Trim27: A Tripartite Motif-Containing G protein-Coupled Receptor for Drug Targeting

Target Name: TRIM27

NCBI ID: G5987

TRIM27

Trim27: A Tripartite Motif-Containing G protein-Coupled Receptor for Drug Targeting

Introduction

TRIM27, a member of the G protein-coupled receptor (GPCR) family, is a potential drug target and biomarker for various diseases. The GPCR family is a signal transduction molecule widely present in the body, responsible for sensing external stimuli and This translates into biochemical reactions within the cell. TRIM27, as a GPCR, plays an important role in a variety of physiological and pathological processes. This article will elaborate on the structure, function, pharmacology and application prospects of TRIM27 in drug research and development.

structure

TRIM27 is a short signal peptide containing three conserved tripartite domains: 伪-helix, 尾-sheet, and 纬-turn. Its gene coding region is located on human chromosome 11 (11p15.2). TRIM27 is composed of two heterologous termini, one from mouse and the other from human.

Function

TRIM27 is a GPCR that is mainly involved in cell signal transduction processes. It plays an important role in a variety of physiological processes, such as cell proliferation, differentiation, migration, and apoptosis. TRIM27 also plays a key role during tumor occurrence and development. Studies have shown that the expression level of TRIM27 is related to the invasion and metastasis capabilities of various tumors. In addition, TRIM27 plays an important role in immune cell functions, such as T cell activation, B cell activation, and memory cell development.

Pharmacology

As a drug target, TRIM27 has high pharmacological value. Currently, there are multiple drugs targeting TRIM27 entering clinical research. These drugs mainly target the active site of TRIM27 and block the TRIM27-mediated signal transduction pathway by interfering with the interaction between TRIM27 and its target.

Drug research and development for TRIM27 mainly focuses on the following aspects:

1. Compounds that antagonize the active site of TRIM27: These compounds can inhibit the signal transduction activity of TRIM27 by specifically interacting with the active site of TRIM27. For example, some compounds, such as BHQ-1, BHQ-2 and BHQ-3, are known to have such effects.

2. Block the interaction between TRIM27 and the target: These compounds can block the TRIM27-mediated signal transduction pathway by interfering with the binding of TRIM27 to the target protein. For example, using gene editing technology, the gene of TRIM27 can be modified so that it cannot bind to certain target proteins.

3. Modulate the activity of TRIM27: Some drugs change the activity of TRIM27 by regulating the phosphorylation status, protein level or intracellular localization of TRIM27. These drugs may have different mechanisms of action, but they all affect the role of TRIM27 in cells.

4. Drugs targeting TRIM27: Drugs targeting TRIM27 mainly exert anti-tumor and immunomodulatory effects by inhibiting the expression of TRIM27 in tumor cells and immune cells. These drugs include immune checkpoint inhibitors, vascular endothelial growth factor (VEGF) antagonists, and prostate cancer cell growth inhibitors.

in conclusion

TRIM27 is a GPCR with a wide range of physiological and pathological functions. Through studies on its structure, function and pharmacology, it can be discovered that TRIM27 plays a key role in biological processes such as tumor occurrence, development, and immune response. At present, drug research targeting TRIM27 has made some progress, but there are still many challenges that need to be overcome. In the future, with the continuous development of medicinal chemistry technology and bioinformatics technology, it is expected to more effectively explore the application value of TRIM27 in drug research and development.

Protein Name: Tripartite Motif Containing 27

Functions: E3 ubiquitin-protein ligase that mediates ubiquitination of various substrates and thereby plays a role in diffent processes including proliferation, apoptosis, immune response or autophagy (PubMed:24144979, PubMed:29688809, PubMed:36111389). Ubiquitinates PIK3C2B and inhibits its activity by mediating the formation of 'Lys-48'-linked polyubiquitin chains; the function inhibits CD4 T-cell activation. Acts as a regulator of retrograde transport: together with MAGEL2, mediates the formation of 'Lys-63'-linked polyubiquitin chains at 'Lys-220' of WASHC1, leading to promote endosomal F-actin assembly (PubMed:23452853). Has a transcriptional repressor activity by cooperating with EPC1. Induces apoptosis by activating Jun N-terminal kinase and p38 kinase and also increases caspase-3-like activity independently of mitochondrial events. May function in male germ cell development. Has DNA-binding activity and preferentially bound to double-stranded DNA. Forms a complex with and ubiquitinates the ubiquitin-specific protease USP7, which in turn deubiquitinates RIPK1 resulting in the positive regulation of TNF-alpha-induced apoptosis (PubMed:24144979). In addition, acts with USP7 or PTPN11 as an inhibitor of the antiviral signaling pathway by promoting kinase TBK1 ubiquitination and degradation (PubMed:26358190, PubMed:29688809). Alternatively, facilitates mitophagy via stabilization of active TBK1 (PubMed:36111389). Negatively regulates autophagy flux under basal conditions by directly polyubiquitinating ULK1 (PubMed:35670107). During starvation-induced autophagy, catalyzes non-degradative ubiquitination of the kinase STK38L promoting its activation and phosphorylation of ULK1 leading to its ubiquitination and degradation to restrain the amplitude and duration of autophagy (PubMed:35670107)

The "TRIM27 Target / Biomarker Review Report" is a customizable review of hundreds up to thousends of related scientific research literature by AI technology, covering specific information about TRIM27 comprehensively, including but not limited to:
•   general information;
•   protein structure and compound binding;
•   protein biological mechanisms;
•   its importance;
•   the target screening and validation;
•   expression level;
•   disease relevance;
•   drug resistance;
•   related combination drugs;
•   pharmacochemistry experiments;
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•   advantages and risks of development, etc.
The report is helpful for project application, drug molecule design, research progress updates, publication of research papers, patent applications, etc. If you are interested to get a full version of this report, please feel free to contact us at BD@silexon.ai

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