ArticleBritish journal of pharmacology2006
Biological properties of a specific Galpha q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 65 citations in OpenAlex.
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- Anti-Inflammatory and Antiplatelet Interactions on PAF and ADP Pathways of NSAIDs, Analgesic and Antihypertensive Drugs for Cardioprotection-In Vitro Assessment in Human Platelets.Medicina (Kaunas, Lithuania) · 2025Article
- Gαq/11 aggravates acute lung injury in mice by promoting endoplasmic reticulum stress-mediated NETosis.Molecular medicine (Cambridge, Mass.) · 2025Article
- How Protein Depletion Balances Thrombosis and Bleeding Risk in the Context of Platelet's Activatory and Negative Signaling.International journal of molecular sciences · 2024Review
- L-asparaginase induces IP3R-mediated ER CaCell death discovery · 2024Article
- Lysophosphatidic Acid Receptor 3 (LPA3): Signaling and Phosphorylation Sites.International journal of molecular sciences · 2024Article
- Lidocaine induces apoptosis in head and neck squamous cell carcinoma through activation of bitter taste receptor T2R14.Cell reports · 2023Article
- TMEM16A activation for the fast block to polyspermy in the African clawed frog does not require conventional activation of egg PLCs.The Journal of general physiology · 2023Article
- Somatic and terminal CB1 receptors are differentially coupled to voltage-gated sodium channels in neocortical neurons.Cell reports · 2023Article
- Exploring pharmacological inhibition of GBritish journal of pharmacology · 2022Article
- Gαq Is the Specific Mediator of PAR-1 Transactivation of Kinase Receptors in Vascular Smooth Muscle Cells.International journal of molecular sciences · 2022Article
- Review
- Targeting Oncogenic GαCancers · 2021Review
- Receptor-specific CaiScience · 2021Article
- Combined Inhibition of GαClinical cancer research : an official journal of the American Association for Cancer Research · 2021Article
- Functional evidence for biased inhibition of G protein signaling by YM-254890 in human coronary artery endothelial cells.European journal of pharmacology · 2021Article
- Natriuretic peptide receptor-C-mediated attenuation of vascular smooth muscle cell hypertrophy involves Gqα/PLCβ1 proteins and ROS-associated signaling.Pharmacology research & perspectives · 2018Article
- Signaling properties of the human chemokine receptors CXCR4 and CXCR7 by cellular electric impedance measurements.PloS one · 2017Article
- Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors.Nature chemistry · 2016Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1 The effects of YM-254890, a specific Galpha(q/11) inhibitor, on platelet functions, thrombus formation under high-shear rate condition and femoral artery thrombosis in cynomolgus monkeys were investigated. 2 YM-254890 concentration dependently inhibited ADP-induced intracellular Ca(2+) elevation, with an IC(50) value of 0.92+/-0.28 microM. 3 P-selectin expression induced by ADP or thrombin receptor agonist peptide (TRAP) was strongly inhibited by YM-254890, with IC(50) values of 0.51+/-0.02 and 0.16+/-0.08 microM, respectively. 4 YM-254890 had no effect on the binding of fibrinogen to purified GPIIb/IIIa, but strongly inhibited binding to TRAP-stimulated washed platelets. 5 YM-254890 completely inhibited platelet shape change induced by ADP, but not that induced by collagen, TRAP, arachidonic acid, U46619 or A23187. 6 YM-254890 attenuated ADP-, collagen-, TRAP-, arachidonic acid- and U46619-induced platelet aggregation with IC(50) values of <1 microM, whereas it had no effect on phorbol 12-myristate 13-acetate-, ristocetin-, thapsigargin- or A23187-induced platelet aggregation. 7 High-shear stress-induced platelet aggregation and platelet-rich thrombus formation on a collagen surface under high-shear flow conditions were concentration dependently inhibited by YM-254890. 8 The antithrombotic effect of YM-254890 was evaluated in a model of cyclic flow reductions in the femoral artery of cynomolgus monkeys. The intravenous bolus injection of YM-254890 dose dependently inhibited recurrent thrombosis without affecting systemic blood pressure or prolonging template bleeding time. 9 YM-254890 is a useful tool for investigating Galpha(q/11)-coupled receptor signaling and the physiological roles of Galpha(q/11).
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