Target intelligence / Profile preview

Thromboxane A2 receptor (TBXA2R)

Target
TBXA2R
Molecular classification
G protein-coupled receptor, Enzyme, Cytochrome P450
01

Overview

The Thromboxane A2 (TXA2) pathway is a critical signaling cascade in cardiovascular physiology, primarily mediated by the enzyme Thromboxane A synthase (TBXAS1) and the Thromboxane A2 receptor (TBXA2R, also known as the TP receptor) (MedlinePlus, Wikipedia). TBXAS1 converts prostaglandin H2 into TXA2, a potent but short-lived lipid mediator that induces platelet aggregation and vascular smooth muscle contraction (NIH, irjpl.org). These effects are executed through the activation of the TP receptor, a G protein-coupled receptor (GPCR) expressed on platelets and vascular cells (ResearchGate, Patsnap). Dysregulation of this pathway is strongly linked to atherothrombotic events, including myocardial infarction and stroke, as well as inflammatory conditions and cancer progression (NIH, Frontiers). Pharmacological modulation of the pathway includes the use of aspirin to inhibit TXA2 synthesis, specific thromboxane synthase inhibitors like ozagrel, and TP receptor antagonists like ramatroban, which aim to prevent pathological thrombosis while minimizing bleeding risks (DrOracle, NIH).

Other names
Thromboxane A2 pathway componentsTP receptorThromboxane prostanoid receptorTXA2 receptorThromboxane A synthase 1TBXAS1TXASCYP5A1BDPLT13BDPLT14
02

Mechanism of action

Inhibition of Thromboxane A synthase (TBXAS1) to prevent TXA2 synthesis; Antagonism of the Thromboxane A2 receptor (TBXA2R) to block TXA2-mediated signaling; Irreversible inhibition of Cyclooxygenase-1 (COX-1) to reduce the precursor prostaglandin H2.

03

Biological functions

Platelet aggregationVasoconstrictionHemostasisSignal transductionInflammationAngiogenesisSmooth muscle contraction
04

Disease associations

Cardiovascular diseaseStrokeMyocardial infarctionAtherosclerosisAsthmaCancerGhosal hematodiaphyseal dysplasia
05

Safety considerations

Increased bleeding riskGastrointestinal toxicityThromboxane escape (activation of TP receptor by aspirin-insensitive isoprostanes)
06

Interacting drugs

Aspirin

7 more in the full profile.

07

Biomarkers

Serum Thromboxane B2 (TXB2)Urinary 11-dehydro-thromboxane B2Arachidonic acid-induced platelet aggregation

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