ArticleBritish journal of pharmacology2008
Identification and pharmacological characterization of the prostaglandin FP receptor and FP receptor variant complexes.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed, 96 citations in OpenAlex.
- Comparison of efficacy of four prostaglandin analogues by bilateral treatment in healthy subjects.Japanese journal of ophthalmology · 2012Trial
- New role for the anandamide metabolite prostaglandin FJournal of lipid research · 2023Article
- Genotype and Phenotype Influence the Personal Response to Prostaglandin Analogues and Beta-Blockers in Spanish Glaucoma and Ocular Hypertension Patients.International journal of molecular sciences · 2023Article
- A Review of Prostanoid Receptors: Expression, Characterization, Regulation, and Mechanism of Action.Journal of cell communication and signaling · 2021Review
- Deletion of the gene encoding prostamide/prostaglandin F synthase reveals an important role in regulating intraocular pressure.Prostaglandins, leukotrienes, and essential fatty acids · 2021Article
- Prostaglandin F2α agonist-induced suppression of 3T3-L1 cell adipogenesis affects spatial formation of extra-cellular matrix.Scientific reports · 2020Article
- Matrix Metalloproteinases and Glaucoma Treatment.Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics · 2020Review
- Cannabinoids and the expanded endocannabinoid system in neurological disorders.Nature reviews. Neurology · 2020Review
- Druggable Targets in Endocannabinoid Signaling.Advances in experimental medicine and biology · 2020Review
- The Effect of Prostaglandin Analogue Bimatoprost on Thyroid-Associated Orbitopathy.Investigative ophthalmology & visual science · 2018Article
- New approaches and challenges to targeting the endocannabinoid system.Nature reviews. Drug discovery · 2018Review
- Ocular hypotensive effects of prostaglandin analogs in Japanese patients with normal-tension glaucoma: a literature review.Clinical ophthalmology (Auckland, N.Z.) · 2018Review
- The Endocannabinoid System as a Therapeutic Target in Glaucoma.Neural plasticity · 2016Review
- 4'-O-methylhonokiol increases levels of 2-arachidonoyl glycerol in mouse brain via selective inhibition of its COX-2-mediated oxygenation.Journal of neuroinflammation · 2015Article
- Fixed-combination treatments for intraocular hypertension in Chinese patients - focus on bimatoprost-timolol.Drug design, development and therapy · 2015Review
- Substrate-selective COX-2 inhibition as a novel strategy for therapeutic endocannabinoid augmentation.Trends in pharmacological sciences · 2014Review
- Prostamide F(2) α receptor antagonism combined with inhibition of FAAH may block the pro-inflammatory mediators formed following selective FAAH inhibition.British journal of pharmacology · 2014Article
- The impact of timolol maleate on the ocular tolerability of fixed-combination glaucoma therapies.Clinical ophthalmology (Auckland, N.Z.) · 2014Review
- Bimatoprost-loaded ocular inserts as sustained release drug delivery systems for glaucoma treatment: in vitro and in vivo evaluation.PloS one · 2014Article
- Anandamide-derived prostamide F2α negatively regulates adipogenesis.The Journal of biological chemistry · 2013Article
Corrections and comments
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Authors and funding
15 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeA prostamide analogue, bimatoprost, has been shown to be effective in reducing intraocular pressure, but its precise mechanism of action remains unclear. Hence, to elucidate the molecular mechanisms of this effect of bimatoprost, we focused on pharmacologically characterizing prostaglandin FP receptor (FP) and FP receptor variant (altFP) complexes. EXPERIMENTAL APPROACH: FP receptor mRNA variants were identified by reverse transcription-polymerase chain reaction. The FP-altFP4 heterodimers were established in HEK293/EBNA cells co-expressing FP and altFP4 receptor variants. A fluorometric imaging plate reader was used to study Ca2+ mobilization. Upregulation of cysteine-rich angiogenic protein 61 (Cyr61) mRNA was measured by Northern blot analysis, and phosphorylation of myosin light chain (MLC) by western analysis. KEY
resultsSix splicing variants of FP receptor mRNA were identified in human ocular tissues. Immunoprecipitation confirmed that the FP receptor is dimerized with altFP4 receptors in HEK293/EBNA cells co-expressing FP and altFP4 receptors. In the studies of the kinetic profile for Ca2+ mobilization, prostaglandin F2alpha (PGF2alpha) elicited a rapid increase in intracellular Ca2+ followed by a steady state phase. In contrast, bimatoprost elicited an immediate increase in intracellular Ca2+ followed by a second phase. The prostamide antagonist, AGN211335, selectively and dose-dependently inhibited the bimatoprost-initiated second phase of Ca2+ mobilization, Cyr61 mRNA upregulation and MLC phosphorylation, but did not block the action of PGF2alpha. CONCLUSION AND IMPLICATIONS: Bimatoprost lacks effects on the FP receptor but may interact with the FP-altFP receptor heterodimer to induce alterations in second messenger signalling. Hence, FP-altFP complexes may represent the underlying basis of bimatoprost pharmacology.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.