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 company and world-leader in GPCR1-focused structure-based drug design (SBDD) and development, an d 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

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

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.

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

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

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 reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally involved in colon cancer

targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer Depletion of GPR108 dramatically inhibited the survival of various cancers. Furthermore, in vitro and in vivo assays demonstrated that GA was dependent on GPR108 to exert anti-cancer 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

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid receptor-dependent activation of EGFR "Background Fentanyl is an opioid analgesic and is widely used in ovarian cancer 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

September 2022 "Background Cancer driver genes are usually ranked by mutation frequency, which does with few driver mutations overall, because these few mutations should be strong enough to initiate 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

September 2022 "Research on cancer therapies focuses on processes such as angiogenesis, cell signaling last decade, increasing evidence of its antitumoral properties in more than a dozen different types of cancer

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

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

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

Upregulated in Hepatocellular Carcinoma "Hepatocellular carcinoma (HCC) is at the forefront of the global cancer , with some members of the RGS family being associated with liver cancer as well. Considering this, we investigated the role of RGS20 as a potential prognostic marker in 28 different cancer By using the Cancer Genome Atlas (TCGA) and Gene Expression Omnibus (GEO) data, our analysis revealed Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer."

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

bioactive phospholipids implicated in a wide range of cellular activities that regulate a diverse array of biological of attention because of its involvement in various diseases, such as idiopathic pulmonary fibrosis, cancers

and infectious diseases (Proudfoot 2002), and in recent years attention has increasingly focused on cancer The involvement of chemokines and their receptors in several aspects of cancer biology, represents a inhibitor of the CCR5 used in HIV therapy; and the small molecule plerixafor, a CXCR4 antagonist used in cancer A lot of effort has been put forward to target CKRs especially in cancer, nevertheless, targeting this receptors redundancy and the fact that different chemokine receptors are overexpressed and promote cancer

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

previous phase III clinical candidate for the treatment of Crohn's disease, we developed a chemical biology

, 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 Individual cancer types were enriched for highly impactful, recurrent mutations at selected cognate positions 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

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology,

September 2022 Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR and a middle sized flexible molecule "A GA-guided multidimensional virtual-system coupled molecular dynamics (GA-mD-VcMD) simulation was conducted to elucidate binding mechanisms of a middle-sized flexible molecule, bosentan, to a GPCR protein, human endothelin receptor type B (hETB). GA-mD-VcMD is a generalized ensemble method that produces a free-energy landscape of the ligand-receptor binding by searching large-scale motions accompanied with stable maintenance of the fragile cell-membrane structure. All molecular components (bosentan, hETB, membrane, and solvent) were represented with an all-atom model. Then sampling was conducted from conformations where bosentan was distant from the binding site in the hETB binding pocket. The deepest basin in the resultant free-energy landscape was assigned to native-like complex conformation. The following binding mechanism was inferred. First, bosentan fluctuating randomly in solution is captured using a tip region of the flexible N-terminal tail of hETB via nonspecific attractive interactions (fly casting). Bosentan then slides occasionally from the tip to the root of the N-terminal tail (ligand–sliding). During this sliding, bosentan passes the gate of the binding pocket from outside to inside of the pocket with an accompanying rapid reduction of the molecular orientational variety of bosentan (orientational selection). Last, in the pocket, ligand–receptor attractive native contacts are formed. Eventually, the native-like complex is completed. The bosentan-captured conformations by the tip-region and root-region of the N-terminal tail correspond to two basins in the free-energy landscape. The ligand-sliding corresponds to overcoming of a free-energy barrier between the basins." Read more at the source #DrGPCR #GPCR #IndustryNews