AnaSpec Launches Industry’s First Fluorimetric Assay for Measuring Glutaminyl Cyclase Activity

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 (PTM) 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. The aggregation of β-amyloid plaques is one of the hallmarks of Alzheimer’s Disease (AD).[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.

References
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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).