Last update 01 Nov 2024

GPR171

Last update 01 Nov 2024

Basic Info

Synonyms

G protein-coupled receptor 171, G-protein coupled receptor 171, G-protein coupled receptor H963

+ [4]

Introduction

G-protein coupled receptor for Big LEN, a 16-amino acid neuropeptide produced from the precursor protein, proSAAS (encoded by PCSK1N). Acts through a G(i)-alpha-mediated pathway in response to Big LEN. Big LEN-GPR171 system plays an important role in regulating feeding and metabolism. Also plays a role in modulating fear and anxiety-like behaviors in the basolateral amygdala. Big LEN-GPR171 modulates the mu-type opioid receptor signaling and antinociception (By similarity). Acts as a negative regulator T cell function (PubMed:34615877).

Drugs associated with GPR171

MS0015203

Target

GPR171

Mechanism

GPR171 agonists

Active Org.

Icahn School of Medicine at Mount Sinai

Originator Org.

Icahn School of Medicine at Mount Sinai

Active Indication

Anxiety Disorders [+1]

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Targeting GPR171 small molecule (ConfometRx)

Target

GPR171

Mechanism

GPR171 agonists

Active Org.

ConfometRx, Inc.

Originator Org.

ConfometRx, Inc.

Active Indication

Pain

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with GPR171

100 Translational Medicine associated with GPR171

0 Patents (Medical) associated with GPR171

Literatures (Medical) associated with GPR171

09 Aug 2024·Medicine

Bioinformatics analysis of the tumor microenvironment in melanoma – Constructing a prognostic model based on CD8+ T cell-related genes: An observational study

Article

Author: He, Zhenghao ; Luo, Zhijun ; Chen, Manli

This research endeavor seeks to explore the microenvironment of melanoma tumors and construct a prognostic model by focusing on genes specific to CD8+ T cells. The single-cell sequencing data of melanoma underwent processing with the Seurat package, subsequent to which cell communication network analysis was conducted using the iTALK package and transcription factor analysis was performed using the SCENIC package. Univariate COX and LASSO regression analyses were utilized to pinpoint genes linked to the prognosis of melanoma patients, culminating in the creation of a prognostic model through multivariate COX analysis. The model was validated using the GSE65904 and GSE35640 datasets. Multi-omics analysis was conducted utilizing the maftools, limma, edgeR, ChAMP, and clusterProfiler packages. The examination of single-cell sequencing data revealed the presence of 8 cell types, with the transcription factors RFXAP, CLOCK, MGA, RBBP, and ZNF836 exhibiting notably high expression levels in CD8+ T cells as determined by the SCENIC package. Utilizing these transcription factors and their associated target genes, a prognostic model was developed through COX and LASSO analyses, incorporating the genes GPR171, FAM174A, and BPI. This study validated the model with independent datasets and conducted additional analysis involving multi-omics and immune infiltration to identify a more favorable prognosis for patients in the low-risk group. The findings provide valuable insights into the tumor microenvironment of melanoma and establish a reliable prognostic model. The integration of multi-omics and immune infiltration analyses enhances our understanding of the pathogenesis of melanoma. The identification of specific genes holds promise as potential biomarkers for individuals with melanoma, serving as important indicators for predicting patient outcomes and determining their response to immunotherapy.

27 Jun 2024·Journal of Medicinal Chemistry

Potent, Selective Agonists for the Cannabinoid-like Orphan G Protein-Coupled Receptor GPR18: A Promising Drug Target for Cancer and Immunity

Article

Author: Oneto, Angelo ; Namasivayam, Vigneshwaran ; Łażewska, Dorota ; Kieć-Kononowicz, Katarzyna ; Latacz, Gniewomir ; Boshta, Nader M ; Kremers, Sarah ; Schoeder, Clara T ; Mahardhika, Andhika B ; Neumann, Alexander ; Schabikowski, Jakub ; Załuski, Michal ; Müller, Christa E ; Ressemann, Anastasiia ; Perri, Filomena

The human orphan G protein-coupled receptor GPR18, activated by Δ⁹-tetrahydrocannabinol (THC), constitutes a promising drug target in immunology and cancer. However, studies on GPR18 are hampered by the lack of suitable tool compounds. In the present study, potent and selective GPR18 agonists were developed showing low nanomolar potency at human and mouse GPR18, determined in β-arrestin recruitment assays. Structure-activity relationships were analyzed, and selectivity versus cannabinoid (CB) and CB-like receptors was assessed. Compound 51 (PSB-KK1415, EC₅₀ 19.1 nM) was the most potent GPR18 agonist showing at least 25-fold selectivity versus CB receptors. The most selective GPR18 agonist 50 (PSB-KK1445, EC₅₀ 45.4 nM) displayed >200-fold selectivity versus both CB receptor subtypes, GPR55, and GPR183. The new GPR18 agonists showed minimal species differences, while THC acted as a weak partial agonist at the mouse receptor. The newly discovered compounds represent the most potent and selective GPR18 agonists reported to date.

14 Jun 2024·Combinatorial Chemistry & High Throughput Screening

Establishing a Ten Disulfidptosis-related Gene Signature for Prognostic Prediction in Skin Cutaneous Melanoma

Article

Author: Li, Haiyan ; Chen, Zedong ; Cai, Limin ; Huang, Yuanjie ; Chen, Chen

Aim:Disulfidptosis is a new metabolic-related regulated cell death associated with cancer growth. This study aimed to investigate the molecular mechanisms associated with disulfidptosis in skin cutaneous melanoma (SKCM) and establish a disulfidptosis-related gene signature for prognostic prediction in SKCM.Methods:Disulfidptosis-associated genes were identified from RNA-seq data of SKCM. A risk score signature was developed and validated through univariate Cox and LASSO analyses. Additionally, the immune microenvironment related to the risk score signature was investigated. Finally, a disulfidptosis-related genes-transcription factor -miRNA network was developed, and the expression levels of five disulfidptosis-related genes were initially verified in SKCM cell lines.Results:A total of 107 disulfidptosis-related differentially expressed genes in SKCM samples were identified. A ten-disulfidptosis-gene signature was established, including BIN2, CCL3L3, CCL8, CD79A, CIITA, CXCR3, DEFB1, GPR171, IL2RB, and SOCS1. The SKCM samples were divided into high- and low-risk groups, of which samples in the low-risk group showed better survival performance. The receiver operating characteristic curve analysis confirmed the good potency of the disulfidptosis-related gene prognostic model. Except for DEFB1, the other nine genes were positively related with T cell CD8+, T cell CD4+ memory activated, T cell gamma delta, NK cell activated, and macrophage M1, and they were all negatively related with NK cell resting, macrophage M0, macrophage M2, and mast cell activated. Finally, we verified downregulated levels of SOCS1 and DEFB1 and upregulated CXCR3, BIN2, and CCL3L3 in A875 and A375.Conclusion:We successfully established ten disulfidptosis-related genes' prediction prognostic signatures for SKCM patients.

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GPR171

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