SensoLyte« Green Glutaminyl Cyclase Activity Assay - Industry's First
SensoLyte Green Glutaminyl Cyclase Assay Kit

SensoLyte« Green Glutaminyl Cyclase Activity Assay Kit (Cat# AS-72230)

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Industry's First
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✓ Sensitive - detects as low as 1.5 ng/mL of active Glutaminyl Cyclase
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✓ Long wavelength, green fluorimetric assay kit (Ex/Em=490/520 nm) ľ minimal autofluorescence
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✓ Fluorescence signal proportional to enzyme activity
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✓ Convenient two-step homogeneous assay format
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✓ Assay can be completed in 1.5 hours
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✓ Validated with human and plant Glutaminyl Cyclase
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✓ Validated with human biological samples (Figure 2)
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✓ Adaptable to high throughput screening (HTS)
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inhibitor
Figure 1.1-Benzyl-Imidazole inhibition of Glutaminyl Cyclase activity measured with SensoLyte« Green Glutaminyl Cyclase Activity Assay Kit.
inhibition
Figure 2. Glutaminyl Cyclase Activity in Human Body Fluids. Human cerebrospinal fluid (CSF) and saliva were diluted 2.5-fold using assay buffer ▒Glutaminyl Cyclase inhibitor and were tested for the enzyme activity using SensoLyte« Green Glutaminyl Cyclase Assay Kit.

Product Catalog #

SensoLyte« Green Glutaminyl Cyclase Activity Assay *Fluorimetric*

AS-72230

AnaSpec is pleased to announce the release of the first commercially available 96-well format fluorimetric assay for measuring Glutaminyl Cyclase (QC) activity - the SensoLyte« Green Glutaminyl Cyclase Activity Assay Kit.

Glutaminyl cyclase (QC), an enzyme found in animals and plants, catalyzes the cyclization of N-terminal Glutamine, and to a lesser extent Glutamate, to pyroglutamate.1 This post-translational modification to pyroglutamate, present in many biologically active peptides and proteins, protects against degradation by aminopeptidases and in many cases determines functionality of protein or peptide.2-7

Pyroglutamate modification sometimes may lead to negative side effects. pGlu (or pE) modified β-amyloid peptides (pGlu-Aβ) aggregate much faster than non-pyroglutamic Aβ and form toxic oligomers that may damage neurons.8-10 CCL2 (monocyte chemoattractant protein 1, MCP-1), implicated in a number of diseases has in its mature form an N-terminal pGlu. This modification protects it against aminopeptidase degradation, and improves receptor activation and signal transduction in vitro.11 Increased levels of pE-CCL2 has been implicated in thyroid carcinoma proliferation and metastasis,12 and atherosclerosis,11 and other inflammatory disorders.11 Thus, Glutaminyl Cyclase (QC) inhibitors are attractive drug candidates.

inhibition
Glutaminyl
Figure 3. SensoLyte« Green Glutaminyl Cyclase Assay Principle.

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References:

  1. Schilling, S. et al. Biol Chem 389, 983 (2008).
  2. Kumar, A. et al. Curr Sci 102, 288 (2012).
  3. Castaldo, C. et al. PLOS One 8, 1 (2013).
  4. Booth, ER. et al. BMC Biol 2, 1 (2004).
  5. Schilling, S. et al. Biol. Chem 384, 1583 (2003).
  6. Huang, W-L. et al. J. Mol. Biol. 401, 374 (2010).
  7. Gontsarova, A. et al. Clin Chim Acta 389, 152 (2008).
  8. Sullivan, PC. et al. Neur Lett 505, 109 (2011).
  9. Wirths, O. et al. J Biol Chem 285, 41517 (2010).
  10. Hartlage-Rubsamen, M. et al. Acta Neuropathol 121, 705 (2011).
  11. Cynis, H. et al. EMBO Mol Med 3, 545 (2011).
  12. Kehlen, A. et al. Endocr Relat Cancer 20, 79 (2012).