August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis "β-Arrestins are ubiquitously expressed intracellular proteins with many functions They have participated in various cellular processes such as cell proliferation, migration, apoptosis physiological processes, these activities are also involved in the onset and progression of various cancers processes has important implications for understanding the therapeutic intervention and treatment of cancer

September 2022 GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response cells, such as inhibition of cell proliferation, colony formation, migration, invasion and xenograft tumor growth in nude mice as well as induction of G1-phase cell cycle arrest, and vice versa. Besides, we found that GASP1 knockout obviously improved the response of breast cancer cells to paclitaxel Collectively, this study demonstrates that GASP1 enhances malignant behaviors of breast cancer cells

October 2022 Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent 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 Fluorescent probes allowed semi-quantitative receptor mapping in living cells and validated the specific expression of A2BAR in CRC cell lines.

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 However, in epithelial cells, OGR1 promotes epithelial to mesenchymal transition (EMT) and inflammation localization and alternative signaling pathways may be responsible for the differential effect of OGR1 in each cell

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis "β-Arrestins are ubiquitously expressed intracellular proteins with many functions They have participated in various cellular processes such as cell proliferation, migration, apoptosis physiological processes, these activities are also involved in the onset and progression of various cancers 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 In KISS1R overexpressing triple-negative breast cancer (TNBC) cells, stimulation has been associated lines after KP-10 (shortest active kisspeptin peptide) stimulation. We show that both cell lines express KISS1R mRNA and respond to KP-10 by elevating calcium mobilisation Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression.

September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer disease that is expected to become the second cause of cancer fatalities during the next decade. -mediated knockdown of YES1 and transfection of epitogue-tagged YAP mutants in PANC-1 and MiaPaCa-2 cancer cells, models of the aggressive squamous subtype of PDAC. and suppessed the growth of MiaPaCa-2 cells xenografted into the flank of nude mice.

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 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 Combinatorial use of AVPR1A and AVPR2 antagonists promoted apoptosis synergistically in CRPC cells.

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 metastasis, TNM stage III as well as nuclear grade G3 tumors. Transcriptome-based bioinformatics analysis revealed that GPER was linked to pro-metastatic pathways

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

The study reports that human white blood cells express an average of 160 GPCR mRNAs, ranging from 123 , suggesting a potential role in regulating red blood cell production and offering a novel avenue for Additionally, the study identified unique expression patterns of GPCRs in different immune cell types , including B cells, CD4+ T cells, CD8+ T cells, natural killer (NK) cells, and dendritic cells. also opens doors for exploring the roles of these receptors in various pathological states, including cancer

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

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.

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."

involved in a wide array of physiological and disease functions, yet knowledge of their role in colon cancer stem cell maintenance is still lacking. A truncated form of β-catenin, ∆N133β-catenin, devoid of lysine, as well as serine/threonine residues reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally involved in colon cancer

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 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an Analysis of CD4+ T cells activated under T helper (Th) 1, Th2, Th17 and regulatory T (Treg) cell differentiation FoxP3+CD25+CD127- iTreg cells. GLP-1R in human CD4+ T cells. Given the high induction of GLP-1R in human iTreg cells, we hypothesize that GLP-1R+ iTreg cells play

into studies focused on obtaining detailed molecular information in the intracellular context ("in-cell ") or those focused on characterizing molecules or events at the cell surface ("on-cell"). In this review, we outline some key NMR techniques applied for on-cell NMR studies through both solution with cell surface membrane proteins such as G-protein coupled receptors (GPCRs) and receptor tyrosine We also provide a brief survey of the applicability of on-cell NMR approaches to other classes of cell

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

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."

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

One suggested theory is that cannabinoids regulate a variety of physiological processes within the cells Murine L6 skeletal muscle cells were used in order to clarify additional possible molecular signaling Skeletal muscle cells have often been used; it is well-documented that they express cannabinoid receptors In the current work, it is demonstrated that skeletal muscle cells exhibit functional expression of CB1 Thus, in skeletal muscle cells, a possible physiological expression of CB1 receptors was identified.

September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell However, the role of β2-AR in oral cancer is not well identified. significance in relation with the clinicopathological features and overall survival of oral squamous cell

August 2022 TAS2R supports odontoblastic differentiation of human dental pulp stem cells in the inflammatory Background: Inflammatory microenvironment promotes odontoblastic differentiation in human dental pulp stem cells

Canonical chemokine receptors – scavenging “decoys” Chemokine receptors coordinate cell migration upon line, together with an increase in migration, consistent with the role of β-arrestin in receptor desensitization In line, β-Arrestin KO cells showed a major reduction in CCL14 scavenging by CCR1, in contrast with a Scavenging may allow cells to continuously migrate by remaining responsive to chemokines (S. D’Amico et. al 2000), becoming incapable of promoting cell migration, a phenomenon which is likely to

August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well As well, it has not been reported whether the effects of temperature on biosensor activity are reversible We also present a detailed protocol for monitoring cAMP levels in live cells expressing endogenous or Temperature optimization studies were carried out using HEK293H cells transiently transfected with the

October 2022 "Study of small molecule binding to live cells provides important information on the characterization Here we developed and validated a label-free, liquid chromatography-mass spectrometry (LC-MS) based cell This versatile method allows quantitative characterization of ligand binding to cell surface expressed