Angiotensin II converting enzyme (ACE2), a carboxypeptidase, is part of the renin-angiotensin system (RAS) that controls regulation of blood pressure by cleaving the C-terminal dipeptide of Angiotensin II to convert it into Angiotensin 1-7. It also cleaves Angiotensin I to produce Ang 1-9, of unknown function. ACE2 is a receptor of human coronaviruses, such as SARS and HCoV-NL63. It is expressed on the vascular endothelial cells of heart and kidney. The inhibitors of ACE2 could be able to regulate hypertension by changing vascular permeability. Screening for small molecule and peptide inhibitors might also help in finding treatment for coronavirus mediated infection.
Features and Benefits
The Angiotensin II Converting Enzyme (ACE2) Inhibitor Screening Kit is compatible with high-throughput handling systems.
Suitability
The kit is suitable for Screening/characterizing inhibitors/ligands of ACE2.
Principle
The Angiotensin II Converting Enzyme (ACE2) Inhibitor Screening Kit can be used to screen for potent inhibitors of ACE2 activity, it utilizes the ability of an active ACE2 to cleave a synthetic MCA based peptide substrate to release a free fluorophore. The released MCA can be easily quantified using a fluorescence microplate reader. In the presence of an ACE2 specific inhibitor, the enzyme loses its peptidase activity which results in decrease of fluorescence intensity.
Other Notes
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1. For fluorescence measurements, it is supposed to use White flat-bottom 96-well plates or Black flat-bottom 96-well plates?
2. What are the considerations for selecting two time points (T1 & T2) in the linear range of the plot?
1 answer
Technical Support
·2 years ago
This kit requires the use of white flat-bottom 96-well plates. T1 and T2 values are solely dependent on the assay and plate set up. The T1 and T2 should be chosen within the linear range of the kinetic plot of the standard or samples. See the link below for a reference that may be useful. https://pubmed.ncbi.nlm.nih.gov/36009234/
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