Prostaglandin (PG) signaling regulates a wide variety of physiological and pathological processes, including Prostaglandin E2 (PGE2) and its receptor EP4 modulate ciliogenesis by increasing the anterograde intraflagellar Many G-protein-coupled receptors (GPCRs) including EP4 are localized in cilia for modulating cAMP signaling

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer."

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 Last, in the pocket, ligand–receptor attractive native contacts are formed.

Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial Infarction by Activating levels of TGF-1β and Wnt1 or Akt activation. and activating β-arrestin-2, PP2A, and GSK3β. Exendin-4, and possibly through G protein-coupled receptors (GPCRs), increases levels of cAMP and upregulates ), thus reduces fibrosis and prevents the activation of β-catenin and collagen deposition.

collection of new pain-relieving compounds that, like morphine and other drugs, provide relief via activation of opioid receptors, but without inducing many dangerous and unwanted side-effects that have driven

patients is involved in leukocyte chemotaxis to the synovium "The rheumatoid arthritis (RA) inflammatory process GPR15 is a G protein-coupled receptor (GPCR) located on chromosome 3 and has similarity in its sequence with chemokine receptors.

30, 2021 -- Orion Biotechnology, a clinical stage company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs) with a novel drug modality, proven discovery platform and best-in-class molecules, OB-004 is a GPCR targeted protein analog of CCL2 that targets the CCR2 receptor.

We demonstrate that the chemoreceptor genes, srg-36 and srg-37, which encode G protein-coupled receptors However, it remains unclear what signals activate the EGL-30 pathway in axon regeneration. Here, we show that SRG-36 and SRG-37 act as upstream GPCRs that activate EGL-30. Consistent with this, we found that ascr#5 activates the axon regeneration pathway via SRG-36/SRG-37 Thus, ascaroside signaling promotes axon regeneration by activating the GPCR-Gqα pathway.

Current progress in our knowledge of the itch processing, the numerous mediators and receptors involved Currently, inhibitors of IL-31, IL-4/13, NK1 receptors, opioids and cannabinoids, JAK, PDE4 or TRP are

G protein-coupled receptor 3 (GPR3) belongs to the class A rhodopsin-type GPCR family and is highly expressed GPR3 is unique in its ability to constitutively activate the Gαs protein without a ligand, which elevates

authorization for the Company’s TAVNEOS (avacopan), an orally administered selective complement 5a receptor a rituximab or cyclophosphamide regimen, indicated for the treatment of adult patients with severe, active

, Belgium – March 10, 2022 – Confo Therapeutics, a leader in the discovery of medicines targeting G-protein coupled receptors (GPCRs), today announced that the first subjects have been dosed in the company’s first-in-human trial of their clinical candidate CFTX-1554, a novel inhibitor of the angiotensin II type 2 receptor

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD),

remains unknown, and there is no ideal drug for the specific treatment of pSS. β-arrestin2 is a key protein that mediates desensitization and internalization of G protein-coupled receptors (GPCRs) and it participates First, excessive activation of β-arrestin2 and GRP78-ATF6-CHOP apoptosis signaling were detected in specimens IFNα to stimulate human salivary gland epithelial cells (HSGECs), and the results showed that IFNα activated In summary, our results suggest that excessive activation of GRP78-ATF6-CHOP apoptosis signaling is involved

The drugs also target relatively low-hanging fruit: like cytokines or tyrosine kinase receptors. To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better

August 2022 "The common mechanisms by which members of the G protein-coupled receptor (GPCR) family respond

Taking advantage of a striking deficit of both NPS receptor (NPSR1) and NPS precursor knockout mice in Overall, these results demonstrate that stimulus salience encoding is critically associated with NPS activity

libraries and sophisticated bioinformatics expertise with Sosei Heptares’ world-leading StaR® (stabilized receptor silicon platform, announced a strategic collaboration to discover therapeutic antibodies against G protein-coupled receptors (GPCR) identified by Sosei Heptares."

June 2022 "G protein-coupled receptors (GPCRs) represent a major therapeutic target class as they play a key role in many (patho-) physiological processes. GPCRs respond to a wide variety of signals that range in size from photons to proteins (Foord et al.,

It is generally considered that TNBC is an estrogen-independent breast cancer, while a new estrogen receptor , namely G protein-coupled estrogen receptor (GPER), is demonstrated to mediate estrogenic actions in

) and Université de Montréal (Québec, Canada; “UdM”), to discover novel small molecules targeting G-Protein Coupled Receptors (GPCRs) in a metabolic disease area."

The grant should help expand Confo Therapeutic’s research on G protein-coupled receptor (GPCR) drug candidates

me great pleasure to announce the fourth hybrid symposium on regulatory autoantibodies targeting G-protein-coupled receptors (GPCRs) in Lübeck. GPCRs are involved in a variety of physiological and pathophysiological processes.

pre-clinical stage biotechnology company transforming the discovery of novel GPCR-targeted therapies (G-Protein Coupled Receptors), today announced the promotion of Senior Vice President, Head of Research, Peter

September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the

behavior of salivary adenoid cystic carcinoma via the PI3K/AKT signaling pathway "Background CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand CCL25 to promote

September 2022 "The Smoothened receptor (SMO, a 7 pass transmembrane domain, Class F GPCR family protein In the absence of HH signaling, SMO is inhibited by Patched 1 (PTC1; a 12 pass transmembrane domain protein cilia, thus making way for SMO to localize in the primary cilia, as an essential prerequisite for its activation

January 2022 "G-protein-coupled receptors’ star has been on the rise in biotech in recent years as researchers