Parstatin (human)

Product Name:Parstatin (human)

CAS No:1065755-99-8

Purity:95%

Molar Mass:4467.29

Chemical Formula:C191H330N64O53S3

Storage:Store at -20 degrees Celsius

Sequence:MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPR

Application:Parstatin is a peptide derived from the parathyroid hormone (PTH) precursor protein. It consists of the N-terminal portion of the parathyroid hormone, and it functions as an antagonist of the PTH receptor. In humans, parstatin plays a role in regulating bone metabolism and calcium homeostasis by inhibiting the action of PTH. Research on parstatin focuses on its potential therapeutic applications in treating bone disorders such as osteoporosis and hyperparathyroidism, as well as its role in regulating calcium levels and overall bone health.

Current Research:

Parstatin is a 41-amino acid peptide generated from the proteolytic cleavage of protease-activated receptor 1 (PAR1) upon thrombin activation. This N-terminal fragment has garnered significant interest due to its diverse biological activities, particularly its anti-angiogenic and cardioprotective properties.
Biological Activities
Anti-Angiogenic Effects: Parstatin effectively inhibits endothelial cell migration and proliferation, with an IC?? of approximately 3 ??M. It induces cell cycle arrest and promotes caspase-3 activation, leading to apoptosis in vitro. These actions contribute to its capacity to suppress angiogenesis, the formation of new blood vessels, which is crucial in processes like tumor growth and wound healing.
Cardioprotective Effects: In vivo studies have demonstrated that parstatin administration prior to ischemic events confers immediate cardioprotection. This effect is mediated through the activation of Gi-protein pathways, including p38 MAPK, ERK1/2, nitric oxide synthase (NOS), and ATP-sensitive potassium (K_ATP) channels. Parstatin exerts its protective effects on both cardiomyocytes and the coronary circulation, suggesting potential therapeutic applications in ischemia-reperfusion injuries.
Mechanism of Action
Upon thrombin activation, PAR1 undergoes cleavage, releasing parstatin. This peptide can penetrate cells and modulate various signaling pathways. Its anti-angiogenic activity is attributed to the inhibition of endothelial cell functions essential for new vessel formation. The cardioprotective effects involve the recruitment of intracellular signaling cascades that enhance cell survival and function during ischemic stress.
Research Applications
Parstatin serves as a valuable tool in biomedical research, particularly in:
Angiogenesis Studies: Investigating the mechanisms underlying blood vessel formation and identifying potential therapeutic targets for diseases characterized by abnormal angiogenesis, such as cancer and diabetic retinopathy.
Cardiovascular Research: Exploring protective strategies against ischemic heart diseases and understanding the molecular pathways involved in cardioprotection.
Conclusion
Parstatin, derived from PAR1 activation, exhibits significant anti-angiogenic and cardioprotective properties. Its ability to modulate critical cellular processes positions it as a promising candidate for therapeutic development in conditions involving aberrant angiogenesis and ischemic injuries. Ongoing research continues to elucidate its mechanisms of action and potential clinical applications.

Reference:

Zania, P., Gourni, D., Aplin, A. C., Nicosia, R. F., Flordellis, C. S., Maragoudakis, M. E., & Tsopanoglou, N. E. (2009). Parstatin, the cleaved peptide on proteinase-activated receptor 1 activation, is a potent inhibitor of angiogenesis. Journal of Pharmacology and Experimental Therapeutics, 328(2), 378-389.