Endothelin (endothelin, ET) exists not only in vascular endothelium, is also widely present in various tissues and cells, is an important factor in regulating cardiovascular function, based on the maintenance of vascular tone and homeostasis plays an important role in the cardiovascular system. It is a polypeptide composed of 21 amino acids, a molecular weight of 2400D, N terminal position of the two cysteine disulfide to connect 1-15,3-11, C is the number of hydrophobic amino terminal residues. N-terminal structure determines its receptor affinity, C-terminal receptor binding to determine their position. ET-1 and two isomers of the family that ET-2, ET-3, the difference is the individual amino acid residues play a major role in the cardiovascular is ET-1 (Endothelin 1). Endothelial cells are stimulated synthesis and release of ET-1, which is mainly regulated at the transcriptional level, stimulating ET-1 synthesis include: epinephrine, thromboxane, vasopressin, angiotensin, insulin, cytokines, and vascular wall shear force and the pressure change and the physico-chemical factors such as hypoxia, ET-1 stimulation of the synthesis process requires a Ca2 (-dependent protein kinase C (PKC) involved. inhibition of ET-1 synthesis factors: NO, PGI2, Atrial natriuretic peptide and heparin. ET-1 in plasma half-life is very short (<5min), quickly binds to receptors on the organization, its clear position mainly in the lungs and kidney, ET-degrading enzymes will soon be decomposed .
Role: endothelin (Endothelin, ET) is a Japanese scholar Yanagisawa, etc. from cultured porcine aortic endothelial cells, a kind of isolated and purified by a 21 amino acid residues of the peptide, endothelin is by far the most powerful vasoconstrictor known substances, their duration of action lasting, not for receptors, H1 receptors and 5-HT receptor antagonist antagonist, may be isoproterenol, atrial natriuretic peptide and calcitonin gene-related peptide hormone suppression. Thus, endothelin is an endogenous vasoconstrictor long-acting regulatory factors. Endothelin there is a strong positive inotropic effect and vasoconstrictor reflex rise of blood pressure effects can also cause heart suppression, resulting in cardiac insufficiency. But also induced myocardial cell sugar overload, arrhythmias, and myocardial energy metabolism. Currently a large number of studies have shown hinder severe angina, AMI, myocardial 1 / R injury, percutaneous transluminal angioplasty ET synthesis and release of the body to increase significantly hinder, or vascular reactivity for ET hyperthyroidism, are likely to promote the development of the pathological process. The application of ET or ET antagonist antibody may be ischemic heart disease prevention.
Impact: The discovery of endothelin people on endothelial cells to further deepen the understanding that the endothelium is not only a semi-permeable membrane to maintain blood flow and exchange of material, is also a specialized regulatory organization, plays a signal receiving, processing and re-export of role for the maintenance of homeostasis plays an important regulatory role in circulation. Studies have shown that tissue hypoxia, oxidative metabolism can be enhanced and increased levels of catecholamine stimulation of endothelin original transcription. Angiotensin can promote the release of endothelin. In the heart and blood vessels have extensive endothelin receptors, endothelin receptor binding and tissue corresponding to activate the second information cGMP, secondary to increased levels of inositol triphosphate-induced increase in intracellular calcium, and exerts its biological effects .
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