专肽生物_定制多肽合成服务_多肽合成定制服务_多肽合成厂家_多肽合成公司

功能性人凝血酶受体的克隆和表达揭示了一种具有七个跨膜结构域和一个大的细胞外氨基末端延伸的蛋白质。凝血酶在这个延伸范围内裂解，从而产生一个新的受体氨基末端，该末端起到束缚配体的作用并激活受体。已经发现模拟这种新的氨基末端的14个氨基酸的肽是有效的凝血酶受体活化剂以及血小板活化的有效激动剂。

Cloning and expression of a functional human thrombin receptor have revealed a protein with seven transmembrane domains and a large extracellular amino-terminal extension. Thrombin cleaves within this extension, thereby creating a new receptor amino-terminus that functions as a tethered ligand and activates the receptor. A 14-amino acid peptide mimicking this new amino-terminus has been found to be a potent thrombin receptor activator as well as an effective agonist for platelet activation.

"Hypertension is a common condition that affects millions of people worldwide. It is characterized by an elevated blood pressure and the subsequent damage to the heart, kidneys, and other tissues. Metyrapone is a drug that inhibits the synthesis of corticosteroids from cholesterol in the adrenal glands. It was shown to reduce blood pressure in vivo by blocking the formation of cytosolic calcium and subsequent release of vasopressin. The use of metyrapone as a hypertension treatment has been limited due to its side effects on the liver. A new model system using basic fibroblasts (BF) instead of liver cells has been developed to study this drugs effects on hypertension without causing liver lesions. This model has proven successful for other drugs with similar biological properties, such as Hytrinol, which also blocks corticosteroid synthesis from cholesterol but does not cause liver lesions. The BF system can be used for testing new drugs that are selective for PAR1 receptors, which are"