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https://www.readbyqxmd.com/read/27872865/cxcr3-ccr5-and-crth2-chemokine-receptor-expression-in-lymphocytes-infiltrating-thyroid-nodules-with-coincident-hashimoto-s-thyroiditis-obtained-by-fine-needle-aspiration-biopsy
#1
Jan Jiskra, Marie Antošová, Jan Krátký, Hana Vítková, Zdeňka Límanová, Helena Marečková, Eliška Potluková
Objective. To determine the expression of chemokine receptors in lymphocytes from thyroid nodules and peripheral blood in patients with and without Hashimoto's thyroiditis (HT). Patients and Methods. The study included 46 women with thyroid nodules and HT and 60 women with thyroid nodules without HT (controls) who underwent a fine needle aspiration biopsy (FNAB). Expression of chemokine receptors CXCR3, CCR5, and CRTH2 was assessed by flow cytometry in lymphocytes from FNAB samples and from peripheral blood...
2016: Journal of Immunology Research
https://www.readbyqxmd.com/read/27735066/anti-inflammatory-therapies-in-atopic-dermatitis
#2
REVIEW
A Heratizadeh, T Werfel
The pathogenesis of atopic dermatitis (AD) is multifactorial and complex. Consequently, clinical signs and symptoms vary strongly depending on individually relevant trigger factors and the stage of the disease. So far, treatment of AD was commonly limited to topical treatment or, in more severe cases, to systemic drugs mostly approved for other indications than AD. However, emerging data on new anti-inflammatory agents have been published in the recent years. As these new substances specifically focus on immune responses in AD, these are partially considered as possible 'breakthrough' in the treatment of AD...
December 2016: Allergy
https://www.readbyqxmd.com/read/27621597/two-phase-ii-randomized-trials-on-the-crth2-antagonist-azd1981-in-adults-with-asthma
#3
Piotr Kuna, Leif Bjermer, Göran Tornling
BACKGROUND: Chemoattractant receptor-homologous molecule expressed on T helper type 2 (Th2) cell (CRTh2) receptor antagonists is being investigated for asthma. OBJECTIVES: The aim of this study was to assess the effects of the CRTh2 receptor antagonist, AZD1981 (with/without inhaled corticosteroids [ICSs]), on lung function and asthma control. PATIENTS AND METHODS: Adults aged 18-60 years were enrolled in two randomized, placebo-controlled, parallel-group trials (protocol number: D9830C00003 [study 1, n=209] and protocol number: D9830C00004 [study 2, n=510])...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27558866/an-s-warfarin-and-azd1981-interaction-in-vitro-and-clinical-pilot-data-suggest-the-n-deacetylated-amino-acid-metabolite-as-the-primary-perpetrator
#4
Ken Grime, Rikard Pehrson, Pär Nordell, Michael Gillen, Wolfgang Kühn, Timothy Mant, Marie Brännström, Petter Svanberg, Barry Jones, Clive Brealey
AIM: AZD1981 is an orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) receptor antagonist progressed to phase II trials for the treatment of allergic asthma. Previously performed in vitro human hepatocyte incubations identified N-deacetylated AZD1981 as a primary metabolite. We report on metabolite exposure from a clinical excretion balance, on in vitro studies performed to determine the likelihood of a metabolite-dependent drug-drug interaction (DDI) and on a clinical warfarin DDI study...
August 24, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27525671/assessing-the-new-and-emerging-treatments-for-atopic-dermatitis
#5
Lawrence F Eichenfield, Sheila F Friedlander, Eric L Simpson, Alan D Irvine
The newer and emerging treatments for atopic dermatitis (AD) focus on blockade of inflammatory cytokines, especially those that derive from T helper cell type 2 (TH2) and are associated with a pathway of immunoglobulin E (IgE) sensitization. Among the proinflammatory cytokines that have been identified as promising therapeutic targets are chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2), IgE, thymic stromal lymphopoietin (TSLP), and several monoclonal antibodies that block key cytokine pathways in the innate immune response...
June 2016: Seminars in Cutaneous Medicine and Surgery
https://www.readbyqxmd.com/read/27498997/discovery-of-anti-inflammatory-role-of-prostaglandin-d2
#6
Takahisa Murata, Toko Maehara
Nonsteroidal anti-inflammatory drugs (NSAIDs) including aspirin are one of the most frequently used classes of drug worldwide and inhibit prostaglandin (PG) production by inhibiting cyclooxygenase activity. Although NSAIDs are broadly used against inflammatory diseases, they have side effects including alimentary canal disorders, kidney damage, infection and cardiovascular disorders. Thus, it is necessary to elucidate the pathophysiological role of each PG in various diseases to develop better therapies with fewer and milder side effects...
December 1, 2016: Journal of Veterinary Medical Science
https://www.readbyqxmd.com/read/27481693/prostaglandin-d2-signaling-mediated-by-the-crth2-receptor-is-involved-in-mk-801-induced-cognitive-dysfunction
#7
Yusuke Onaka, Norihito Shintani, Takanobu Nakazawa, Takuya Kanoh, Yukio Ago, Toshio Matsuda, Ryota Hashimoto, Kazutaka Ohi, Hiroyuki Hirai, Kin-Ya Nagata, Masataka Nakamura, Atsushi Kasai, Atsuko Hayata-Takano, Kazuki Nagayasu, Kazuhiro Takuma, Asao Ogawa, Akemichi Baba, Hitoshi Hashimoto
Chemoattractant receptor-homologous molecule expressed on T helper type 2 cells (CRTH2), which is a second receptor for prostaglandin (PG) D2, is involved in inflammatory responses in peripheral tissue; however, its role in cognitive function remains unclear. Here, we demonstrate that CRTH2 is involved in cognitive function using a well-established animal model of cognitive dysfunction induced by MK-801, an N-methyl-d-aspartate receptor antagonist. Genetic deletion and pharmacological inhibition of CRTH2 suppressed MK-801-induced cognitive dysfunction...
November 1, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27354118/the-oral-crth2-antagonist-qaw039-fevipiprant-a-phase-ii-study-in-uncontrolled-allergic-asthma
#8
Veit J Erpenbeck, Todor A Popov, David Miller, Steven F Weinstein, Sheldon Spector, Baldur Magnusson, Wande Osuntokun, Paul Goldsmith, Markus Weiss, Jutta Beier
BACKGROUND: There is an unmet medical need for allergic asthma patients who are uncontrolled on conventional therapies. The aim of this study was to collect efficacy and safety data for QAW039, an oral chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) receptor antagonist, for the treatment of asthma. METHODS: This was an exploratory phase II, double-blind, randomized, placebo-controlled multi-center study. Patients with mild-to-moderate uncontrolled allergic asthma (N = 170) were either without or weaned off inhaled corticosteroids (ICS) and long-acting β-agonists (LABA) and randomized (1:1) to QAW039 (500 mg once daily) or to placebo for 28 days...
August 2016: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27317944/pharmacological-characterization-of-crth2-antagonist-las191859-long-receptor-residence-time-translates-into-long-lasting-in-vivo-efficacy
#9
Marta Calbet, Miriam Andrés, Clara Armengol, Mónica Bravo, Peter Eichhorn, Rosa López, Vicente García-González, Richard Roberts, Montserrat Miralpeix
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTh2) is a G protein-coupled receptor expressed on the leukocytes most closely associated with asthma and allergy like eosinophils, mast cells, Th2-lymphocytes and basophils. At present it is clear that CRTh2 mediates most prostaglandin D2 (PGD2) pro-inflammatory effects and as a result antagonists for this receptor have reached asthma clinical studies showing a trend of lung function improvement. The challenge remains to identify compounds with improved clinical efficacy when administered once a day...
September 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27310331/pharmacokinetics-safety-and-tolerability-of-fevipiprant-qaw039-a-novel-crth2-receptor-antagonist-results-from-2-randomized-phase-1-placebo-controlled-studies-in-healthy-volunteers
#10
Veit J Erpenbeck, Eva Vets, Lien Gheyle, Wande Osuntokun, Michael Larbig, Srikanth Neelakantham, David Sandham, Gerald Dubois, Walid Elbast, Paul Goldsmith, Markus Weiss
We evaluated the pharmacokinetics (PK), safety, and tolerability of a novel oral CRTh2 antagonist, fevipiprant (QAW039), in healthy subjects. Peak concentrations of fevipiprant in plasma were observed 1-3 hours postdosing. Concentrations declined in a multiexponential manner, followed by an apparent terminal phase (t1/2 , ∼20 hours). Steady state was achieved in 4 days with <2-fold accumulation. Elimination was partly by renal excretion (≤30% of the dose) and glucuronidation. Food had minimal impact on the PK of fevipiprant, and it was well tolerated at single and multiple oral doses up to 500 mg/day...
July 2016: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/27091669/effect-of-prostaglandin-d2-on-vegf-release-by-nasal-polyp-fibroblasts
#11
Kengo Kanai, Mitsuhiro Okano, Tazuko Fujiwara, Shin Kariya, Takenori Haruna, Ryotaro Omichi, Sei-Ichiro Makihara, Yuji Hirata, Kazunori Nishizaki
BACKGROUND: Vascular endothelial growth factor (VEGF) is known to be associated with the pathogenesis of chronic rhinosinusitis with nasal polyps (CRSwNP). VEGF is produced by a variety of cells including fibroblasts. It was recently reported that prostaglandin (PG) E2 induces VEGF release by nasal polyp fibroblasts. However, little is known regarding possible regulation of VEGF by other PGs. We have reported that molecules that regulate PGD2 metabolism play roles in the pathogenesis of CRS including in local eosinophilia and type 2 cytokine production...
April 15, 2016: Allergology International: Official Journal of the Japanese Society of Allergology
https://www.readbyqxmd.com/read/27079298/elevated-levels-of-circulating-cd4-crth2-t-cells-characterize-severe-asthma
#12
N S Palikhe, C Laratta, D Nahirney, D Vethanayagam, M Bhutani, H Vliagoftis, L Cameron
BACKGROUND: Chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) is a receptor for PGD2 and expressed by T cells, eosinophils, basophils, and ILC2 cells. CRTh2 expression by CD4(+) T cells identifies the Th2 subset, and these cells have been characterized as allergen-specific central memory Th2 cells. Recently, activation of the PGD2 -CRTh2 pathway in the lungs was associated with severe asthma. OBJECTIVE: To assess circulating levels of Th2 cells and related mediators in severe asthma and those who experience asthma exacerbations...
June 2016: Clinical and Experimental Allergy: Journal of the British Society for Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/26995677/prostaglandin-d2-is-a-novel-repressor-of-ifn%C3%AE-induced-indoleamine-2-3-dioxygenase-via-the-dp1-receptor-and-camp-pathway
#13
Nesrine Kamal Bassal, Bernard P Hughes, Maurizio Costabile
Expression of elevated levels of Indoleamine 2,3-dioxygenase (IDO) is well established as a mechanism of cancer induced immunosuppression. Pharmacological inhibition of IDO activity is thus a promising alternative in the treatment of cancer. Previously we demonstrated that cyclooxygenase derived metabolites of arachidonic acid inhibited the interferon-gamma mediated induction of IDO in both THP-1 cells and human monocytes. Here we identified that of the five primary prostanoids produced by COX-1/COX-2, only PGD2 displayed significant repressor activity...
July 2016: Prostaglandins, Leukotrienes, and Essential Fatty Acids
https://www.readbyqxmd.com/read/26976630/il-12-drives-functional-plasticity-of-human-group-2-innate-lymphoid-cells
#14
Ai Ing Lim, Silvia Menegatti, Jacinta Bustamante, Lionel Le Bourhis, Matthieu Allez, Lars Rogge, Jean-Laurent Casanova, Hans Yssel, James P Di Santo
Group 2 innate lymphoid cells (ILC2) include IL-5- and IL-13-producing CRTh2(+)CD127(+)cells that are implicated in early protective immunity at mucosal surfaces. Whereas functional plasticity has been demonstrated for both human and mouse ILC3 subsets that can reversibly give rise to IFN-γ-producing ILC1, plasticity of human or mouse ILC2 has not been shown. Here, we analyze the phenotypic and functional heterogeneity of human peripheral blood ILC2. Although subsets of human CRTh2(+)ILC2 differentially express CD117 (c-kit receptor), some ILC2 surface phenotypes are unstable and can be modulated in vitro...
April 4, 2016: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/26928963/eosinophils-contribute-to-intestinal-inflammation-via-chemoattractant-receptor-homologous-molecule-expressed-on-th2-cells-crth2-in-experimental-crohn-s-disease
#15
Balázs Radnai, Eva M Sturm, Angela Stančić, Katharina Jandl, Sandra Labocha, Nerea Ferreirós, Magdalena Grill, Carina Hasenoehrl, Gregor Gorkiewicz, Gunther Marsche, Ákos Heinemann, Christoph Högenauer, Rudolf Schicho
BACKGROUND AND AIMS: Prostaglandin [PG] D2 activates two receptors, DP and CRTH2. Antagonism of CRTH2 has been shown to promote anti-allergic and anti-inflammatory effects. We investigated whether CRTH2 may play a role in Crohn's disease [CD], focusing on eosinophils which are widely present in the inflamed mucosa of CD patients and express both receptors. METHODS: Using the 2,4,6-trinitrobenzenesulfonic acid [TNBS]-induced colitis model, involvement of CRTH2 in colitis was investigated by pharmacological antagonism, immunohistochemistry, Western blotting, immunoassay, and leukocyte recruitment...
September 2016: Journal of Crohn's & Colitis
https://www.readbyqxmd.com/read/26922232/structure-activity-relationships-sar-and-structure-kinetic-relationships-skr-of-sulphone-based-crth2-antagonists
#16
Maria Antonia Buil, Marta Calbet, Marcos Castillo, Jordi Castro, Cristina Esteve, Manel Ferrer, Pilar Forns, Jacob González, Sara López, Richard S Roberts, Sara Sevilla, Bernat Vidal, Laura Vidal, Pere Vilaseca
Monocyclic and bicyclic ring systems were investigated as the "core" section of a series of diphenylsulphone-containing acetic acid CRTh2 receptor antagonists. A range of potencies were observed and single-digit nanomolar potencies were obtained in both the monocyclic and bicyclic cores. Residence times for the monocyclic compounds were very short. Some of the bicyclic cores displayed better residence times. A methyl group in the northern part of the core, between the head and tail was a necessary requirement for the beginnings of long residence times...
May 4, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26916831/fevipiprant-qaw039-a-slowly-dissociating-crth2-antagonist-with-the-potential-for-improved-clinical-efficacy
#17
COMPARATIVE STUDY
David A Sykes, Michelle E Bradley, Darren M Riddy, Elizabeth Willard, John Reilly, Asadh Miah, Carsten Bauer, Simon J Watson, David A Sandham, Gerald Dubois, Steven J Charlton
Here we describe the pharmacologic properties of a series of clinically relevant chemoattractant receptor-homologous molecules expressed on T-helper type 2 (CRTh2) receptor antagonists, including fevipiprant (NVP-QAW039 or QAW039), which is currently in development for the treatment of allergic diseases. [(3)H]-QAW039 displayed high affinity for the human CRTh2 receptor (1.14 ± 0.44 nM) expressed in Chinese hamster ovary cells, the binding being reversible and competitive with the native agonist prostaglandin D2(PGD2)...
May 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/26874579/eosinophil-chemotaxis-assay-in-nasal-polyps-by-using-a-novel-optical-device-ez-taxiscan-role-of-cc-chemokine-receptor-3
#18
Hidekazu Saito, Kohei Honda, Chikara Asaka, Shigeharu Ueki, Kazuo Ishikawa
BACKGROUND: The chemokine receptor, CC-chemokine receptor 3 (CCR3), and its major ligands, eotaxin, RANTES, and MCP-4, are involved in eosinophil chemotaxis. It is thought that CCR3 plays an important role in the recruitment and activation of eosinophils in nasal polyposis. We examined nasal polyp extract-induced eosinophil chemotaxis and the effect of a CCR3 antagonist using EZ-TAXIScan, a novel real-time chemotaxis assay device. METHODS: Nasal polyps were obtained from chronic rhinosinusitis (CRS) patients during surgery...
July 2016: Allergology International: Official Journal of the Japanese Society of Allergology
https://www.readbyqxmd.com/read/26820529/prostaglandin-d2-elicits-the-reversible-neurite-retraction-in-hypothalamic-cell-line
#19
Hiroyoshi Tsuchiya, Hirofumi Hohjoh, Yoko Fujiwara, Yukihiko Sugimoto, Taka-Aki Koshimizu
Prostaglandins (PGs) play important roles in diverse physiological processes in the central nervous system. PGD2 is the most abundant PG in the brain and acts through specific receptors, DP1 and CRTH2. We investigated the effects of PGD2 on the morphology of the hypothalamic cell line mHypoE-N37 (N37). In N37 cells, serum starvation induced neurite outgrowth and PGD2 elicited neurite retraction, although we failed to detect transcripts for DP1 and CRTH2. Such an effect of PGD2 was efficiently mimicked by its metabolite, 15-deoxy-Δ(12,14)-prostaglandin J2...
February 19, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/26808004/target-oriented-therapy-emerging-drugs-for-atopic-dermatitis
#20
Felix Lauffer, Johannes Ring
INTRODUCTION: Atopic dermatitis (AD) is a chronic inflammatory skin disease with a life-time prevalence of 10 - 20% in western countries. Patients suffer from stigmatizing eczematous skin lesions, persisting itch and sleep disorders. Starting usually in early childhood the course of AD is heterogeneous. While most frequently AD disappears before adolescence, about 30% of patients show a chronic persisting course. There is an urgent need for new therapeutic options as until now, specific drugs are missing...
2016: Expert Opinion on Emerging Drugs
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