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GPCRs in Oncology and Immunology Minireview: functional roles of tissue kallikrein, kinins, and kallikrein-related peptidases in lung cancer.

Gαi-derived peptide binds the µ-opioid receptor. receptor Gpr111/Adgrf2 causes enamel hypomineralization in mice by alteration of the expression of kallikrein-related peptidase 4 (Klk4) during pH cycling process. Reviews, GPCRs, and more NMR applications to GPCR recognition by peptide ligands.

September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its N-terminal fragment 1 to 36 "The parathyroid hormone (PTH)-related protein (PTHrP) is indispensable

Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled Receptor Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed However, involvement of the human Mas-related G-protein coupled receptor D (MRGPRD) in the regulation

Coordinated transcriptomics and peptidomics of central nervous system identify neuropeptides and their Overall, 57 neuropeptide precursor genes were identified and 128 various mature peptides were predicted Using peptidomic analysis of CNS of G. molesta, we identified total of 28 mature peptides and precursor-related peptides from 16 precursors.

vasopressin 2 receptor "Abstract Background and purpose: Venomous animals express numerous Kunitz-type peptides The mambaquaretin-1 (MQ1) peptide identified from the Dendroaspis angusticeps venom is the most selective antagonist of the arginine-vasopressin V2 receptor (V2R) and the only unique Kunitz-type peptide active We aimed to exploit other mamba venoms to enlarge the V2R-Kunitz peptide family and gain insight into MQs were produced by solid-phase peptide synthesis and characterized in vitro by binding and functional

that removes the inhibitory GAIN domain on the extracellular side of receptor and releases a stalk peptide We further provide physiological evidence of GPR110 activation via stalk peptide.

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), which ought to facilitate neurotransmission, and improve cognition. Yet, despite this upregulation, associated physiological effects are not observed in AD patients. This paradox solicits urgent attention to find a suitable justification for disturbed neurotransmission in AD. This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate neurotransmission and AD progression." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization, mitochondria-targeting and -activating properties of human salivary histatin 1 "Human salivary histatin 1 (Hst1) exhibits a series of cell-activating properties, such as promoting cell spreading, migration, and metabolic activity. We recently have shown that fluorescently labeled Hst1 (F-Hst1) targets and activates mitochondria, presenting an important molecular mechanism. However, its regulating signaling pathways remain to be elucidated. We investigated the influence of specific inhibitors of G protein-coupled receptors (GPCR), endocytosis pathways, extracellular signal-regulated kinases 1/2 (ERK1/2) signaling, p38 signaling, mitochondrial respiration and Na+/K+-ATPase activity on the uptake, mitochondria-targeting and -activating properties of F-Hst1. We performed a siRNA knockdown (KD) to assess the effect of Sigma-2 receptor (S2R) /Transmembrane Protein 97 (TMEM97)—a recently identified target protein of Hst1. We also adopted live cell imaging to monitor the whole intracellular trafficking process of F-Hst1. Our results showed that the inhibition of cellular respiration hindered the internalization of F-Hst1. The inhibitors of GPCR, ERK1/2, phagocytosis, and clathrin-mediated endocytosis (CME) as well as siRNA KD of S2R/TMEM97 significantly reduced the uptake, which was accompanied by the nullification of the promoting effect of F-Hst1 on cell metabolic activity. Only the inhibitor of CME and KD of S2R/TMEM97 significantly compromised the mitochondria-targeting of Hst1. We further showed the intracellular trafficking and targeting process of F-Hst1, in which early endosome plays an important role. Overall, phagocytosis, CME, GPCR, ERK signaling, and S2R/TMEM97 are involved in the internalization of Hst1, while only CME and S2R/TMEM97 are critical for its subcellular targeting. The inhibition of either internalization or mitochondria-targeting of Hst1 could significantly compromise its mitochondria-activating property." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS increase in SRE-luc activity was noticed when COS-7 cells expressing GnIHR were challenged with both GnIH peptides However, GnIH peptides did not alter NFAT-RE-luc activity and ERK phosphorylation levels. Our results provide additional evidence for the understanding of signaling pathways activated by GnIH peptides

November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in high-resolution techniques to investigate peptidergic transmission and expression throughout the brain in model systems. Neuropeptides exhibit distinct characteristics which includes their post-translational processing, release from dense core vesicles, and ability to activate G-protein-coupled receptors (GPCRs). These complex properties have driven the need for development of specialized tools that can sense neuropeptide expression, cell activity, and release. Current research has focused on isolating when and how neuropeptide transmission occurs, as well as the conditions in which neuropeptides directly mediate physiological and adaptive behavioral states. Here we describe the current technological landscape in which the field is operating to decode key questions regarding these dynamic neuromodulators." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

Here, we discovered that the epithelial-cell-derived antimicrobial peptides defensins activated orphan

cell-induced inflammation "Gut intraepithelial lymphocytes (IELs) are thought to calibrate glucagon-like peptide

apoptosis in colorectal cancer through disrupting TRAF6-TAB2-TAK1-JNK/p38 MAPK signaling Metallo-protease Peptidase induces ROS-dependent apoptosis in ovarian cancer cells by targeting PAR-1 G protein-coupled receptors related anti-multiple myeloma antibody to the human GPRC5D homodimer Identification of a G-protein coupled receptor-related Structural and Molecular Insights into GPCR Function Structure and dynamics of the pyroglutamylated RF-amide peptide

G protein-coupled receptors (GPCRs) are membrane-bound proteins that sense external stimuli and relay developing therapeutic agents that target specific receptor dimer states to modulate signaling in diseases related Graaf, C., et al., Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March Harikumar, K.G., et al., Glucagon-like peptide-1 receptor dimerization differentially regulates agonist Schelshorn, D., et al., Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1

Previous findings suggest that parallel pathways independently relay innate threat signals from different Here, we report that neurons expressing calcitonin gene-related peptide (CGRP) in the parvocellular subparafascicular parabrachial nucleus in the brainstem respond to multi-sensory threat cues from various sensory modalities and relay innate threat pathways may provide insights into developing therapeutic candidates for innate fear-related

By comparison, we found that the Releasing Hormone-Related Peptides (GnRHs) system of Sternorrhyncha Independent secondary losses of the adipokinetic hormone/corazonin-related peptide receptor (ACP) and

, Antoinette MaassenVanDenBrink, et al. for their work on Intracellular pathways of calcitonin gene-related peptide-induced relaxation of human coronary arteries: A key role for Gβγ subunit instead of cAMP. receptor 1 is discarded by exosomes after internalization Intracellular pathways of calcitonin gene-related peptide-induced relaxation of human coronary arteries: A key role for Gβγ subunit instead of cAMP GPCR dynamics using single-molecule fluorescence Droplet-based microfluidic platform for detecting agonistic peptides

October 2022 "Endogenous parathyroid hormone (PTH) and PTH-related peptide (PTHrP) bind to the parathyroid

for their study on G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related Cellular Respiration G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related approach GRN knockdown regulates the expression and alternative splicing of genes associated with aphasia-related protein-coupled receptor helix 8 solution structure and orientation using a neurotensin receptor 1 peptide Positive Topline Data from its Phase 2a Obesity Study and Capsule to Tablet PK Study for its Oral Non-Peptide

region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination of closely related including yeasts, mating between cells of opposite mating type depends on the molecular recognition of two peptidyl First, we switched GPCRs between S. pombe and the closely related species Schizosaccharomyces octosporus amino acid residues of Map3, F214 and F215, are key residues important for discrimination of closely related

September 2022 "Endogenous parathyroid hormone (PTH) and PTH-related peptide (PTHrP) bind to the parathyroid

injury in mice by inhibiting endoplasmic reticulum stress Two C-terminal isoforms of Aplysia tachykinin-related peptide receptors exhibit phosphorylation-dependent and independent desensitization mechanisms Get ready Ixodes scapularis has five different GPCRs specifically activated by ACP (adipokinetic hormone/corazonin-related peptide) GPCRs in Oncology and Immunology S1P Signaling Genes as Prominent Drivers of BCR-ABL1-Independent

the loss of fruiting body formation in the social amoeba Dictyostelium discoideum evolved under low relatedness

GPCR Binders, Drugs, and more Cytotoxicity-related effects of imidazolium and chlorinated bispyridinium GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer Scientist, Drug Metabolism and Pharmacokinetics PhD Opportunity - Investigation Of The Role Of The Formyl Peptide

C5a is established to interact with a set of genomically related transmembrane receptors, like C5aR1 highly refined model structures of C5aR2, respectively in free (inactive), complexed to C-terminal peptide