Understanding and use of Gorelatide

introduction

Gorelatide, also known as n-acetyl-serine – aspartic acid – proline – proline -(N-Acetyl-Ser-Asp-Lys-Pro), abbreviated as Ac-S-D-K-P, is an endogenous tetrapeptide, nitrogen end acetylation, widely distributed in various tissues and body fluids in the body. This tetrapeptide is released by prolyl oligopeptidase (POP), which is mainly caused by its precursor thymosin. The concentration in the blood is usually on the nanomole scale.

okinetics

According to the pharmacokinetic study of Gorelatide, after intravenous injection, Gorelatide rapidly degrades with a half-life of only 4 ~ 5min. Gorelatide is cleared from human plasma by two mechanisms: Angiotensin-converting enzyme (ACE) -guided hydrolysis; Glomerular filtration. The hydrolysis of angiotensin converting enzyme (ACE) is the main pathway of gorelatide metabolism.

Biological activity

Gorelatide is a kind of multifunctional physiological regulatory factor with various biological activities. It was earlier reported that Gorelatide could prevent the entry of the original hematopoietic stem cells into the S phase and make them stationary in the G0 phase, inhibiting the activity of the hematopoietic stem cells. It was subsequently found that Gorelatide can improve epidermal replanting capacity by promoting blood vessel formation and accelerate wound healing in damaged vascularized epidermal grafts. Gorelatide can inhibit the differentiation of bone marrow stem cells stimulated by MGM into macrophages, thus playing an anti-inflammatory role. Gorelatide has recently been found to inhibit the proliferation of a variety of cells.

use

As a polypeptide organic matter, Gorelatide can be used as a drug raw material.


Post time: Apr-26-2023