Last update 01 Nov 2024

CRTH2 x DP1

Last update 01 Nov 2024

Basic Info

Related Targets

CRTH2DP1

Drugs associated with CRTH2 x DP1

AMG-009

Target

CRTH2 x DP1

Mechanism

CRTH2 antagonists [+1]

Active Org.-

Originator Org.

Amgen, Inc.

Active Indication-

Inactive Indication

Asthma [+1]

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with CRTH2 x DP1

100 Translational Medicine associated with CRTH2 x DP1

0 Patents (Medical) associated with CRTH2 x DP1

Literatures (Medical) associated with CRTH2 x DP1

01 Aug 2023·Theriogenology

miR-665 overexpression inhibits the apoptosis of luteal cells in small ruminants suppressing HPGDS

Article

Author: Fu, Lin ; Li, Qianyong ; Zhang, Dezhi ; Zhou, Peng ; Yang, Heng ; Li, Licai

Evidence has shown that microRNA-665 (miR-665) is highly expressed in the mid-luteal phase compared with the early and end-luteal phase of the corpus luteum (CL) life cycle.However, whether miR-665 is a pos. regulator of the life span of the CL is still unknown.The objective of this study is to explore the effect of miR-665 on the structural luteolysis in the ovarian CL.In this study, the targeting relationship between miR-665 and hematopoietic prostaglandin synthase (HPGDS) was firstly verified by dual luciferase reporter assay.Then, quant. real-time PCR (qRT-PCR) was used to detect the expression of miR-665 and HPGDS in luteal cells.Following miR-665 overexpression, the apoptosis rate of the luteal cells was determined using flow cytometry; B-cell lymphoma-2 (BCL-2) and caspase-3 mRNA and protein were measured using qRT-PCR and Western blot (WB) anal.Finally, the DP1 and CRTH2 receptors of PGD2, a synthetic product of HPGDS, were localized using immunofluorescence.Results confirmed that HPGDS was a direct target gene of miR-665, and miR-665 expression was neg. correlated with HPGDS mRNA expression in luteal cells.Meanwhile, after miR-665 was overexpressed, the apoptotic rate of the luteal cells showed a significant decrease (P < 0.05) and this was accompanied by elevated expression levels of anti-apoptotic factor BCL-2 mRNA and protein and decreased expression levels of apoptotic factor caspase-3 mRNA and protein (P < 0.01).Moreover, the immune fluorescence staining results showed that the DP1 receptor was also significantly decreased (P < 0.05), but the CRTH2 receptor was significantly increased (P < 0.05) in luteal cells.Overall, these results indicate that miR-665 reduces the apoptosis of luteal cells via inhibiting caspase-3 expression and promoting BCL-2 expression, and the biol. function of miR-665 may be attributed to its target gene HPGDS which regulates the balance of DP1 and CRTH2 receptors expression in luteal cells.As a consequence, this study suggests that miR-665 might be a pos. regulator of the life span of the CL rather than destroy the integrity of CL in small ruminants.

18 Mar 2022·Clinical ScienceQ2 · MEDICINE

Role of prostaglandin D2 receptors in the pathogenesis of abdominal aortic aneurysm formation

Q2 · MEDICINE

Article

Author: Kim, Ha Won ; Huo, Yuqing ; Fujise, Ken ; Ushio-Fukai, Masuko ; Fukai, Tohru ; Annex, Brian H. ; Fulton, David J. ; Blomkalns, Andra L. ; Guha, Avirup ; Horimatsu, Tetsuo ; Weintraub, Neal L. ; Winkler, Michael A. ; Ogbi, Mourad ; Young, Lufei ; Long, Xiaochun ; Benson, Tyler W. ; Lee, Richard ; Agarwal, Gautam

AbstractProstaglandin D2 (PGD2) released from immune cells or other cell types activates its receptors, D prostanoid receptor (DP)1 and 2 (DP1 and DP2), to promote inflammatory responses in allergic and lung diseases. Prostaglandin-mediated inflammation may also contribute to vascular diseases such as abdominal aortic aneurysm (AAA). However, the role of DP receptors in the pathogenesis of AAA has not been systematically investigated. In the present study, DP1-deficient mice and pharmacological inhibitors of either DP1 or DP2 were tested in two distinct mouse models of AAA formation: angiotensin II (AngII) infusion and calcium chloride (CaCl2) application. DP1-deficient mice [both heterozygous (DP1+/−) and homozygous (DP1−/−)] were protected against CaCl2-induced AAA formation, in conjunction with decreased matrix metallopeptidase (MMP) activity and adventitial inflammatory cell infiltration. In the AngII infusion model, DP1+/− mice, but not DP1−/− mice, exhibited reduced AAA formation. Interestingly, compensatory up-regulation of the DP2 receptor was detected in DP1−/− mice in response to AngII infusion, suggesting a potential role for DP2 receptors in AAA. Treatment with selective antagonists of DP1 (laropiprant) or DP2 (fevipiprant) protected against AAA formation, in conjunction with reduced elastin degradation and aortic inflammatory responses. In conclusion, PGD2 signaling contributes to AAA formation in mice, suggesting that antagonists of DP receptors, which have been extensively tested in allergic and lung diseases, may be promising candidates to ameliorate AAA.

26 Oct 2021·mBioQ1 · BIOLOGY

Differential Effects of Prostaglandin D ₂ Signaling on Macrophages and Microglia in Murine Coronavirus Encephalomyelitis

Q1 · BIOLOGY

ArticleOA

Author: Perlman, Stanley ; Verma, Abhishek Kumar ; Zheng, Jian ; Mack, Matthias ; Ginhoux, Florent

Current understanding about the roles of microglia versus macrophages in viral encephalitis is limited. We previously showed that the signaling of a single prostaglandin, PGD 2 , through its DP1 receptor on myeloid cells is critical for optimal immune responses in infected mice.

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