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

28 May 2014

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.

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).