Genomes and Genes
Gene Symbol: SSTR1
Description: somatostatin receptor 1
Alias: SRIF-2, SS-1-R, SS1-R, SS1R, somatostatin receptor type 1
Publications161 found, 100 shown here
- Prud homme G, Glinka Y, Wang Q. Immunological GABAergic interactions and therapeutic applications in autoimmune diseases. Autoimmun Rev. 2015;14:1048-56 pubmed publisher..However, the immune effects of GABAergic drugs in patients are not well documented. GABAergic immunobiology is a recent area of research, which shows potential for the development of new therapies for autoimmune diseases. ..
- Connor E, Evock Clover C, Walker M, Elsasser T, Kahl S. COMPARATIVE GUT PHYSIOLOGY SYMPOSIUM: Comparative physiology of glucagon-like peptide-2: Implications and applications for production and health of ruminants. J Anim Sci. 2015;93:492-501 pubmed publisher..g., through specific feed additives), which are more likely to achieve consumer acceptance, are needed. Opportunities to address these challenges are discussed. ..
- Takenoya F, Wang L, Kageyama H, Hirako S, Wada N, Hashimoto H, et al. Neuropeptide W-Induced Hypophagia is Mediated Through Corticotropin-Releasing Hormone-Containing Neurons. J Mol Neurosci. 2015;56:789-98 pubmed publisher..While NPW administration decreased feeding activity, the CRH antagonist inhibited this effect. These results strongly suggest that NPW regulates feeding behavior through CRH neurons in the mouse brain. ..
- Polhemus D, Gao J, Scarborough A, Trivedi R, McDonough K, Goodchild T, et al. Radiofrequency Renal Denervation Protects the Ischemic Heart via Inhibition of GRK2 and Increased Nitric Oxide Signaling. Circ Res. 2016;119:470-80 pubmed publisher..These findings provide new insights into the remote cardioprotective effects of RF-RDN acting directly on cardiac myocytes to attenuate cell death and protect against ischemic injury. ..
- Wang S, Bao Z, Liang Q, Long J, Xiao Z, Jiang Z, et al. Octreotide stimulates somatostatin receptor-induced apoptosis of SW480 colon cancer cells by activation of glycogen synthase kinase-3?, A Wnt/?-catenin pathway modulator. Hepatogastroenterology. 2013;60:1639-46 pubmed..Cell apoptosis of SW480 cells was measured by apoptosis-DNA ladder assay. SSTR1, SSTR2, SSTR3, SSTR4, and SSTR5 mRNA expression levels were confirmed by RT-PCR; ?-catenin, TCF-4, cyclin D1, c-..
- Ambrożewicz E, Wojcik P, Wroński A, Łuczaj W, Jastrząb A, Zarkovic N, et al. Pathophysiological Alterations of Redox Signaling and Endocannabinoid System in Granulocytes and Plasma of Psoriatic Patients. Cells. 2018;7: pubmed publisher..In addition, increased expression of CB1 receptors leads to increased oxidative stress, lipid modifications, and inflammation, which, in turn, may promote the progression of psoriasis into the advanced, arthritic form of the disease. ..
- Kucharava K, Sekulic Jablanovic M, Horvath L, Bodmer D, Petkovic V. Pasireotide protects mammalian cochlear hair cells from gentamicin ototoxicity by activating the PI3K-Akt pathway. Cell Death Dis. 2019;10:110 pubmed publisher..somatostatin and its selective analogs have provided neuroprotection by activating five somatostatin receptor (SSTR1-SSTR5) subtypes...
- Seemann S, Lupp A. Administration of AMD3100 in endotoxemia is associated with pro-inflammatory, pro-oxidative, and pro-apoptotic effects in vivo. J Biomed Sci. 2016;23:68 pubmed
- Sutton B, Palmer N, Langefeld C, Xue B, Proctor A, Ziegler J, et al. Association of SSTR2 polymorphisms and glucose homeostasis phenotypes: the Insulin Resistance Atherosclerosis Family Study. Diabetes. 2009;58:1457-62 pubmed publisher..CONCLUSIONS We observed evidence for association of SSTR2 polymorphisms with measures of glucose homeostasis. Thus, variants in SSTR2 may influence pathways of S(I)to modulate glucose homeostasis. ..
- Koyama H, Iwakura H, Dote K, Bando M, Hosoda H, Ariyasu H, et al. Comprehensive Profiling of GPCR Expression in Ghrelin-Producing Cells. Endocrinology. 2016;157:692-704 pubmed publisher..These results will lead to a greater understanding of the physiology of ghrelin and facilitate the development of ghrelin-modulating drugs. ..
- Raffetto J, Qiao X, Beauregard K, Khalil R. Estrogen receptor-mediated enhancement of venous relaxation in female rat: implications in sex-related differences in varicose veins. J Vasc Surg. 2010;51:972-81 pubmed publisher..The decreased venous contraction and enhanced E2/ER-mediated venous relaxation would lead to more distensible veins in female rats. ..
- Chow E, Quach H, Zhang Y, Wang J, Evans D, Li A, et al. Disrupted Murine Gut-to-Human Liver Signaling Alters Bile Acid Homeostasis in Humanized Mouse Liver Models. J Pharmacol Exp Ther. 2017;360:174-191 pubmed
- Tolkach Y, Merseburger A, Herrmann T, Kuczyk M, Serth J, Imkamp F. Signatures of Adverse Pathological Features, Androgen Insensitivity and Metastatic Potential in Prostate Cancer. Anticancer Res. 2015;35:5443-51 pubmed..surface associated (MUC1), MYC binding protein 2, E3 ubiquitin protein ligase (MYCBP2), somatostatin receptor 1 (SSTR1), topoisomerase (DNA) II alpha 170 kDa (TOP2A) and exportin 6 (XPO6)...
- Beneyto M, Morris H, Rovensky K, Lewis D. Lamina- and cell-specific alterations in cortical somatostatin receptor 2 mRNA expression in schizophrenia. Neuropharmacology. 2012;62:1598-605 pubmed publisher..Thus, we used in situ hybridization to quantify the mRNA expression levels of SST receptors subtype 1 (SSTR1) and subtype 2 (SSTR2) in DLPFC area 9 from 23 matched pairs of subjects with schizophrenia and normal comparison ..
- Adori C, Glück L, Barde S, Yoshitake T, Kovacs G, Mulder J, et al. Critical role of somatostatin receptor 2 in the vulnerability of the central noradrenergic system: new aspects on Alzheimer's disease. Acta Neuropathol. 2015;129:541-63 pubmed publisher..We modeled these pathogenic changes in Sstr2(-/-) mice and, unlike in Sstr1(-/-) or Sstr4(-/-) genotypes, they showed selective, global and progressive degeneration of their central ..
- Husain B, Nanavaty I, Marathe S, Rajendran R, Vaidya V. Hippocampal transcriptional and neurogenic changes evoked by combination yohimbine and imipramine treatment. Prog Neuropsychopharmacol Biol Psychiatry. 2015;61:1-9 pubmed publisher..expression of the Î±2A-adrenoceptor (Adra2a), serotonin 5HT2C receptor (Htr2c) and the somatostatin receptor 1 (Sstr1), which modulate antidepressant action...
- Hanafi N, Mohamed A, Sheikh Abdul Kadir S, Othman M. Overview of Bile Acids Signaling and Perspective on the Signal of Ursodeoxycholic Acid, the Most Hydrophilic Bile Acid, in the Heart. Biomolecules. 2018;8: pubmed publisher..This review provides an overview of BA signaling, with the main emphasis on past and present perspectives on UDCA signals in the heart. ..
- Fatima A, Waters S, O Boyle P, Seoighe C, Morris D. Alterations in hepatic miRNA expression during negative energy balance in postpartum dairy cattle. BMC Genomics. 2014;15:28 pubmed publisher..This study highlights the potential role of miRNAs in transcription regulation of hepatic gene expression during SNEB in dairy cattle. ..
- KÃ¤chele M, Hennige A, Machann J, Hieronimus A, Lamprinou A, Machicao F, et al. Variation in the Phosphoinositide 3-Kinase Gamma Gene Affects Plasma HDL-Cholesterol without Modification of Metabolic or Inflammatory Markers. PLoS ONE. 2015;10:e0144494 pubmed publisher..Even though the molecular pathways connecting PI3KÎ³ and HDL metabolism remain to be further elucidated, this finding could add a novel aspect to the pathophysiological role of PI3KÎ³ in atherogenesis. ..
- Mittal S, Khole S, Jagadish N, Ghosh D, Gadgil V, Sinkar V, et al. Andrographolide protects liver cells from H2O2 induced cell death by upregulation of Nrf-2/HO-1 mediated via adenosine A2a receptor signalling. Biochim Biophys Acta. 2016;1860:2377-2390 pubmed publisher..We speculate that andrographolide can be used as a therapeutic drug to combat oxidative stress implicated in pathogenesis of various diseases such as diabetes, osteoporosis, neurodegenerative diseases etc. ..
- Dalmo J, Spetz J, Montelius M, Langen B, Arvidsson Y, Johansson H, et al. Priming increases the anti-tumor effect and therapeutic window of 177Lu-octreotate in nude mice bearing human small intestine neuroendocrine tumor GOT1. EJNMMI Res. 2017;7:6 pubmed publisher..In vitro studies have shown that irradiation can up-regulate the expression of SSTR1, 2 and 5, and increase 177Lu-octreotate uptake...
- Strack J, Heni H, Gilsbach R, Hein L, Aktories K, Orth J. Noncanonical G-protein-dependent modulation of osteoclast differentiation and bone resorption mediated by Pasteurella multocida toxin. MBio. 2014;5:e02190 pubmed publisher..In particular, modulation of G protein-coupled receptor activity in osteoclast progenitors by small molecules might be of specific interest. ..
- Parker B, Wertz S, Pollard C, Desimine V, Maning J, McCrink K, et al. Novel Insights into the Crosstalk between Mineralocorticoid Receptor and G Protein-Coupled Receptors in Heart Adverse Remodeling and Disease. Int J Mol Sci. 2018;19: pubmed publisher..Novel findings revealing non-conventional roles of GPCR signaling molecules, specifically of GPCR-kinase (GRK)-5, in cardiac MR regulation are also highlighted. ..
- Ruggeri R, Ferrau F, Campenni A, Simone A, Barresi V, Giuffre G, et al. Immunohistochemical localization and functional characterization of somatostatin receptor subtypes in a corticotropin releasing hormone- secreting adrenal phaeochromocytoma: review of the literature and report of a case. Eur J Histochem. 2009;53:1-6 pubmed..Immunostaining for SSTR subtypes showed a positive reaction for SSTR1, SSTR2A, SSTR2B, antisera on tumour cells...
- Howick K, Wallace Fitzsimons S, Kandil D, Chruscicka B, Caliş M, Murphy E, et al. A Dairy-Derived Ghrelinergic Hydrolysate Modulates Food Intake In Vivo. Int J Mol Sci. 2018;19: pubmed publisher..Further mechanistic studies are required in order to confirm efficacy as a ghrelinergic bioactive in susceptible population groups. ..
- Zhu F, Ji X, Zhong X, Hu H, Liang L, Chen J, et al. [Effects of mild hypothermia on β-adrenergic signaling pathway in a cardiac arrest swine model]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2018;30:134-139 pubmed publisher..45±0.05 vs. 0.80±0.08, P < 0.05). Mild hypothermia can reduce the degree of cardiac function injury after CPR, and its mechanism may be related to the reduction of impaired myocardial β-AR signaling after CPR. ..
- Szolcsanyi J, Pinter E, Helyes Z, Petho G. Inhibition of the function of TRPV1-expressing nociceptive sensory neurons by somatostatin 4 receptor agonism: mechanism and therapeutical implications. Curr Top Med Chem. 2011;11:2253-63 pubmed..for this function, experiments were focused on actions of sstR4 receptor agonists as this subtype, similarly to sstR1, is not involved in endocrine regulation...
- Mata K, Li W, Reslan O, Siddiqui W, Opsasnick L, Khalil R. Adaptive increases in expression and vasodilator activity of estrogen receptor subtypes in a blood vessel-specific pattern during pregnancy. Am J Physiol Heart Circ Physiol. 2015;309:H1679-96 pubmed publisher..GPER may contribute to aortic relaxation while enhanced ER? expression could mediate other genomic vascular effects during pregnancy. ..
- Charron M, Vuguin P. Lack of glucagon receptor signaling and its implications beyond glucose homeostasis. J Endocrinol. 2015;224:R123-30 pubmed publisher..These findings suggest that glucagon signaling plays an important role in multiple organs. Thus, treatment options designed to block Gcgr activation in diabetics may have implications beyond glucose homeostasis. ..
- De Buck M, Berghmans N, PÃ¶rtner N, Vanbrabant L, Cockx M, Struyf S, et al. Serum amyloid A1Î± induces paracrine IL-8/CXCL8 via TLR2 and directly synergizes with this chemokine via CXCR2 and formyl peptide receptor 2 to recruit neutrophils. J Leukoc Biol. 2015;98:1049-60 pubmed publisher..g., lipopolysaccharide) inflammatory mediators induce primary chemoattractants such as serum amyloid A that synergize in an autocrine (monocyte) or a paracrine (neutrophil) fashion with secondary chemokines induced in stromal cells. ..
- Liu H, Pathak P, Boehme S, Chiang J. Cholesterol 7?-hydroxylase protects the liver from inflammation and fibrosis by maintaining cholesterol homeostasis. J Lipid Res. 2016;57:1831-1844 pubmed..Maintaining bile acid and cholesterol homeostasis is important for protecting against liver injury and nonalcoholic fatty liver disease. ..
- Sizdahkhani S, Feldman M, Piazza M, Ksendzovsky A, Edwards N, Ray Chaudhury A, et al. Somatostatin receptor expression on von Hippel-Lindau-associated hemangioblastomas offers novel therapeutic target. Sci Rep. 2017;7:40822 pubmed publisher..We explored this possibility by demonstrating consistent histologic expression of SSTR1, 2a, 4, and 5 in VHL-HBs...
- De Toni L, Di Nisio A, Speltra E, Rocca M, Ghezzi M, Zuccarello D, et al. Polymorphism rs2274911 of GPRC6A as a Novel Risk Factor for Testis Failure. J Clin Endocrinol Metab. 2016;101:953-61 pubmed publisher..Our results suggest that GPRC6A inactivation or sub-function contributes to reduced exposure to androgens, leading to cryptorchidism during fetal life and/or low sperm production in adulthood. ..
- Guo D, Pan A, Dror R, Mocking T, Liu R, Heitman L, et al. Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor. Mol Pharmacol. 2016;89:485-91 pubmed publisher..Our results also suggest that ZM241385 follows a multistep dissociation pathway, consecutively interacting with distinct receptor regions, a mechanism that may also be common to many other GPCRs. ..
- Murza A, Sainsily X, CÃ´tÃ© J, Bruneau Cossette L, Besserer Offroy Ã, LongprÃ© J, et al. Structure-activity relationship of novel macrocyclic biased apelin receptor agonists. Org Biomol Chem. 2017;15:449-458 pubmed publisher..These macrocyclic compounds represent very useful pharmacological tools to explore the therapeutic potential of the apelinergic system. ..
- Marcinak J, Vakilynejad M, Kogame A, Tagawa Y. Evaluation of the Pharmacokinetics and Safety of a Single Oral Dose of Fasiglifam in Subjects with Mild or Moderate Hepatic Impairment. Drugs R D. 2018;18:109-118 pubmed publisher..Hepatic status did not significantly impact systemic exposure of fasiglifam in this study, in fact, a decrease was observed, suggesting no dose reduction would be required for patients with hepatic impairment. ..
- Masyuk T, Masyuk A, Larusso N. TGR5 in the Cholangiociliopathies. Dig Dis. 2015;33:420-5 pubmed publisher..Collectively, these data suggest the involvement of TGR5 in PLD and that TGR5 targeting in cystic cholangiocytes may have therapeutic potential. ..
- Ahlers K, Chakravarti B, Fisher R. RGS6 as a Novel Therapeutic Target in CNS Diseases and Cancer. AAPS J. 2016;18:560-72 pubmed publisher..Together, these findings demonstrate the critical role of RGS6 in regulating both G protein-dependent CNS pathology and G protein-independent cancer pathology implicating RGS6 as a novel therapeutic target. ..
- Herr D, Reolo M, Peh Y, Wang W, Lee C, Rivera R, et al. Sphingosine 1-phosphate receptor 2 (S1P2) attenuates reactive oxygen species formation and inhibits cell death: implications for otoprotective therapy. Sci Rep. 2016;6:24541 pubmed publisher..Cumulatively, these results suggest that S1P2 may serve as a therapeutic target for attenuating cisplatin-mediated ototoxicity. ..
- Traylor Knowles N, Rose N, Palumbi S. The cell specificity of gene expression in the response to heat stress in corals. J Exp Biol. 2017;220:1837-1845 pubmed publisher..Joint information about expression patterns in response to heat and cell specificity will allow greater dissection of the regulatory pathways and specific cell reactions that lead to coral bleaching. ..
- Desplantes R, Leveque C, Müller B, Lotierzo M, Ferracci G, Popoff M, et al. Affinity biosensors using recombinant native membrane proteins displayed on exosomes: application to botulinum neurotoxin B receptor. Sci Rep. 2017;7:1032 pubmed publisher..Engineered exosomes provide thus a novel means to study membrane proteins for biotechnology and clinical applications. ..
- Wang Y, Jin L, Song Y, Zhang M, Shan D, Liu Y, et al. ?-arrestin 2 mediates cardiac ischemia-reperfusion injury via inhibiting GPCR-independent cell survival signalling. Cardiovasc Res. 2017;113:1615-1626 pubmed publisher..We define an upregulation of Arrb2 as a pathogenic factor in cardiac I/R injury, and also reveal a novel GPCR-independent mechanism of Arrb2-mediated cell death signalling in the heart. ..
- Abd Alla J, Graemer M, Fu X, Quitterer U. Inhibition of G-protein-coupled Receptor Kinase 2 Prevents the Dysfunctional Cardiac Substrate Metabolism in Fatty Acid Synthase Transgenic Mice. J Biol Chem. 2016;291:2583-600 pubmed publisher..Thus, GRK2 inhibition is a novel approach that targets the dysfunctional substrate metabolism of the failing heart. ..
- Trivellin G, Correa R, Batsis M, Faucz F, Chittiboina P, Bjelobaba I, et al. Screening for GPR101 defects in pediatric pituitary corticotropinomas. Endocr Relat Cancer. 2016;23:357-365 pubmed..A rare germline GPR101 variant was found in one patient with CD but in vitro studies did not support a consistent pathogenic effect. GPR101 is unlikely to be involved in the pathogenesis of CD. ..
- Thompson A, Stephens J, Bain S, Kanamarlapudi V. Molecular Characterisation of Small Molecule Agonists Effect on the Human Glucagon Like Peptide-1 Receptor Internalisation. PLoS ONE. 2016;11:e0154229 pubmed publisher..This study illustrates pharmacology of differential activation of GLP-1R by GLP-1 and compounds 2 and B. ..
- Chen Z, Wu D, Li L, Chen L. Apelin/APJ System: A Novel Therapeutic Target for Myocardial Ischemia/Reperfusion Injury. DNA Cell Biol. 2016;35:766-775 pubmed..In this review, we discuss how the mechanisms of the apelin/APJ system reverse MIRI in detail and elaborate on APJ agonists, which may be used for therapy of MIRI. ..
- Minsel I, Mentlein R, Sel S, Diebold Y, Bräuer L, Muhlbauer E, et al. Somatostatin actions via somatostatin receptors on the ocular surface are modulated by inflammatory processes. Endocrinology. 2009;150:2254-63 pubmed publisher..surface and in the lacrimal apparatus, we investigated the distribution pattern of SS and its receptors 1-5 (SSTR1-5) by means of RT-PCR, real-time RT-PCR, Western blot and immunodot blot analysis as well as immunohistochemistry ..
- Nakayama Y, Wada R, Yajima N, Hakamada K, Yagihashi S. Profiling of somatostatin receptor subtype expression by quantitative PCR and correlation with clinicopathological features in pancreatic endocrine tumors. Pancreas. 2010;39:1147-54 pubmed publisher..The hormones and MIB1 index were examined using immunohistochemical techniques. The mRNA levels of SSTR1, SSTR2, SSTR3, and SSTR5 were high in PET compared with AC, whereas the expression of SSTR4 was low in PET and AC...
- Gao B, Huang Q, Jie Q, Lu W, Wang L, Li X, et al. GPR120: A bi-potential mediator to modulate the osteogenic and adipogenic differentiation of BMMSCs. Sci Rep. 2015;5:14080 pubmed publisher..These findings provide new hope for developing novel remedies to treat osteoporosis by adjusting the GPR120-mediated differentiation balance of BMMSCs. ..
- Gautam A, Wang C, Zeng J, Wang J, Lu J, Wei J, et al. Expression and clinical significance of SALL4 and LGR5 in patients with lung cancer. Oncol Lett. 2015;10:3629-3634 pubmed..By contrast, LGR5 demonstrated 97% sensitivity, but the specificity was poor. Therefore, SALL4 may be an extremely useful diagnostic marker for lung cancer, but LGR5 is not as useful. ..
- LeBlanc M, Lehmann R. Domain-specific control of germ cell polarity and migration by multifunction Tre1 GPCR. J Cell Biol. 2017;216:2945-2958 pubmed publisher..We propose that this bifurcation of the Tre1 G protein-coupled receptor signaling response via G protein-dependent and independent branches enables distinct spatiotemporal regulation of germ cell migration. ..
- Chen G, Fu S, Feng W, Huang B, Xu S, Wang W, et al. AMP010014A09 in Sus Scrofa Encodes an Analog of G Protein-Coupled Receptor 109A, Which Mediates the Anti-Inflammatory Effects of Beta-Hydroxybutyric Acid. Cell Physiol Biochem. 2017;42:1420-1430 pubmed publisher..Our results indicated that AMP+ encodes a G protein-coupled receptor in Sus scrofa that inhibits cAMP levels and mediates anti-inflammatory effects in swine monocytes. ..
- Fasciani A, Quilici P, Biscaldi E, Flamini M, Fioravanti A, Orlandi P, et al. Overexpression and functional relevance of somatostatin receptor-1, -2, and -5 in endometrium and endometriotic lesions. J Clin Endocrinol Metab. 2010;95:5315-9 pubmed publisher..Thus, the use of these receptors may provide new strategies for the diagnosis and treatment of endometriosis. ..
- Li S, Yang C, Zhang L, Gao X, Wang X, Liu W, et al. Promoting axon regeneration in the adult CNS by modulation of the melanopsin/GPCR signaling. Proc Natl Acad Sci U S A. 2016;113:1937-42 pubmed publisher..Thus, our results provide a strategy to promote axon regeneration after CNS injury by modulating neuronal activity through GPCR signaling. ..
- Kamp M, Shim R, Nicholls A, Oliveira A, Mason L, Binge L, et al. G Protein-Coupled Receptor 43 Modulates Neutrophil Recruitment during Acute Inflammation. PLoS ONE. 2016;11:e0163750 pubmed publisher..Therefore, GPR43 and a microbiota composition that allows for SCFA production function to modulate neutrophil recruitment during inflammatory responses. ..
- Piekielna Ciesielska J, Ferrari F, Calo G, Janecka A. Cyclopeptide Dmt-[D-Lys-p-CF3-Phe-Phe-Asp]NH2, a novel G protein-biased agonist of the mu opioid receptor. Peptides. 2018;101:227-233 pubmed publisher..Such biased ligands are able to separate the biological actions of an activated receptor and have the potential to become more effective drug candidates with fewer side effects. ..
- Ahmed M, Bychkov E, Li L, Gurevich V, Gurevich E. GRK3 suppresses L-DOPA-induced dyskinesia in the rat model of Parkinson's disease via its RGS homology domain. Sci Rep. 2015;5:10920 pubmed publisher..RH-dead mutant was ineffective, whereas GRK3 knockdown exacerbated âˆ†FosB accumulation. Our findings reveal a novel mechanism of GRK3 control of the dopamine receptor signaling and the role of Gq in LID. ..
- Friis K, Iturrioz X, Thomsen J, Alvear Perez R, Bahrami S, Llorens Cortes C, et al. Directed Molecular Evolution of an Engineered Gammaretroviral Envelope Protein with Dual Receptor Use Shows Stable Maintenance of Both Receptor Specificities. J Virol. 2016;90:1647-56 pubmed publisher..We provide indirect evidence that such reduced affinity leads to reduced receptor internalization and propose a novel model in which too rapid receptor internalization may decrease virus entry. ..
- Altara R, Manca M, BrandÃ£o R, Zeidan A, Booz G, Zouein F. Emerging importance of chemokine receptor CXCR3 and its ligands in cardiovascular diseases. Clin Sci (Lond). 2016;130:463-78 pubmed publisher..In this review, we provide evidence to support our contention that CXCR3 and its ligands actively participate in the development and progression of CVDs, and may additionally have utility as diagnostic and prognostic biomarkers. ..
- Ou Z, Sun Y, Lin L, You N, Liu X, Li H, et al. Olig2-Targeted G-Protein-Coupled Receptor Gpr17 Regulates Oligodendrocyte Survival in Response to Lysolecithin-Induced Demyelination. J Neurosci. 2016;36:10560-10573 pubmed..Pharmacological inhibition of Gpr17 promoted remyelination, highlighting the potential for Gpr17-targeted therapeutic approaches in demyelination diseases. ..
- Saloman J, Scheff N, Snyder L, Ross S, Davis B, Gold M. Gi-DREADD Expression in Peripheral Nerves Produces Ligand-Dependent Analgesia, as well as Ligand-Independent Functional Changes in Sensory Neurons. J Neurosci. 2016;36:10769-10781 pubmed..These findings highlight both the potential and the limitations of this exciting technology as well as the necessity to identify the mechanisms underlying any observed phenotype. ..
- Almquist J, Hovdal D, Ahlström C, Fjellström O, Gennemark P, Sundqvist M. Overexpressing cell systems are a competitive option to primary adipocytes when predicting in vivo potency of dual GPR81/GPR109A agonists. Eur J Pharm Sci. 2018;114:155-165 pubmed publisher..This work suggests that data from the overexpressing cell systems are sufficient to predict in vivo potency of GPR81/GPR109A agonists, an approach contributing to faster and leaner drug discovery. ..
- Gaidarov I, ANTHONY T, Gatlin J, Chen X, Mills D, Solomon M, et al. Embelin and its derivatives unravel the signaling, proinflammatory and antiatherogenic properties of GPR84 receptor. Pharmacol Res. 2018;131:185-198 pubmed publisher..These data suggest that GPR84 may be a target of therapeutic value and that distinct modes of receptor modulation (inhibition vs. stimulation) may be required for inflammatory and atherosclerotic indications. ..
- Li Y. GRK6 expression in patients with hepatocellular carcinoma. Asian Pac J Trop Med. 2013;6:220-3 pubmed publisher..Our results suggested that GRK6 overexpression plays an important role in HCC. Monitoring the expression of GRK6 maybe helpful in early diagnosis and prognosis of HCC. ..
- Le Duigou C, Savary E, Kullmann D, Miles R. Induction of Anti-Hebbian LTP in CA1 Stratum Oriens Interneurons: Interactions between Group I Metabotropic Glutamate Receptors and M1 Muscarinic Receptors. J Neurosci. 2015;35:13542-54 pubmed publisher..Changes in EPSP amplitude distributions in dual recordings were consistent with a presynaptic locus of expression. ..
- Nogués L, Reglero C, Rivas V, Salcedo A, Lafarga V, Neves M, et al. G Protein-coupled Receptor Kinase 2 (GRK2) Promotes Breast Tumorigenesis Through a HDAC6-Pin1 Axis. EBioMedicine. 2016;13:132-145 pubmed publisher..Our data suggest that GRK2 acts as an important onco-modulator by strengthening the functionality of key players in breast tumorigenesis such as HDAC6 and Pin1. ..
- Fu Q, Cheng J, Zhang J, Zhang Y, Chen X, Xie J, et al. [MiR-145 inhibits drug resistance to Oxaliplatin in colorectal cancer cells through regulating G protein coupled receptor 98]. Zhonghua Wei Chang Wai Ke Za Zhi. 2017;20:566-570 pubmed..41±0.16 vs. 1.98±0.13, P<0.05). MiR-145 inhibits drug resistance to L-OHP of HCT116 cells through suppressing the expression of target gene GPR98. ..
- Schattauer S, Land B, Reichard K, Abraham A, Burgeno L, Kuhar J, et al. Peroxiredoxin 6 mediates GÎ±i protein-coupled receptor inactivation by cJun kinase. Nat Commun. 2017;8:743 pubmed publisher..Here the authors show that opioid receptor activation recruits peroxiredoxin 6 (PRDX6) to the receptor-GÎ±i complex by c-Jun N-terminal kinase, resulting in GÎ±i depalmitoylation and enhanced receptor-GÎ±i association. ..
- Zou Y, Weis W, Kobilka B. N-terminal T4 lysozyme fusion facilitates crystallization of a G protein coupled receptor. PLoS ONE. 2012;7:e46039 pubmed publisher..This approach adds to the protein engineering strategies that enable crystallographic studies of GPCRs alone or in complex with a signaling partner. ..
- Black J, Premont R, Daaka Y. Feedback regulation of G protein-coupled receptor signaling by GRKs and arrestins. Semin Cell Dev Biol. 2016;50:95-104 pubmed publisher..Hence, a better understanding of their overall signal regulation is of great translational interest and research continues to exploit the pharmacologic potential for modulating their activity. ..
- Fang J, Liu X, Bolanos L, Barker B, Rigolino C, Cortelezzi A, et al. A calcium- and calpain-dependent pathway determines the response to lenalidomide in myelodysplastic syndromes. Nat Med. 2016;22:727-34 pubmed publisher..Our study describes a cellular mechanism by which LEN, acting through CRBN and IKZF1, has cytotoxic effects in MDS and AML that depend on a calcium- and calpain-dependent pathway. ..
- Nag J, Rudina T, Maoz M, Grisaru Granovsky S, Uziely B, Bar Shavit R. Cancer driver G-protein coupled receptor (GPCR) induced β-catenin nuclear localization: the transcriptional junction. Cancer Metastasis Rev. 2018;37:147-157 pubmed publisher..We discuss recent advances in understanding the molecular path leading to β-catenin nuclear localization and transcriptional activity and their implications for future cancer therapy research. ..
- Keshelava A, Solis G, Hersch M, Koval A, Kryuchkov M, Bergmann S, et al. High capacity in G protein-coupled receptor signaling. Nat Commun. 2018;9:876 pubmed publisher..We estimate the channel capacity of this system to be above two, implying that at least four concentration levels of the agonist can be distinguished reliably. These findings shed light on the basic principles of GPCR signaling. ..
- Brailoiu E, Barlow C, Ramirez S, Abood M, Brailoiu G. Effects of Platelet-Activating Factor on Brain Microvascular Endothelial Cells. Neuroscience. 2018;377:105-113 pubmed publisher..Our studies reveal that PAF alters the BBB permeability by multiple mechanisms, which may be relevant for central nervous system (CNS) inflammatory disorders. ..
- Matsui K, Ozawa M, Kiso M, Yamashita M, Maekawa T, Kubota M, et al. Stimulation of alpha2-adrenergic receptors impairs influenza virus infection. Sci Rep. 2018;8:4631 pubmed publisher..Clonidine may thus protect against lung damage caused by influenza virus infection. Our results identify Î±2-AR-mediated signaling as a key pathway to exploit in the development of anti-influenza agents. ..
- Hussain H, Du Y, Scull N, Mortensen J, Tarrasch J, Bae H, et al. Accessible Mannitol-Based Amphiphiles (MNAs) for Membrane Protein Solubilisation and Stabilisation. Chemistry. 2016;22:7068-73 pubmed publisher..The ease of preparation together with the enhanced membrane protein stabilisation efficacy demonstrates the value of these agents for future membrane protein research. ..
- Nag S, Mokha S. Activation of the trigeminal ?2-adrenoceptor produces sex-specific, estrogen dependent thermal antinociception and antihyperalgesia using an operant pain assay in the rat. Behav Brain Res. 2016;314:152-8 pubmed publisher..These findings may help the discovery of effective analgesics for each sex. ..
- Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, et al. Activation mechanism of endothelin ETB receptor by endothelin-1. Nature. 2016;537:363-368 pubmed publisher..A comparison with the M2 muscarinic receptor suggests a shared mechanism for signal transduction in class A G-protein-coupled receptors. ..