Recombinant Human PTGIR protein

The prostacyclin receptor (PTGIR), also known as the prostaglandin I2 receptor or IP receptor, is a G protein-coupled receptor (GPCR) that plays a critical role in cardiovascular homeostasis, inflammation, and pain regulation. It primarily binds prostacyclin (PGI2), a potent vasodilator and platelet aggregation inhibitor produced by vascular endothelial cells. Upon activation, PTGIR couples with Gαs proteins, triggering intracellular cAMP signaling pathways that mediate its anti-thrombotic, anti-inflammatory, and vasoprotective effects. Dysregulation of PTGIR signaling has been implicated in cardiovascular diseases, pulmonary hypertension, and inflammatory disorders.

Recombinant PTGIR protein refers to the receptor protein artificially produced using recombinant DNA technology, typically expressed in mammalian, insect, or bacterial cell systems. This engineered protein retains the structural and functional characteristics of native PTGIR, enabling researchers to study its ligand-binding properties, signaling mechanisms, and interactions with drugs or therapeutic candidates. Mammalian expression systems (e.g., HEK293 cells) are often preferred for producing properly folded, post-translationally modified PTGIR suitable for pharmacological assays.

The development of recombinant PTGIR has advanced drug discovery efforts, particularly for therapies targeting thrombosis and pulmonary arterial hypertension. It facilitates high-throughput screening of receptor agonists/antagonists and structural studies using techniques like cryo-EM or X-ray crystallography. Current research focuses on understanding receptor desensitization mechanisms and designing biased ligands that selectively activate beneficial signaling pathways while minimizing side effects. As a therapeutic target, PTGIR continues to offer potential for treating conditions where vascular function and platelet activity are compromised.