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https://www.readbyqxmd.com/read/29068046/gpr35-mediates-lodoxamide-induced-migration-inhibitory-response-but-not-cxcl17-induced-migration-stimulatory-response-in-thp-1-cells-is-gpr35-a-receptor-for-cxcl17
#1
Soo-Jin Park, Seung-Jin Lee, So-Yeon Nam, Dong-Soon Im
GPR35 has long been considered an orphan G protein-couple receptor, and although no endogenous ligand of GPR35 has been discovered, synthetic agonists and antagonists have been developed. CXCL17 (a chemokine) has been reported to be an endogenous ligand of GPR35, and it has even been suggested that it be called CXCR8 (Journal of Immunology 2015; 194:29-33). However, no supporting report on the CXCL17-GPR35 relation has been issued since, although GPR35 is supposed to be a potential therapeutic target in several pathologic conditions...
October 25, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28961156/exome-array-analysis-identifies-gpr35-as-a-novel-susceptibility-gene-for-anthracycline-induced-cardiotoxicity-in-childhood-cancer
#2
Sara Ruiz-Pinto, Guillermo Pita, Ana Patiño-García, Javier Alonso, Antonio Pérez-Martínez, Antonio J Cartón, Federico Gutiérrez-Larraya, María R Alonso, Daniel R Barnes, Joe Dennis, Kyriaki Michailidou, Carmen Gómez-Santos, Deborah J Thompson, Douglas F Easton, Javier Benítez, Anna González-Neira
OBJECTIVES: Pediatric cancer survivors are a steadily growing population; however, chronic anthracycline-induced cardiotoxicity (AIC) is a serious long-term complication leading to considerable morbidity. We aimed to identify new genes and low-frequency variants influencing the susceptibility to AIC for pediatric cancer patients. PATIENTS AND METHODS: We studied the association of variants on the Illumina HumanExome BeadChip array in 83 anthracycline-treated pediatric cancer patients...
September 27, 2017: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/28943434/the-role-and-clinical-significance-of-the-cxcl17-cxcr8-gpr35-axis-in-breast-cancer
#3
Ya Jie Guo, Yu Jie Zhou, Xiao Li Yang, Zhi Min Shao, Zhou Luo Ou
BACKGROUND: Chemokine (C-X-C motif) ligand 17 (CXCL17) is the latest member of the chemokine family. However, its function in various cancer types is unknown. The G protein-coupled receptor 35 (GPR35) was identified as the receptor of CXCL17 and named recently as CXCR8. The function of the CXCL17-CXCR8 (GPR35) biological axis in cancer has not been reported. METHODS: The expression of CXCL17 and CXCR8 (GPR35) in breast cancer cell lines and a tissue microarray (TMA) was detected through western blot and immunohistochemistry (IHC)...
November 25, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28940377/g-protein-coupled-receptors-not-currently-in-the-spotlight-free-fatty-acid-receptor-2-and-gpr35
#4
REVIEW
Graeme Milligan
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in the human genome are the targets of a clinically used medicine. In many cases this is likely to reflect a lack of understanding of the basic underpinning biology of many G protein-coupled receptors that are not currently in the spotlight, as well as a paucity of pharmacological tool compounds and appropriate animal models to test in vivo function of such G protein-coupled receptors in both normal physiology and in the context of disease...
September 21, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28690198/punicalagin-a-ptp1b-inhibitor-induces-m2c-phenotype-polarization-via-up-regulation-of-ho-1-in-murine-macrophages
#5
Xiaolong Xu, Yuhong Guo, Jingxia Zhao, Shasha He, Yan Wang, Yan Lin, Ning Wang, Qingquan Liu
Current data have shown that punicalagin (PUN), an ellagitannin isolated from pomegranate, possesses anti-inflammatory and anti-oxidant properties; however, its direct targets have not yet been reported. This is the first report that PTP1B serves as a direct target of PUN, with IC50 value of 1.04μM. Results from NPOI further showed that the Kon and Koff of PUN-PTP1B complex were 3.38e2M(-1)s(-1) and 4.13e-3s(-1), respectively. The active site Arg24 of PTP1B was identified as a key binding site of PUN by computation simulation and point mutation...
July 8, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28648739/g-protein-coupled-receptor-35-contributes-to-mucosal-repair-in-mice-via-migration-of-colonic-epithelial-cells
#6
Takuya Tsukahara, Nahla Hamouda, Daichi Utsumi, Kenjiro Matsumoto, Kikuko Amagase, Shinichi Kato
G protein-coupled receptor 35 (GPR35), a receptor for lysophosphatidic acid, is highly expressed in the gastrointestinal tract. Recently, GPR35 has been implicated in the onset of inflammatory bowel disease (IBD), but its role in physiological and pathological processes in the colon remains undefined. In this study, we investigated the contribution of GPR35-mediated signalling to mucosal repair of colonic epithelium in IBD. GPR35 function was examined in a wound healing model, using young adult mouse colon epithelium (YAMC) cells, and in a dextran sulphate sodium (DSS)-induced mouse model of colitis...
June 23, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28446062/metabolite-sensing-g-protein-coupled-receptors-facilitators-of-diet-related-immune-regulation
#7
Jian K Tan, Craig McKenzie, Eliana Mariño, Laurence Macia, Charles R Mackay
Nutrition and the gut microbiome regulate many systems, including the immune, metabolic, and nervous systems. We propose that the host responds to deficiency (or sufficiency) of dietary and bacterial metabolites in a dynamic way, to optimize responses and survival. A family of G protein-coupled receptors (GPCRs) termed the metabolite-sensing GPCRs bind to various metabolites and transmit signals that are important for proper immune and metabolic functions. Members of this family include GPR43, GPR41, GPR109A, GPR120, GPR40, GPR84, GPR35, and GPR91...
April 26, 2017: Annual Review of Immunology
https://www.readbyqxmd.com/read/28425521/chemical-genomic-analysis-of-gpr35-signaling
#8
Heidi Haibei Hu, Huayun Deng, Shizhang Ling, Haiyan Sun, Terry Kenakin, Xinmiao Liang, Ye Fang
GPR35, a family A orphan G protein-coupled receptor, has been implicated in inflammatory, neurological, and cardiovascular diseases. However, not much is known about the signaling and functions of GPR35. We performed a label-free kinome short hairpin RNA screen and identified a putative signaling network of GPR35 in HT-29 cells, some of which was validated using gene expression, biochemical and cellular assays. The results showed that GPR35 induced hypoxia-inducible factor 1α, and was involved in synaptic transmission, sensory perception, the immune system, and morphogenetic processes...
May 22, 2017: Integrative Biology: Quantitative Biosciences From Nano to Macro
https://www.readbyqxmd.com/read/28289782/neuro-psychopharmacological-perspective-of-orphan-receptors-of-rhodopsin-class-a-family-of-g-protein-coupled-receptors
#9
REVIEW
Muhammad Zahid Khan, Ling He
BACKGROUND: In the central nervous system (CNS), G protein-coupled receptors (GPCRs) are the most fruitful targets for neuropsychopharmacological drug development. Rhodopsin (class A) is the most studied class of GPCR and includes orphan receptors for which the endogenous ligand is not known or is unclear. Characterization of orphan GPCRs has proven to be challenging, and the production pace of GPCR-based drugs has been incredibly slow. OBJECTIVE: Determination of the functions of these receptors may provide unexpected insight into physiological and neuropathological processes...
April 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28207301/mucosal-chemokines
#10
Marcela Hernández-Ruiz, Albert Zlotnik
Several chemokines have important functions in mucosal immunity. While there are many chemokines, 4 of them (CCL25, CCL28, CXCL14, and CXCL17) are especially important in mucosal immunity because they are homeostatically expressed in mucosal tissues. Of these, only CCL25 and CCL28 have been widely recognized as mucosal chemokines. In this study, we review the physiology of these chemokines with specific emphasis on their function in mucosal immunity. CCL25 recruits certain important subsets of T cells that express CCR9 to the small intestine...
February 2017: Journal of Interferon & Cytokine Research
https://www.readbyqxmd.com/read/27989666/structure-activity-relationships-of-benzothiazole-gpr35-antagonists
#11
Manahil M Abdalhameed, Pingwei Zhao, Dow P Hurst, Patricia H Reggio, Mary E Abood, Mitchell P Croatt
The first structure-activity relationships for a benzothiazole scaffold acting as an antagonist at GPR35 is presented. Analogues were designed based on a lead compound that was previously determined to have selective activity as a GPR35 antagonist. The synthetic route was modular in nature to independently explore the role of the middle and both ends of the scaffold. The activities of the analogues illustrate the importance of all three segments of the compound.
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27976894/discovery-of-2h-chromen-2-one-derivatives-as-g-protein-coupled-receptor-35-agonists
#12
Lai Wei, Jixia Wang, Xiuli Zhang, Ping Wang, Yaopeng Zhao, Jiaqi Li, Tao Hou, Lala Qu, Liying Shi, Xinmiao Liang, Ye Fang
A family of 2H-chromen-2-one derivatives were identified as G protein-coupled receptor-35 (GPR35) agonists using dynamic mass redistribution assays in HT-29 cells. The compounds with 1H-tetrazol-5-yl in 3-substituted position displayed higher potency than the corresponding carboxyl analogs, and the hydroxyl group in the 7-position also played an important role in GPR35 agonistic activity. 6-Bromo-7-hydroxy-8-nitro-3-(1H-tetrazol-5-yl)-2H-chromen-2-one (50) was found to be the most potent GPR35 agonist with an EC50 of 5...
January 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27777084/crosstalk-between-the-gut-and-the-liver-via-susceptibility-loci-novel-advances-in-inflammatory-bowel-disease-and-autoimmune-liver-disease
#13
REVIEW
Xinyang Li, Jun Shen, Zhihua Ran
Inflammatory bowel disease (IBD) is an autoimmune disorder characterized by chronic, relapsing intestinal inflammation. Autoimmune liver disease (AILD) may be involved in IBD as an extra-intestinal manifestation (EIM). Epidemiologic and anatomic evidence have demonstrated an intimate crosstalk between the gut and the liver. In this review, we briefly introduced nine groups of susceptibility loci shared by inflammatory bowel and autoimmune liver disease for the first time. The genome-wide association studies (GWAS) evidence of pathways involving crosstalk between the gut and the liver is clarified and explained...
February 2017: Clinical Immunology: the Official Journal of the Clinical Immunology Society
https://www.readbyqxmd.com/read/27755520/-the-kynurenic-acid-hypothesis-a-new-look-at-etiopathogenesis-and-treatment-of-schizophrenia
#14
REVIEW
Marta Flis, Kinga Szymona, Justyna Morylowska-Topolska, Anna Urbańska, Paweł Krukow, Martyna Kandefer-Szerszeń, Barbara Zdzisińska, Ewa M Urbańska, Hanna Karakuła-Juchnowicz
Kynurenic acid (KYNA) is a neuroactive metabolite of tryptophan formed in the brain and in the periphery, known to block ionotropic glutamate receptors and α7 nicotinic receptors, and to act as a ligand of G protein-coupled GPR35 receptors and human aryl hydrocarbon (AHR) receptors. KYNA seems to modulate a number of mechanisms involved in the pathogenesis of schizophrenia including dopaminergic transmission in mesolimbic and mesocortical areas or glutamatemediated neurotransmission. The kynurenine hypothesis of schizophrenia links the occurrence of positive and negative symptoms of schizophrenia and cognitive impairments characteristic for the disease with the disturbances of kynurenine pathway function...
September 29, 2016: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/27424891/label-free-cell-phenotypic-identification-of-d-luciferin-as-an-agonist-for-gpr35
#15
Heidi Hu, Huayun Deng, Ye Fang
D-Luciferin (also known as beetle or firefly luciferin) is one of the most widely used bioluminescent reporters for monitoring in vitro or in vivo luciferase activity. The identification of several natural phenols and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as agonists for GPR35, an orphan G protein-coupled receptor, had motivated us to examine the pharmacological activity of D-Luciferin, given that it also contains phenol and carboxylic acid moieties. Here, we describe label-free cell phenotypic assays that ascertain D-Luciferin as a partial agonist for GPR35...
2016: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27350736/comprehensive-mutation-screening-for-10-genes-in-chinese-patients-suffering-very-early-onset-inflammatory-bowel-disease
#16
Yuan Xiao, Xin-Qiong Wang, Yi Yu, Yan Guo, Xu Xu, Ling Gong, Tong Zhou, Xiao-Qin Li, Chun-Di Xu
AIM: To perform sequencing analysis in patients with very early-onset inflammatory bowel disease (VEO-IBD) to determine the genetic basis for VEO-IBD in Chinese pediatric patients. METHODS: A total of 13 Chinese pediatric patients with VEO-IBD were diagnosed from May 2012 and August 2014. The relevant clinical characteristics of these patients were analyzed. Then DNA in the peripheral blood from patients was extracted. Next generation sequencing (NGS) based on an Illumina-Miseq platform was used to analyze the exons in the coding regions of 10 candidate genes: IL-10, IL-10RA, IL-10RB, NOD2, FUT2, IL23R, GPR35, GPR65, TNFSF15, and ADAM30...
June 28, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/27347941/computational-analysis-of-single-nucleotide-polymorphisms-associated-with-altered-drug-responsiveness-in-type-2-diabetes
#17
Valerio Costa, Antonio Federico, Carla Pollastro, Carmela Ziviello, Simona Cataldi, Pietro Formisano, Alfredo Ciccodicola
Type 2 diabetes (T2D) is one of the most frequent mortality causes in western countries, with rapidly increasing prevalence. Anti-diabetic drugs are the first therapeutic approach, although many patients develop drug resistance. Most drug responsiveness variability can be explained by genetic causes. Inter-individual variability is principally due to single nucleotide polymorphisms, and differential drug responsiveness has been correlated to alteration in genes involved in drug metabolism (CYP2C9) or insulin signaling (IRS1, ABCC8, KCNJ11 and PPARG)...
June 25, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27131920/kynurenic-acid-and-zaprinast-induce-analgesia-by-modulating-hcn-channels-through-gpr35-activation
#18
Francesco Resta, Alessio Masi, Maria Sili, Annunziatina Laurino, Flavio Moroni, Guido Mannaioni
Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels have a key role in the control of cellular excitability. HCN2, a subgroup of the HCN family channels, are heavily expressed in small dorsal root ganglia (DRG) neurons and their activation seems to be important in the determination of pain intensity. Intracellular elevation of cAMP levels activates HCN-mediated current (Ih) and small DRG neurons excitability. GPR35, a Gi/o coupled receptor, is highly expressed in small DRG neurons, and we hypothesized that its activation, mediated by endogenous or exogenous ligands, could lead to pain control trough a reduction of Ih current...
September 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27064272/g-protein-coupled-receptor-35-mediates-human-saphenous-vein-vascular-smooth-muscle-cell-migration-and-endothelial-cell-proliferation
#19
Jennifer E McCallum, Amanda E Mackenzie, Nina Divorty, Carolyn Clarke, Christian Delles, Graeme Milligan, Stuart A Nicklin
Vascular smooth muscle cell (VSMC) migration and proliferation is central to neointima formation in vein graft failure following coronary artery bypass. However, there are currently no pharmacological interventions that prevent vein graft failure through intimal occlusion. It is hence a therapeutic target. Here, we investigated the contribution of GPR35 to human VSMC and endothelial cell (EC) migration, using a scratch-wound assay, and also the contribution to proliferation, using MTS and BrdU assays, in in vitro models using recently characterized human GPR35 ortholog-selective small-molecule agonists and antagonists...
2015: Journal of Vascular Research
https://www.readbyqxmd.com/read/27002183/metabolism-meets-immunity-the-role-of-free-fatty-acid-receptors-in-the-immune-system
#20
REVIEW
Elisa Alvarez-Curto, Graeme Milligan
There are significant numbers of nutrient sensing G protein-coupled receptors (GPCRs) that can be found in cells of the immune system and in tissues that are involved in metabolic function, such as the pancreas or the intestinal epithelium. The family of free fatty acid receptors (FFAR1-4, GPR84), plus a few other metabolite sensing receptors (GPR109A, GPR91, GPR35) have been for this reason the focus of studies linking the effects of nutrients with immunological responses. A number of the beneficial anti-inflammatory effects credited to dietary fats such as omega-3 fatty acids are attributed to their actions on FFAR4...
August 15, 2016: Biochemical Pharmacology
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