Genomes and Genes
Gene Symbol: CYSLTR2
Description: cysteinyl leukotriene receptor 2
Alias: CYSLT2, CYSLT2R, GPCR21, HG57, HPN321, KPG_011, PSEC0146, hGPCR21, cysteinyl leukotriene receptor 2, G-protein coupled receptor GPCR21, G-protein coupled receptor HG57, cysteinyl leukotriene CysLT2 receptor
Publications132 found, 100 shown here
- Mellor E, Frank N, Soler D, Hodge M, Lora J, Austen K, et al. Expression of the type 2 receptor for cysteinyl leukotrienes (CysLT2R) by human mast cells: Functional distinction from CysLT1R. Proc Natl Acad Sci U S A. 2003;100:11589-93 pubmed..We now report that hMCs express the type 2 receptor for cysLTs (CysLT2R) as well, and that the amount of surface CysLT2R protein increases in response to priming with IL-4...
- Fukai H, Ogasawara Y, Migita O, Koga M, Ichikawa K, Shibasaki M, et al. Association between a polymorphism in cysteinyl leukotriene receptor 2 on chromosome 13q14 and atopic asthma. Pharmacogenetics. 2004;14:683-90 pubmedb>Cysteinyl leukotriene receptor 2 (CYSLTR2) is one of the receptors for the cysteinyl leukotrienes (CYSLTs), which cause bronchoconstrictions, vascular hyperpermeability and mucus hypersecretion in asthmatic patients...
- Hui Y, Cheng Y, Smalera I, Jian W, Goldhahn L, Fitzgerald G, et al. Directed vascular expression of human cysteinyl leukotriene 2 receptor modulates endothelial permeability and systemic blood pressure. Circulation. 2004;110:3360-6 pubmed..are mediated by 2 receptors: cysteinyl leukotriene 1 receptor (CysLT1R) and cysteinyl leukotriene 2 receptor (CysLT2R). However, the distinct contribution of CysLT2R to the vascular actions of CysLTs has not been addressed...
- Thompson C, Cloutier A, Bosse Y, Poisson C, Larivee P, McDonald P, et al. Signaling by the cysteinyl-leukotriene receptor 2. Involvement in chemokine gene transcription. J Biol Chem. 2008;283:1974-84 pubmedCysteinyl-leukotrienes are involved in inflammation and act on at least two G-protein-coupled receptors, CysLT1 and CysLT2. However, the role of the CysLT2 receptor as well as its signaling remain poorly understood...
- Gimpl G, Fahrenholz F. The oxytocin receptor system: structure, function, and regulation. Physiol Rev. 2001;81:629-83 pubmed..One has to conclude that the physiological regulation of the OT system will remain puzzling as long as the molecular mechanisms of genomic and nongenomic actions of steroids have not been clarified...
- Song X, Zhu S, Xie Y, Liu J, Sun L, Zeng D, et al. JTC801 Induces pH-dependent Death Specifically in Cancer Cells and Slows Growth of Tumors in Mice. Gastroenterology. 2018;154:1480-1493 pubmed publisher..Levels of CA9 are increased in human cancer tissues. JTC801 might be developed for treatment of pancreatic cancer. ..
- Qi L, Huang C, Wu X, Tao Y, Yan J, Shi T, et al. Hierarchical Specification of Pruriceptors by Runt-Domain Transcription Factor Runx1. J Neurosci. 2017;37:5549-5561 pubmed publisher..the interleukin-31 receptor A (IL-31ra) and its coreceptor oncostatin M receptor (Osmr), the cysteinyl leukotriene receptor 2 (Cysltr2), somatostatin, and neurotensin...
- Hua F, Shang S, Yang Y, Zhang H, Xu T, Yu J, et al. TRIB3 Interacts With β-Catenin and TCF4 to Increase Stem Cell Features of Colorectal Cancer Stem Cells and Tumorigenesis. Gastroenterology. 2019;156:708-721.e15 pubmed publisher..Knockdown of TRIB3 decreases colon neoplasia in mice, migration of CRC cells, and their growth as xenograft tumors in mice. Strategies to block TRIB3 activity might be developed for treatment of CRC. ..
- Chen C, Perry T, Chitko McKown C, Smith A, Cheung L, Beshah E, et al. The regulatory actions of retinoic acid on M2 polarization of porcine macrophages. Dev Comp Immunol. 2019;98:20-33 pubmed publisher..were independently upregulated by both IL-4 and ATRA, including the adenosine receptor A2B (ADORA2B), cysteinyl leukotriene receptor 2 (CYSLTR2) and the vitamin D receptor (VDR)...
- Liu T, Barrett N, Kanaoka Y, Yoshimoto E, Garofalo D, Cirka H, et al. Type 2 Cysteinyl Leukotriene Receptors Drive IL-33-Dependent Type 2 Immunopathology and Aspirin Sensitivity. J Immunol. 2018;200:915-927 pubmed publisher..These responses were mitigated by deletions of either Cysltr2 or leukotriene C4 synthase (Ltc4s)...
- Di Gennaro A, Araújo A, Busch A, Jin H, Wågsäter D, Vorkapic E, et al. Cysteinyl leukotriene receptor 1 antagonism prevents experimental abdominal aortic aneurysm. Proc Natl Acad Sci U S A. 2018;115:1907-1912 pubmed publisher..Furthermore, aneurysm progression was specifically mediated through CysLT1 signaling since a selective CysLT2 antagonist was without effect...
- Najar M, Fayyad Kazan M, Raicevic G, Fayyad Kazan H, Meuleman N, Bron D, et al. Advanced Glycation End-Products-, C-Type Lectin- and Cysteinyl/ Leukotriene-Receptors in Distinct Mesenchymal Stromal Cell Populations: Differential Transcriptional Profiles in Response to Inflammation. Cell J. 2018;20:250-258 pubmed publisher..leukotriene B4 (LTB4) receptors (BLT1 and BLT2) and cysteinyl leukotrienes (CysLTs) receptors (CYSLTR1 and CYSLTR2) in distinct populations of MSCs grown under basic or inflammatory conditions...
- Rayner B, Ramesar R. The importance of G protein-coupled receptor kinase 4 (GRK4) in pathogenesis of salt sensitivity, salt sensitive hypertension and response to antihypertensive treatment. Int J Mol Sci. 2015;16:5741-9 pubmed publisher..It may also underlie the difference in hypertension between different geographically derived population groups, and form a basis for pharmacogenomic approaches to treatment of hypertension. ..
- 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. ..
- Dolinska M, Piccini A, Wong W, Gelali E, Johansson A, Klang J, et al. Leukotriene signaling via ALOX5 and cysteinyl leukotriene receptor 1 is dispensable for in vitro growth of CD34+CD38- stem and progenitor cells in chronic myeloid leukemia. Biochem Biophys Res Commun. 2017;490:378-384 pubmed publisher..BCR-ABL+CD34+CD38- cells expressed cysteinyl leukotriene receptors CYSLT1 and CYSLT2. However, montelukast, an inhibitor of CYSLT1, also failed to significantly suppress CFU-C and LTC-IC growth...
- 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. ..
- Guo R, Jiang J, Jing Z, Chen Y, Shi Z, Deng B. Cysteinyl leukotriene receptor 1 regulates glucose-stimulated insulin secretion (GSIS). Cell Signal. 2018;46:129-134 pubmed publisher..Collectively, our findings highlight the essential role of cysLT1R in suppressing pancreatic insulin secretion, and potentially provided a new insight into understanding the mechanical regulation of glucose homeostasis. ..
- Wei J, Chen S, Guo W, Feng B, Yang S, Huang C, et al. Leukotriene D4 induces cellular senescence in osteoblasts. Int Immunopharmacol. 2018;58:154-159 pubmed publisher..However, cysLT2R was not expressed in these cells...
- 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. ..
- Song W, Zhang Y, Wang J, Ma T, Hao L, Wang K. Antagonism of cysteinyl leukotriene receptor 1 (cysLTR1) by montelukast suppresses cell senescence of chondrocytes. Cytokine. 2018;103:83-89 pubmed publisher..In the current study, we found that cysLTR1 but not cysLTR2 is expressed in human primary chondrocytes...
- Ballerini P, Di Iorio P, Ciccarelli R, Caciagli F, Poli A, Beraudi A, et al. P2Y1 and cysteinyl leukotriene receptors mediate purine and cysteinyl leukotriene co-release in primary cultures of rat microglia. Int J Immunopathol Pharmacol. 2005;18:255-68 pubmed..RT-PCR analysis showed that microglia expressed both CysLT1 / CysLT2 receptors, P2Y1ATP receptors and several members of the ATP binding cassette (ABC) transporters including MRP1, ..
- 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. ..
- 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
- Liu C, Lin C, Yao J, Wei Q, Xing G, Cao X. Dynamic expression analysis of armc10, the homologous gene of human GPRASP2, in zebrafish embryos. Mol Med Rep. 2017;16:5931-5937 pubmed publisher..The results of the present study provided novel insight into the spatial and temporal mRNA expression of armc10 in zebrafish, for the further investigation of nervous system diseases. ..
- Fung S, Xu C, Hamel E, Wager Miller J, Woodruff G, Miller A, et al. Novel indole-based compounds that differentiate alkylindole-sensitive receptors from cannabinoid receptors and microtubules: Characterization of their activity on glioma cell migration. Pharmacol Res. 2017;115:233-241 pubmed publisher..Our study describes a new series of indole-based compounds that enable the pharmacological and functional differentiation of alkylindole-sensitive receptors from cannabinoid receptors and microtubules. ..
- Hu B, Kuang Z, Feng S, Wang D, He S, Kong D. Three-Dimensional Biologically Relevant Spectrum (BRS-3D): Shape Similarity Profile Based on PDB Ligands as Molecular Descriptors. Molecules. 2016;21: pubmed..We also applied BRS-3D in histone deacetylase 1 inhibitors screening and GPCR subtype selectivity prediction. The advantages and disadvantages of this approach are discussed. ..
- Sidhu C, Jaggupilli A, Chelikani P, Bhullar R. Regulation of Rac1 GTPase activity by quinine through G-protein and bitter taste receptor T2R4. Mol Cell Biochem. 2017;426:129-136 pubmed publisher..Further investigation will help in better understanding the downstream signal transduction network of T2R4 and its extra-oral physiological roles. ..
- Stempel H, Jung M, PÃ©rez GÃ³mez A, Leinders Zufall T, Zufall F, Bufe B. Strain-specific Loss of Formyl Peptide Receptor 3 in the Murine Vomeronasal and Immune Systems. J Biol Chem. 2016;291:9762-75 pubmed publisher..The genome of at least 19 strains encodes a non-functional Fpr3 variant, whereas at least 13 other strains express an intact receptor. These results provide a foundation for understanding the in vivo function of Fpr3. ..
- Szwejser E, Maciuszek M, Casanova Nakayama A, Segner H, Verburg van Kemenade B, Chadzinska M. A role for multiple estrogen receptors in immune regulation of common carp. Dev Comp Immunol. 2017;66:61-72 pubmed publisher..Results comply with mediation by GPR30, partially functioning via phosphoinositide 3-kinase activation. These results furthermore demonstrate that neuroendocrine-immune communication via estrogen receptors is evolutionary conserved. ..
- Marivin A, Leyme A, Parag Sharma K, DiGiacomo V, Cheung A, Nguyen L, et al. Dominant-negative G? subunits are a mechanism of dysregulated heterotrimeric G protein signaling in human disease. Sci Signal. 2016;9:ra37 pubmed publisher..Thus, ACS is caused by functionally dominant-negative mutations in a heterotrimeric G protein subunit. ..
- Arac D, Strater N, Seiradake E. Understanding the Structural Basis of Adhesion GPCR Functions. Handb Exp Pharmacol. 2016;234:67-82 pubmed..Here, we summarize current knowledge about the structural understanding for the extracellular regions of aGPCRs and discuss their possible functional roles that emerge from the available structural information. ..
- Chaplin R, Thach L, Hollenberg M, Cao Y, Little P, Kamato D. Insights into cellular signalling by G protein coupled receptor transactivation of cell surface protein kinase receptors. J Cell Commun Signal. 2017;11:117-125 pubmed publisher..As such, this represents a novel direction for future research. This review will discuss the main mechanisms of GPCR mediated receptor transactivation and the pathways involved in intracellular responses. ..
- White C, Vanyai H, See H, Johnstone E, Pfleger K. Using nanoBRET and CRISPR/Cas9 to monitor proximity to a genome-edited protein in real-time. Sci Rep. 2017;7:3187 pubmed publisher..We have investigated the utility of CRISPR/Cas9 genome editing to create genome-edited fusion proteins that can be used as BRET donors and propose that this strategy can be used to overcome the need for exogenous donor expression. ..
- Chen I, Furutani K, Kurachi Y. Structural determinants at the M2 muscarinic receptor modulate the RGS4-GIRK response to pilocarpine by impairment of the receptor voltage sensitivity. Sci Rep. 2017;7:6110 pubmed publisher..These results provide novel insights into how membrane potential impacts G-protein signaling by modulating GPCR communication with downstream effectors. ..
- Allen S, Parthasarathy G, Darke P, Diehl R, Ford R, Hall D, et al. Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4. J Biol Chem. 2015;290:20360-73 pubmed publisher..Phosphopeptide mapping by mass spectrometry indicates an increased rate of autophosphorylation of a number of residues in GRK4Î± A486V relative to wild-type GRK4Î±, including Ser-485 in the kinase C-tail. ..
- Singh P, Peng W, Zhang Q, Ding X, Suo W. GRK5 deficiency leads to susceptibility to intermittent hypoxia-induced cognitive impairment. Behav Brain Res. 2016;302:29-34 pubmed publisher..These results suggest that GRK5 deficiency indeed makes the mice more susceptible to wide range of behavioral impairments, including cognitive impairments. ..
- 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. ..
- Xie K, Colgan L, Dao M, Muntean B, Sutton L, Orlandi C, et al. NF1 Is a Direct G Protein Effector Essential for Opioid Signaling to Ras in the Striatum. Curr Biol. 2016;26:2992-3003 pubmed publisher..These results delineate a novel mechanism of GPCR signaling to Ras pathways and establish a critical role of NF1 in opioid addiction. ..
- Guo X, Ma Z, Du B, Li T, Li W, Xu L, et al. Dop1 enhances conspecific olfactory attraction by inhibiting miR-9a maturation in locusts. Nat Commun. 2018;9:1193 pubmed publisher..Our results reveal a Dop1-miR-9a-AC2 circuit that modulates locust olfactory attraction underlying aggregation. This study suggests that miRNAs act as key messengers in the GPCR signaling. ..
- Huang T, Qiu X, Xiao J, Wang Q, Wang Y, Zhang Y, et al. The prognostic role of Leucine-rich repeat-containing G-protein-coupled receptor 5 in gastric cancer: A systematic review with meta-analysis. Clin Res Hepatol Gastroenterol. 2016;40:246-53 pubmed publisher..02-28.72) and lymph node metastasis (positive vs negative: OR 2.30, 95% CI 1.06-5.0). Our meta-analysis indicates that LGR5 may be a predictive factor for invasion and metastasis, and poor prognosis in patients with gastric cancer. ..
- Almeida Santos A, Kangussu L, Moreira F, Santos R, Aguiar D, Campagnole Santos M. Anxiolytic- and antidepressant-like effects of angiotensin-(1-7) in hypertensive transgenic (mRen2)27 rats. Clin Sci (Lond). 2016;130:1247-55 pubmed publisher..Again, Ang-(1-7) reversed this phenotype. Thus, our data showed that Ang-(1-7) can modulate anxiety- and depression-like behaviours in TGRs and warrant further investigation as a new therapy for certain psychiatric disorders. ..
- Ang S, Hutchinson D, Evans B, Hossain M, Patil N, Bathgate R, et al. The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4. Naunyn Schmiedebergs Arch Pharmacol. 2017;390:105-111 pubmed publisher..In contrast, no signaling activity or receptor internalization mechanisms were observed following relaxin-2 and INSL3. In conclusion, relaxin-3 is a high-efficacy agonist at RXFP4 with a comparable signal transduction profile to INSL5. ..
- Kirschmer N, Bandleon S, von Ehrlich Treuenstätt V, Hartmann S, Schaaf A, Lamprecht A, et al. TRPC4? and TRPC4? Similarly Affect Neonatal Cardiomyocyte Survival during Chronic GPCR Stimulation. PLoS ONE. 2016;11:e0168446 pubmed publisher..These findings suggest that TRPC4? and TRPC4? differentially affect Ca2+ signals, calcineurin/NFAT signaling and hypertrophy but similarly impair cardiomyocyte viability during GPCR stimulation. ..
- Faria R, Freitas H, Reis R. P2X7 receptor large pore signaling in avian MÃ¼ller glial cells. J Bioenerg Biomembr. 2017;49:215-229 pubmed publisher..We conclude that large conductance channel and other P2XRs are not involved in the ATP-induced dye uptake, but signaling pathways such as MAPK, PI3-K, microtubules or PKC are involved in pore formation. ..
- Ali H. Emerging Roles for MAS-Related G Protein-Coupled Receptor-X2 in Host Defense Peptide, Opioid, and Neuropeptide-Mediated Inflammatory Reactions. Adv Immunol. 2017;136:123-162 pubmed publisher..I will also examine the novel aspects of MRGPRX2 signaling in MCs as it related to degranulation and review the mechanisms of its regulation. ..
- Xu D, Li R, Wu J, Jiang L, Zhong H. Drug Design Targeting the CXCR4/CXCR7/CXCL12 Pathway. Curr Top Med Chem. 2016;16:1441-51 pubmed..Understanding these complex interactions will provide insight in drug design targeting the CXCR7 as potential anticancer therapy. ..
- Maayah Z, El Kadi A. The role of mid-chain hydroxyeicosatetraenoic acids in the pathogenesis of hypertension and cardiac hypertrophy. Arch Toxicol. 2016;90:119-36 pubmed publisher..This review provides a clear understanding of the role of mid-chain HETEs in the pathogenesis of cardiovascular diseases and their importance as novel targets in the treatment for hypertension and cardiac hypertrophy. ..
- Wittmann H, Seifert R, Strasser A. Mathematical analysis of the sodium sensitivity of the human histamine H3 receptor. In Silico Pharmacol. 2014;2:1 pubmed publisher..Although the present study is focused onto the Na(+)-sensitivity of the hH3R, the resulting equations, describing Na(+)- and ligand-binding to a GPCR, can be used for all other ion-sensitive GPCRs. ..
- Zou Y, Ning T, Shi J, Chen M, Ding L, Huang Y, et al. Association of a gain-of-function variant in LGR4 with central obesity. Obesity (Silver Spring). 2017;25:252-260 pubmed publisher..009) and the Matsuda index (P = 0.027) after an oral glucose tolerance test in young subjects with obesity. The LGR4 A750T variant may contribute to central obesity characterized by abdominal visceral fat accumulation. ..
- Kangussu L, Almeida Santos A, Moreira F, Fontes M, Santos R, Aguiar D, et al. Reduced anxiety-like behavior in transgenic rats with chronically overproduction of angiotensin-(1-7): Role of the Mas receptor. Behav Brain Res. 2017;331:193-198 pubmed publisher..Therefore, facilitation of the Ang-(1-7)/Mas receptor signaling may be further investigated as an additional strategy for the treatment of anxiety-related disorders. ..
- Xia R, Li M, Wu Y, Qi Y, Ye G, Huang J. A new family of insect muscarinic acetylcholine receptors. Insect Mol Biol. 2016;25:362-9 pubmed publisher..Knockdown of CG12796 in the central nervous system had no effect on male courtship behaviours. We suggest that CG12796 represents the first recognized member of a novel mAChR class...
- Jeon T, Yang H, Lee C, Oh S, Seo D, Baik I, et al. Electro-hyperthermia up-regulates tumour suppressor Septin 4 to induce apoptotic cell death in hepatocellular carcinoma. Int J Hyperthermia. 2016;32:648-56 pubmed publisher..Additionally, mEHT significantly inhibited the growth of human HCC xenografts in nude mice. These findings suggest that apoptotic cell death induced by mEHT is mediated by the up-regulation of tumour suppressor SEPT4 in human HCC cells. ..
- De Filippo E, Schiedel A, Manga P. Interaction between G Protein-Coupled Receptor 143 and Tyrosinase: Implications for Understanding Ocular Albinism Type 1. J Invest Dermatol. 2017;137:457-465 pubmed publisher..Identifying tyrosinase as a potential GPR143 binding protein opens new avenues for investigating the mechanisms that regulate pigmentation and neurogenesis. ..
- O Hayre M, Eichel K, Avino S, Zhao X, Steffen D, Feng X, et al. Genetic evidence that β-arrestins are dispensable for the initiation of β2-adrenergic receptor signaling to ERK. Sci Signal. 2017;10: pubmed publisher..These findings provide a molecular framework for β2AR signaling through β-arrestin-independent pathways in key physiological functions and under pathological conditions. ..
- Kono M, Conlon E, Lux S, Yanagida K, Hla T, Proia R. Bioluminescence imaging of G protein-coupled receptor activation in living mice. Nat Commun. 2017;8:1163 pubmed publisher..This imaging strategy reveals the dynamics and spatial specificity of S1P1 activation in normal and pathophysiologic contexts in vivo and can be applied to other GPCRs. ..
- Gupta K, Kotian A, Subramanian H, Daniell H, Ali H. Activation of human mast cells by retrocyclin and protegrin highlight their immunomodulatory and antimicrobial properties. Oncotarget. 2015;6:28573-87 pubmed publisher..Low cost production of AMPs in plants should facilitate their advancement to the clinic overcoming major hurdles in current production systems. ..
- Miller R, Thompson A, Trapella C, Guerrini R, Malfacini D, Patel N, et al. The Importance of Ligand-Receptor Conformational Pairs in Stabilization: Spotlight on the N/OFQ G Protein-Coupled Receptor. Structure. 2015;23:2291-2299 pubmed publisher..These results suggest a mechanism for ligand-aided crystallogenesis whereby potent antagonists stabilize a single ligand-receptor conformational pair. ..
- Zhao N, Wang L, Guo N. Î±-Linolenic acid increases the G0/G1 switch gene 2 mRNA expression in peripheral blood mononuclear cells from obese patients: a pilot study. Lipids Health Dis. 2016;15:36 pubmed publisher..Increased G0S2 gene expression might contribute to the beneficial anti-lipolytic effect of ALA in obese patients. ..
- Barchad Avitzur O, Priest M, Dekel N, Bezanilla F, Parnas H, Ben Chaim Y. A Novel Voltage Sensor in the Orthosteric Binding Site of the M2 Muscarinic Receptor. Biophys J. 2016;111:1396-1408 pubmed publisher..This voltage sensor is crucial for the voltage dependence of agonist binding to the receptor. The tyrosine-based voltage sensor discovered here constitutes a noncanonical by which membrane proteins may sense voltage. ..
- Balemans D, Boeckxstaens G, Talavera K, Wouters M. Transient receptor potential ion channel function in sensory transduction and cellular signaling cascades underlying visceral hypersensitivity. Am J Physiol Gastrointest Liver Physiol. 2017;312:G635-G648 pubmed publisher..We propose that a better understanding of TRP channels and their modulators may facilitate the development of more selective and effective therapies to treat visceral hypersensitivity. ..
- Taguchi K, Bessho N, Hasegawa M, Narimatsu H, Matsumoto T, Kobayashi T. Co-treatment with clonidine and a GRK2 inhibitor prevented rebound hypertension and endothelial dysfunction after withdrawal in diabetes. Hypertens Res. 2018;41:263-274 pubmed publisher..These results suggest that suppression of GRK2 activity affects rebound hypertension-associated vascular endothelial dysfunction by targeting the Akt/eNOS signaling pathway. ..
- Pillai S, Cousens D, Barnes A, Buckley P, Chiano M, Hosking L, et al. A coding polymorphism in the CYSLT2 receptor with reduced affinity to LTD4 is associated with asthma. Pharmacogenetics. 2004;14:627-33 pubmed..mediators in the pathophysiology of asthma for which two receptors have been characterized, CYSLTR1 and CYSLTR2. The leukotriene modifying agents currently used to control bronchoconstriction and inflammation in asthmatic ..
- Byrne E, Sircar R, Miller P, Hedger G, Luchetti G, Nachtergaele S, et al. Structural basis of Smoothened regulation by its extracellular domains. Nature. 2016;535:517-522 pubmed publisher..Our results clarify the structural mechanism by which the activity of a GPCR is controlled by ligand-regulated interactions between its extracellular and transmembrane domains. ..
- Coleman J, Ngo T, Smith N. The G protein-coupled receptor N-terminus and receptor signalling: N-tering a new era. Cell Signal. 2017;33:1-9 pubmed publisher..This review aims to discuss and integrate recent advances in knowledge of the vital roles of the GPCR N-terminus in receptor signalling. ..
- Ivarsson Y, Arnold R, McLaughlin M, Nim S, Joshi R, Ray D, et al. Large-scale interaction profiling of PDZ domains through proteomic peptide-phage display using human and viral phage peptidomes. Proc Natl Acad Sci U S A. 2014;111:2542-7 pubmed publisher..The method can be extended to interrogate all potential eukaryotic, bacterial, and viral SLiMs and we suggest it will be a highly valuable approach for studying cellular and pathogen-host protein-protein interactions. ..
- Di Pizio A, Kruetzfeldt L, Cheled Shoval S, Meyerhof W, Behrens M, Niv M. Ligand binding modes from low resolution GPCR models and mutagenesis: chicken bitter taste receptor as a test-case. Sci Rep. 2017;7:8223 pubmed publisher..The integrated approach validated here may be applicable to additional cases where the sequence identity of the GPCR of interest and the existing experimental structures is low. ..
- Moriyama R, Ueda K, Deura C. Effects of ovarian hormones on GPR120 mRNA expression in mouse pituitary gonadotrophs. Endocr J. 2017;64:1055-1061 pubmed publisher..These results demonstrate that ovarian hormones may directly regulate GPR120 expression in the reproductive cycle at the pituitary level. ..
- Barman N, Choudhury B, Kumar V, Koul M, Gogoi S, Khatoon E, et al. Incidence of elephant endotheliotropic herpesvirus in Asian elephants in India. Vet Microbiol. 2017;208:159-163 pubmed publisher..Moreover, the phylogenetic analysis of the polymerase, helicase, and GPCR genes from the infected tissue samples suggested the presence of EEHV1A virus. ..
- Yi Y, Tsai S, Cheng J, Wang E, Anglesio M, Cochrane D, et al. APELA promotes tumour growth and cell migration in ovarian cancer in a p53-dependent manner. Gynecol Oncol. 2017;147:663-671 pubmed publisher..Our findings uncover a potential oncogenic role for APELA in promoting ovarian tumour progression and provide a possible therapeutic strategy in ovarian cancer by targeting APELA. ..
- Zhou Y, Liu D, Chen S, Sun J, Zhou X, Xing C, et al. " The role of CXCR3 in neurological diseases". Curr Neuropharmacol. 2017;: pubmed publisher..The aim of this review is to provide evidence for the potential of CXCR3 as a therapeutic target for neurological diseases...
- Westphal M, Schafroth M, Sarott R, Imhof M, Bold C, Leippe P, et al. Synthesis of Photoswitchable ?9-Tetrahydrocannabinol Derivatives Enables Optical Control of Cannabinoid Receptor 1 Signaling. J Am Chem Soc. 2017;: pubmed publisher..As such, azo-THCs enable CB1-mediated optical control of inwardly-rectifying potassium channels, as well as adenylyl cyclase...
- McCorvy J, Butler K, Kelly B, Rechsteiner K, Karpiak J, Betz R, et al. Structure-inspired design of ?-arrestin-biased ligands for aminergic GPCRs. Nat Chem Biol. 2017;: pubmed publisher..This strategy may facilitate the structure-guided design of arrestin-biased ligands at other GPCRs, including polypharmacological biased ligands...
- Chen C, Li H, Long Y. GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. Bioorg Med Chem Lett. 2016;26:5603-5612 pubmed publisher..Herein, we summarized the newly disclosed biological characteristics and the druglikeness-based structural evolution of GPR40 agonists to advance the development of GPR40-based anti-diabetic drugs. ..
- Lingerfelt M, Zhao P, Sharir H, Hurst D, Reggio P, Abood M. Identification of Crucial Amino Acid Residues Involved in Agonist Signaling at the GPR55 Receptor. Biochemistry. 2017;56:473-486 pubmed publisher..This information should aid in the rational design of next-generation GPR55 ligands and the creation of the first high-affinity GPR55 radioligand, a tool that is sorely needed in the field. ..
- Piedra M, Berja A, Ramos L, Garcia Unzueta M, Morán J, Ruiz D, et al. Analysis of the influence of the T393C polymorphism of the GNAS gene on the clinical expression of primary hyperparathyroidism. Endocrinol Diabetes Nutr. 2017;64:524-530 pubmed publisher..This trend may be considered as a basis for further studies with larger sample sizes and complementary functional evaluation. ..
- Soundara Rajan T, Giacoppo S, Scionti D, Diomede F, Grassi G, Pollastro F, et al. Cannabidiol Activates Neuronal Precursor Genes in Human Gingival Mesenchymal Stromal Cells. J Cell Biochem. 2017;118:1531-1546 pubmed publisher..J. Cell. Biochem. 118: 1531-1546, 2017. © 2016 Wiley Periodicals, Inc...
- Chien C, Helfinger L, Bostock M, Solt A, Tan Y, Nietlispach D. An Adaptable Phospholipid Membrane Mimetic System for Solution NMR Studies of Membrane Proteins. J Am Chem Soc. 2017;139:14829-14832 pubmed publisher..Three representative MPs, including one G-protein-coupled receptor, were successfully incorporated into SapA-dimyristoylphosphatidylcholine nanoparticles and studied by solution NMR spectroscopy...
- Kim S, Nie H, Nesin V, Tran U, Outeda P, Bai C, et al. The polycystin complex mediates Wnt/Ca(2+) signalling. Nat Cell Biol. 2016;18:752-764 pubmed publisher..These data define PKD1 as a WNT (co)receptor and implicate defective WNT/Ca(2+) signalling as one of the causes of ADPKD. ..
- Mohan M, Chatterjee A, Ganapathy S, Mukherjee S, Srikanthan S, Jolly G, et al. Noncanonical regulation of insulin-mediated ERK activation by phosphoinositide 3-kinase ?. Mol Biol Cell. 2017;28:3112-3122 pubmed publisher..Thus, instead of classically mediating the kinase arm, PI3K? inhibits PP2A by scaffolding and sequestering, playing a key parallel synergistic step in sustaining the function of ERK, a nodal enzyme in multiple cellular processes. ..