Anaspec has announced the release of Hilyte Fluor 488 and 5-FAM labelled Endothelin peptides (human, bovine, porcine, rat).
Endothelins (ET) are highly potent vasoconstrictor proteins distributed throughout all areas of the body and are implicated in a number of conditions and diseases.
Members of the Endothelin family of peptides consist of pre-pro-endothelin-1, a biologically inactive precursor form cleaved by furin covertase to produce Big Endothelin-1 (Big ET-1), which is cleaved again by endothelin converting enzyme (ECE) between Trp-21 and Val-22 to yield the active ET-1 (1- 21).
Alternatively, pulmonary chymase is also capable of generating ET-1 (1-31) by cleaving the Tyr31 - Gly32 bond of big ET-1.
Isoforms include ET-2, ET-3 and ET-4.
All have two disulphide bonds that hold them in a conical spiral shape.
In addition to their vasoconstrictive properties, endothelins have inotropic and mitogenic properties.
They influence salt and water balance, affect intracellular Ca2+ concentrations and signal transduction cascades, contract non-vascular smooth muscle, alter central and peripheral sympathetic activity and stimulate the renin-angiotensin-aldosterone system.
ETs are normally kept at stable levels in healthy individuals, but can become over expressed, leading to high blood pressure, kidney disease and numerous cardiovascular diseases such as pulmonary hypertension, cardiac hypertrophy, myocardial infarction, heart failure and cerebral vasospasm.
ET disregulation is also a key component of tumorigenesis in several types of cancer.
Fluorescently labelled endothelins have various applications in ET-related disease research.
They are utilised as probes in visualising intracellular processes and molecular interactions between ET-1 and potential ET-antagonists or inhibitors at the cellular level.
They are also used for localising and monitoring ECE activity and ET-receptor binding affinity via fluorescence fluctuation spectroscopy.
Specific ET isoform binding sites throughout the body may be studied using labelled ET.
In addition, flow cytometry is used in combination with labelled ET to assay ET - receptor expression during different periods of the cell cycle and in vitro imaging of ET activity is capable with fluorescent ET.
Overall, these peptides offer a wide range of approaches to further studying ET function and ET-related mechanisms.
