protein
Activated HTR7 by binding to its ligands (serotonin, a biogenic neurotransmitter and hormone) can stimulate the activation of adenylate cyclase, thus increasing the production of intracellular second messenger cAMP. The receptor is especially expressed in the brain areas, such as hippocampus, hypothalamus, and cortex. It can increase the density of dendritic spines and promote synaptogenesis in forebrain neurons and regulate neurotransmission. Previous studies have indicated that HTR7 is involved in regulating a variety of biological processes, including thermoregulation, circadian rhythm, mood, learning and memory, and sleep. Hence, HTR7 may be a potential drug target for the treatment of several clinical disorders, such as cognitive disturbances, sleep and circadian rhythmicity disorders, anxiety and depression. And HTR7 antagonists might be used to treat the cognitive definitive deficits and mood disorders. Besides, recent findings show that HTR7 also regulates inflammatory response. For example, HTR7 regulates inflammatory fibrotic process induced by chronic liver injury and 5-HT7 agonist may protect liver tissue from liver fibrosis. HTR7 also plays a critical role in acute and chronic inflammation of the gastrointestinal tract. In addition, some studies show that the functions of HTR7 are required in regulating mammary epithelial structure and function, thus providing a new therapeutic target for mastitis and breast cancer treatment.
Fig.1 Stimulation of HTR7: schematic drawing of signaling pathways and downstream effectors leading to remodeling of neuronal morphology conservation. (Volpicelli F, 2014)
Application of HTR7 Membrane Protein in Literature
The study shows that 5-HTR7 agonist can reduce amyloid beta (Aβ) plaque accumulation and neuronal apoptosis, thereby improving cognition and memory performance. So the 5-HTR7 agonist, AS19, may be a useful therapeutic drug for Alzheimer's disease.
The study suggests that the selective agonist, LP-211 can activate 5-HT7 receptor, thereby regulating explorative-curiosity behavior in rats with differing in visual and spatial memory.
The research indicates that sensitization of capsaicin-sensitive primary sensory neurons by 5-HT7 receptors may result in facilitation of neurogenic inflammation involving calcitonin gene-related peptide (CGRP) in the rat hind paw.
The study indicates that exosome biomarkers can be used for early diagnosis and prognosis of breast cancer patients in clinic. And exosome-carrying TRPC5, NANOG, NEUROD1, HTR7, KISS1R, and HOXC are related to progression-free survival (PFS), overall survival (OS) or disease-free survival (DFS) in breast cancer.
The study shows that 5-HT7 receptor in the ventral hippocampus is involved in the mediation of retrieval of fear memory and stress-induced defecation. 5-HT7 receptor might be used as a drug target for treating mental disorders involving fear memory and gastrointestinal problems.
HTR7 Preparation Options
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