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Glen Report 36-22: New Products Spirocyclopropylene Bridged Nucleic Acids

Locked nucleic acid (LNA) is a popular bicyclic backbone that significantly increases duplex stability. A single substitution can increase melting temperatures by as much as 9 °C without sacrificing specificity,1 and as such, LNA is usually one of the first modifications that come to mind for increasing target affinity regardless of the application.  Since LNA was first described,2, 3 there have been many other similarly locked or bridged nucleic acid backbones that have been published such as S-constrained ethyl (cEt), ethylene-bridged nucleic acid (ENA) and more.4 Another example of bridged nucleic acid is the tricyclic spirocyclopropylene-bridged nucleic acid (scpBNA™).5

As described in the preceding article, scpBNA exhibits high binding affinity and excellent metabolic stability that reduces the number of phosphorothioate bonds required in the oligonucleotide sequence. In collaboration with Summit Pharmaceuticals as well as Luxna Biotech, we are happy to share that we are introducing the scpBNA phosphoramidites of 5-methyl-C and T (Figure 1) to give customers the opportunity to use this unique backbone in their applications. In the future, there are also plans to introduce the purine phosphoramidites. Please stay tuned!

Figure 1. scpBNA Pyrimidine Phosphoramidites

Figure 1. scpBNA Pyrimidine Phosphoramidites

IP Statement:

scpBNATM is a trademark owned by Luxna Biotech Co., Ltd. (Luxna).

scpBNATM phosphoramidites (Products) are protected by WO2015/125783A1, WO2020/204022A1 and their foreign patents/applications controlled by Luxna. 

Glen Research sells the Products under contract with Summit Pharmaceuticals International Corporation, which has the license from Luxna. The resale of the Products is prohibited. The Products can be used only for experimental or research use, and the uses of the Products, including processed products thereof, for any purposes other than experimental or research use is prohibited. The purchase of the Products does not grant any right for the Patents, except for experimental or research use. For any other use, the customer must obtain a license from Luxna ([email protected], +81-6-6170-1228).

References

  1. D.A. Braasch, and D.R. Corey, Chem Biol, 2001, 8, 1-7.
  2. S. Obika, et al., Tetrahedron Letters, 1997, 38, 8735-8738.
  3. S. K. Singh, A. A. Koshkin, J. Wengel, and P. Nielsen, Chemical Communications, 1998, 455-456.
  4. W.B. Wan, and P.P. Seth, J Med Chem, 2016, 59, 9645-9667.
  5. T. Yamaguchi, M. Horiba, and S. Obika, Chem Commun (Camb), 2015, 51, 9737-40.

Product Information

5-Me-C-scpBNA™-CE Phosphoramidite (10-2211-xx)

T-scpBNA™-CE Phosphoramidite (10-2230-xx)