September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid cancer patients for pain management. Although increasing evidence has suggested the direct role of fentanyl on cancer, little is known on the effect of fentanyl on ovarian cancer cells. Methods Proliferation, migration and apoptosis assays were performed in ovarian cancer cells after fentanyl

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in

September 2022 High GPER expression in triple-negative breast cancer is linked to pro-metastatic pathways and predicts poor patient outcomes "Triple-negative breast cancer (TNBC) is a particularly aggressive It is generally considered that TNBC is an estrogen-independent breast cancer, while a new estrogen receptor In quantitative comparison, GPER abundance is correlated with the high-risk subtype of TNBC. metastasis, TNM stage III as well as nuclear grade G3 tumors.

October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the Moreover, in the presence of very high levels of HH, the second effect of FU leads to the local enrichment

Though most of these variants exhibit a loss of function, the molecular defects caused by these underlying scanning to quantitatively compare the plasma membrane expression of 123 known pathogenic rhodopsin variants We identify 69 retinopathy variants, including 20 previously uncharacterized variants, that exhibit diminished Of these apparent class II variants, 67 exhibit a measurable increase in expression in the presence of Nevertheless, estimates from computational modeling suggest that many of the least sensitive variants

July 2022 Cancer Research UK and Sosei Heptares sign agreement to advance cancer immunotherapy candidate into clinical trials "HTL0039732 is a novel EP4 antagonist with potential to treat a wide range of cancers biopharmaceutical company and world-leader in GPCR1-focused structure-based drug design (SBDD) and development, and Cancer Research UK, the world’s largest private funder of cancer research, today announce the signing of an agreement to bring Sosei Heptares’ cancer immunotherapy drug candidate into a first-in-human trial."

September 2022 "Background: Colorectal cancer is the third most common cancer and requires more prognostic The clinical significance of GPR39 in colon cancer has never been reported. Materials: In our study, we compared GPR39 expression between colon cancers and tumor-adjacent tissues by retrieving TCGA data and detected the expression of GPR39 in colon cancers with qPCR and immunohistochemistry

Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled receptors , arrestins, and effectors, activate downstream pathways that often modulate hallmark mechanisms of cancer To test this possibility, we systematically aggregated somatic cancer mutations across class A GPCRs The possibility that multiple different GPCRs could moonlight as drivers or enablers of a given cancer through mutations located at cognate positions across GPCR paralogs opens a window into cancer mechanisms

, with some members of the RGS family being associated with liver cancer as well. By using the Cancer Genome Atlas (TCGA) and Gene Expression Omnibus (GEO) data, our analysis revealed was strongly associated with some important clinical parameters such as alpha-fetoprotein and tumor grade (clear renal cell carcinoma: p < 0.001, lung adenocarcinoma: p = 0.004, mesothelioma: p = 0.039, ovarian serous cystadenocarcinoma: p = 0.048); (d) RGS20 was found to be significantly associated with some

September 2022 "Research on cancer therapies focuses on processes such as angiogenesis, cell signaling Propranolol, initially prescribed for high blood pressure, irregular heart rate, essential tremor, and last decade, increasing evidence of its antitumoral properties in more than a dozen different types of cancer

September 2022 Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin Signaling Axis by Repurposing Vaptans "Men with advanced prostate cancer are treated by androgen deprivation therapy but the disease recurs as incurable castration-resistant prostate cancer (CRPC), requiring new Interrogation of prostate cancer patient sample data revealed that coexpression of AVPR1A and AVPR2 is

regulating proliferation, inflammation, adhesion, migration, insulin release, muscle relaxation, and cancer Several recent studies have demonstrated that TGR5 exerts inconsistent effects in different cancer cells

involved in a wide array of physiological and disease functions, yet knowledge of their role in colon cancer Indeed, EZH2 is found to be directly correlated with high PAR4-driven tumors, and is abundantly expressed reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally involved in colon cancer

October 2022 Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent targeted in a wide range of diseases, but few therapies have been directed against GPCRs in the field of cancer Here, using colorectal cancer (CRC) as a model, we explored the gene expression of a panel of GPCRs in We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with effective at monitoring real-time A2BAR receptor labeling using live-imaging modalities, and displayed high

September 2022 GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response However, its biological function and underlying molecular mechanism in breast cancer have not been clearly Here, we demonstrated that GASP1 was highly expressed in breast cancers, and patients harboring altered Functional studies showed that GASP1 knockout significantly suppressed malignant properties of breast cancer Collectively, this study demonstrates that GASP1 enhances malignant behaviors of breast cancer cells

targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic target of cancer Depletion of GPR108 dramatically inhibited the survival of various cancers. Overall, our findings supported GPR108 as a promising therapeutic target of cancer, and provided a small molecule inhibitor GA directly and selectively targeting GPR108 for cancer therapy."

August 2022 "Chemokines, a subgroup of cytokines along with their receptors, are involved in various biologic processes and regulation of a wide range of immune responses in different physiologic and pathologic states such as tissue repair, infection, and inflammation. C-X-C motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural ligand termed stromal-derived factor-1(SDF-1 or CXCL12). Evidence demonstrated that the ligation of SDF-1 to CXCR4 initiates several intracellular signaling pathways, regulating cell proliferation, survival, chemotaxis, migration, angiogenesis, adhesion, as well as bone marrow (BM)-resident cells homing and mobilization. Additionally, CXCR4 is expressed by tumor cells in blood malignancies and solid tumors." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "August 10, 2022 Cancer Research UK is working with global biopharma Sosei Heptares on a treatment they hope will bring immunotherapy benefits to new cancer types. Cancer Research UK, a charity dedicated to funding lifesaving oncology research, spent £388 million on cancer research last fiscal year.

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer physiological processes, these activities are also involved in the onset and progression of various cancers primary emphasis on the signaling processes which underlie the mechanism of β-arrestins in the onset of cancer processes has important implications for understanding the therapeutic intervention and treatment of cancer

September 2022 "Background Cancer driver genes are usually ranked by mutation frequency, which does not with few driver mutations overall, because these few mutations should be strong enough to initiate cancer

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer physiological processes, these activities are also involved in the onset and progression of various cancers primary emphasis on the signaling processes which underlie the mechanism of β-arrestins in the onset of cancer processes has important implications for understanding the therapeutic intervention and treatment of cancer

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin Signalling and Migration "Kisspeptin is an anti-metastatic mediator in many cancer types, acting through However, controversy remains regarding its role in breast cancer since both pro- and anti-metastatic In KISS1R overexpressing triple-negative breast cancer (TNBC) cells, stimulation has been associated

September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer adenocarcinoma (PDAC) remains an aggressive disease that is expected to become the second cause of cancer -mediated knockdown of YES1 and transfection of epitogue-tagged YAP mutants in PANC-1 and MiaPaCa-2 cancer

October 2022 ADGRL3 genomic variation implicated in neurogenesis and ADHD links functional effects to and in linkage with ADHD in disparate populations from the world over, are predicted as pathogenic variants

However, the role of β2-AR in oral cancer is not well identified.

Biotechnology Inc. and Trevena Inc. could offer potential new weapons against omicron and future viral variants While vaccine-makers race to test their shots against the variant, the monoclonal antibody sotrovimab Sotrovimab is the first monoclonal antibody showing preclinical efficacy against all COVID-19 variants

of attention because of its involvement in various diseases, such as idiopathic pulmonary fibrosis, cancers

sensory #ionchannels to the group leader at the University of Utah investigating Class F #GPCRs in #cancer