Last update 01 Nov 2024

CysLT2

Last update 01 Nov 2024

Basic Info

Synonyms

CysLT(2), CYSLT2, CYSLT2R

+ [6]

Introduction

Receptor for cysteinyl leukotrienes. The response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. Stimulation by BAY u9773, a partial agonist, induces specific contractions of pulmonary veins and might also have an indirect role in the relaxation of the pulmonary vascular endothelium. The rank order of affinities for the leukotrienes is LTC4 = LTD4 >> LTE4.

Drugs associated with CysLT2

ONO-2050297

Target

CysLT1 x CysLT2

Mechanism

CysLT1 antagonists [+1]

Active Org.

Ono Pharmaceutical Co., Ltd.

Originator Org.

Ono Pharmaceutical Co., Ltd.

Active Indication-

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Gemilukast

Target

CysLT1 x CysLT2

Mechanism

CysLT1 antagonists [+1]

Active Org.-

Originator Org.

Ono Pharmaceutical Co., Ltd.

Active Indication-

Inactive Indication

Asthma [+1]

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with CysLT2

JPRN-jRCT2080222716 / Unknown statusPhase 2

ONO-6950 Phase 2a study A multicenter, double-blind, randomized parallel-group study in patients with asthma.

Start Date14 Jan 2015

Sponsor / Collaborator

Ono Pharmaceutical Co., Ltd.

JPRN-JapicCTI-152768 / Unknown statusPhase 2

ONO-6950 Phase 2a study A multicenter, double-blind, randomized parallel-group study in patients with asthma.

Start Date01 Jan 2015

Sponsor / Collaborator

Ono Pharmaceutical Co., Ltd.

NCT01551147 / CompletedPhase 2

A Double-blind, Placebo-controlled, Three-way Crossover Study to Compare the Safety and Efficacy of 8 Days of Therapy With ONO-6950 Versus Placebo and Montelukast (Singulair®) on Asthmatic Responses and Airway Hypersensitivity Following Allergen Challenge in Patients With Asthma

The primary objectives are
to determine the effect of ONO-6950 200 mg QD versus placebo administered for 8 days on early asthmatic response (EAR) and late asthmatic response (LAR) induced by inhaled allergen
to determine the safety and tolerability of ONO-6950 200 mg QD administered for 8 days in patients with asthma
The secondary objectives are:
to compare the effect of ONO-6950 versus montelukast on the % decrease of FEV1 following allergen exposure, and
to determine the effect of ONO-6950 versus placebo and montelukast on allergen-induced airway hyperresponsiveness (AHR) as measured by methacholine challenge

Start Date01 Jun 2012

Sponsor / Collaborator

Ono Pharma USA, Inc.

[+1]

100 Clinical Results associated with CysLT2

100 Translational Medicine associated with CysLT2

0 Patents (Medical) associated with CysLT2

328

Literatures (Medical) associated with CysLT2

01 Dec 2024·Molecular and Biochemical Parasitology

Neuroprotective effects of CysLT2R antagonist on Angiostrongylus cantonensis-induced edema and meningoencephalitis

Article

Author: Lan, Kuang-Ping ; Lai, Shih-Chan ; Chen, Ke-Min

Cysteinyl leukotrienes (CysLTs) can induce a disruption of the blood-brain barrier (BBB), and this reaction is mediated by cysteinyl-leukotriene receptors. In this study, we used A. cantonensis-induced eosinophilic meningoencephalitis as a model to investigate whether the CysLT2 receptor involved in the pathogenesis of angiostrongyliasis meningoencephalitis. The present study provides evidence that the CysLT2 receptor antagonist HAMI3379 reduced the number of infiltrated eosinophils and brain edema in eosinophilic meningoencephalitis. Additionally, we found that HAMI3379 significantly decreased the protein levels of M1 polarisation markers (CD80, iNOS, IL-5 and TNF-α), increased the expression of M2 polarisation markers (CD206, IL-10 and TGF-β) both in vivo and in vitro. Matrix metalloproteinase-9, S100B, GFAP, fibronectin, and claudin-5 were markedly lower after HAMI3379 treatment. Therefore, HAMI3379 reduced the BBB dysfunction in angiostrongyliasis meningoencephalitis. We have identified microRNA-155 as a BBB dysfunction marker in eosinophilic meningoencephalitis. The results showed that microRNA-155 was 15-fold upregulated in eosinophilic meningoencephalitis and 20-fold upregulated after HAMI3379 treatment. Our results suggest that CysLT2R may be involved in A. cantonensis-induced brain edema and eosinophilic meningoencephalitis and that down-regulation of CysLT2R could be a novel and potential therapeutic strategy for the treatment of angiostrongyliasis meningoencephalitis.

07 Oct 2024·Annual Review of Pathology: Mechanisms of Disease

Cysteinyl Leukotrienes in Allergic Inflammation

Review

Author: Lee, Minkyu ; Boyce, Joshua A. ; Barrett, Nora A.

The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, are potent lipid mediators derived from arachidonic acid through the 5-lipoxygenase pathway. These mediators produce both inflammation and bronchoconstriction through three distinct G protein–coupled receptors (GPCRs)—CysLT1, CysLT2, and OXGR1 (also known as CysLT3 or GPR99). While CysLT-mediated functions in the effector phase of allergic inflammation and asthma have been established for some time, recent work has demonstrated novel roles for these mediators and their receptors in the induction and amplification of type 2 inflammation. Additionally, in vitro studies and murine models have uncovered diverse regulatory mechanisms that restrain or amplify CysLT receptor activation and CysLT receptor function. This review provides an overview of CysLT biosynthesis and its regulation, the molecular and functional pharmacology of CysLT receptors, and an overview of the established and emerging roles of CysLTs in asthma, aspirin-exacerbated respiratory disease, and type 2 inflammation.

01 Oct 2024·Brain, Behavior, & Immunity - Health

Autism likelihood in infants born to mothers with asthma is associated with blood inflammatory gene biomarkers in pregnancy

Article

Author: Lane, Alison E ; Karayanidis, Frini ; Baines, Katherine J. ; Campbell, Linda E. ; Murphy, Vanessa E ; Campbell, Linda E ; Woolard, Alix ; Mallise, Carly A ; Williams, Evan J. ; Collison, Adam M ; Robijn, Annelies L ; Baines, Katherine J ; Whalen, Olivia M. ; Murphy, Vanessa E. ; Gibson, Peter G ; Gibson, Peter G. ; Collison, Adam M. ; Whalen, Olivia M ; Robijn, Annelies L. ; Mallise, Carly A. ; Mattes, Joerg ; Lane, Alison E. ; Williams, Evan J

Mothers with asthma or atopy have a higher likelihood of having autistic children, with maternal immune activation in pregnancy implicated as a mechanism. This study aimed to determine, in a prospective cohort of mothers with asthma and their infants, whether inflammatory gene expression in pregnancy is associated with likelihood of future autism. Mothers with asthma were recruited to the Breathing for Life Trial. RNA was extracted from blood samples collected at mid-pregnancy. 300 ng total RNA was hybridized with the nCounter Human Inflammation gene expression panel (Nanostring Technologies, 249 inflammation-related genes). Parents completed the First Year Inventory (FYI) at 12-month follow-up, which assessed an infant's likelihood for autism across 2 behavioural domains: social communication and sensory regulation. A total score ≥19.2 indicated increased likelihood for future autism. Inflammatory gene expression was profiled from 24 mothers: four infants scored in the high autism likelihood range; 20 scored in the low autism likelihood range. Six inflammatory genes were differentially expressed and significantly up-regulated in the high autism likelihood group: CYSLTR2, NOX1, C1QA, CXCL10, C8A, IL23R. mRNA count significantly correlated with social communication FYI score for CYSLTR2 (Pearson r = 0.46, p = 0.024) and CXCL10 (r = 0.43, p = 0.036) and with sensory regulation score for ALOX5 (r = -0.43, p = 0.038) and MAFK (r = -0.46, p = 0.022). In this proof-of-concept study, inflammatory gene expression during pregnancy in mothers with asthma was associated with an infant's likelihood of future autism as well as scores relating to social communication and sensory regulation.

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