Building Blocks for the SPPS of FRET-based fluorogenic protease substrates

Building Blocks for the SPPS of FRET-based fluorogenic protease substrates

Published on 30/08/2016

The classic FRET pair EDANS and DABCYL is now available linked to Fmoc amino acid building blocks that can be readily used in SPPS. Conveniently synthesize your own custom protease substrates!

Building Blocks for the SPPS of FRET-based fluorogenic protease substrates

Traditionally, fluorogenic protease substrates for the screening of protease activity are prepared by peptide synthesis and subsequent regioselective deprotection and functionalization with a fluorophore/quencher pair such as EDANS and DABSYL. For your convenience, we now offer a glutamate and a lysine building block functionalized with EDANS and DABSYL, respectively. Those building blocks are suitable for peptide synthesis using the Fmoc strategy and will allow you to prepare custom protease substrates without additional tedious and yield-reducing functionalization steps post-SPPS.

Screening of protease activity using FRET-based fluorogenic protease substrates

→ Visit our Webshop to find various other Dyes and Fluorescent Labels, as well a selection of Substrates & Inhibitors

References

  • Enzymatic activity characterization of SARS coronavirus 3C-like protease by fluorescence resonance energy transfer technique; S. Chen, L.-l. Chen, H.-b. Luo, T. Sun, J. Chen, F. Ye, J.-h. Cai, J.-k. Shen, X. Shen and H.-l. Jiang; Acta Pharmacol Sin 2005; 26: 99-106.
  • Synthesis and evaluation of fluorescent probes for the detection of calpain activity; S. Mittoo, L. E. Sundstrom and M. Bradley; Analytical Biochemistry 2003; 319: 234-238. doi:http://dx.doi.org/10.1016/S0003-2697(03)00324-5
  • A general method for the preparation of internally quenched fluorogenic protease substrates using solid-phase peptide synthesis; L. L. Maggiora, C. W. Smith and Z. Y. Zhang; Journal of Medicinal Chemistry 1992; 35: 3727-3730. doi:10.1021/jm00099a001
  • Novel fluorogenic substrates for assaying retroviral proteases by resonance energy transfer; E. Matayoshi, G. Wang, G. Krafft and J. Erickson; Science 1990; 247: 954-958. doi:10.1126/science.2106161
  • Design and synthesis of new fluorogenic HIV protease substrates based on resonance energy transfer; G. T. Wang, E. Matayoshi, H. Jan Huffaker and G. A. Krafft; Tetrahedron letters 1990; 31: 6493-6496. doi:http://dx.doi.org/10.1016/S0040-4039(00)97099-0