TRHR Membrane Protein Introduction

Introduction of TRHR

TRHR, a G protein-coupled receptor, is encoded by TRHR gene. It binds to the tripeptide thyrotropin releasing hormone (TRH). It has been extensively studied during the past few decades because it offers numerous possibilities for therapeutic applications. TRHR is found in the brain, and when bound with TRH, it acts to increase intracellular inositol trisphosphate through phospholipase C. Some studies reported TRH and TRHR can cause a variety of thyroidal or non-thyroidal effects, and they are regarded as biomarkers and drug candidates.

Function of TRHR Membrane Protein

TRH receptors (TRHRs) are seven transmembrane domain GTP (G)-protein coupled receptors (GPCR) that are members of group A7 of the rhodopsin-like receptor family. TRHR has been studied in detail in rodents, where two subtypes are identified and named as TRHR1 and TRHR2. TRHR plays a vital role in many biological functions, such as resisting depression, reducing anxiety and improving learning and memory. Lots of research demonstrate that TRHR is associated with several diseases, such as diabetes, breast cancer, depression, spinal cord injury, and amyotrophic lateral sclerosis. Regulation of TRH production in the hypothalamus, patterns of expression of TRH and its receptor in the body, could be beneficial for clinical therapy.

Fig.1 The hypothalamus, pituitary, and the thyroid gland.

Application of TRHR Membrane Protein in Literature

1. Moravcova R., et al. TRH receptor mobility in the plasma membrane is strongly affected by agonist binding and by interaction with some cognate signaling proteins. J Recept Signal Transduct Res. 2018, 38(1), 20-26 PubMed ID: 29137494
   
   

   This article analyzes the proliferation of receptors in the cell membranes of HEK293 cells which steadily express TRH receptor by fluorescence recovery after photobleaching (FRAP), the TRH receptor is markedly reduced upon TRH binding. Meanwhile, the same results also find in Gq/11α, Gβ, β-arrestin2, and phospholipase Cβ1, which suggests that these proteins may also play distinct roles in THR receptor-mediated signaling.

2. Nakano M., et al. Possible involvement of thyrotropin-releasing hormone receptor 3 in the release of prolactin in the metamorphosing bullfrog larvae. Gen Comp Endocrinol. 2018, 267:36-44. PubMed ID: 29864416
   
   

   Authors analyze the expression level of three types of cloned bullfrog TRHRs by reverse transcription-PCR. The data reveals TRHR3 mRNA is expressed in the anterior lobe and that the signals reside mostly in the prolactin (PRL) cells, which suggests TRHR3 mediates the action of TRH on the PRL cells to induce the release of PRL that is prerequisite for growth and metamorphosis in amphibians.

3. Zhang Y., et al. The potential role of thyrotropin-releasing hormone in colonic dysmotility induced by water avoidance stress in rats. Neuropeptides. 2018, 70:47-54. PubMed ID: 29803395
   
   

   Authors in this group investigate the effects and underlying mechanism of thyrotropin releasing hormone (TRH) on colonic contractile disorders induced by chronic water avoidance stress (WAS). These results show TRH may be related to the dysmotility induced by chronic stress.

4. Kelly J.A., et al. First-in-class thyrotropin-releasing hormone (TRH)-based compound binds to a pharmacologically distinct TRH receptor subtype in human brain and is effective in neurodegenerative models. Neuropharmacology. 2015, 89, 193-203. PubMed ID: 25281210
   
   

   This article determines the ability of JAK4D to bind to TRH receptors in human brain and to evaluate its neuropharmacological effects in neurodegenerative animal models. The result shows that JAK4D is an important tool for investigating the hitherto-unidentified central TRH receptor subtype reported herein and an attractive therapeutic candidate for neurodegenerative disorders.

5. Zhang L., et al. Intracellular postsynaptic cannabinoid receptors link thyrotropin-releasing hormone receptors to TRPC-like channels in thalamic paraventricular nucleus neurons. Neuroscience. 2015, 311, 81-91. PubMed ID: 26470810
   
   

   This article evaluates how the TRH receptors engage novel signaling pathways in PVT neurons, and the effect of postsynaptic intracellular CB1 and CB2 receptors on TRPC-like pathway. These results indicate that CB1 and CB2 suppress the TRPC-like channel opening.

TRHR Preparation Options

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