Modern drugs and diagnostics overcome the mentioned handicaps.
Whereas old drugs enter the cells by diffusion, the transfer of nucleic acid drugs across cell membrane is very poor and insufficient. The differentiation between tumorigenic and the surrounding healthy tissue is hardly possible. “Old fashioned” drugs are highly active, but their lack of specificity and sensitivity needs high doses of application correlating with adverse reactions. Keywords: Click Chemistry, Diels Alder Reactioninverse (DARinv), local concentration, Peptide Nucleic Acid (PNA), PNA building block functionalization, Sustainable Pharmacy Introduction It is important to point out that this technology is not restricted to ligation of medicament material it is also a candidate to develop new and highly efficient active compounds for a “sustainable pharmacy”.
This allows local drug concentrations sufficient for imaging and therapy and simultaneously a reduction of the application doses. The high chemical stability and the ease of synthesis qualify these polyamide building blocks as favourites for intracellular delivery and targeting applications. These newly developed derivatives allow independent multi-ligations of multi-faceted components by use of the inverse Diels Alder technology. Here we demonstrate that the replacement of nucleobases with PNA by functional molecules harbouring either a dienophile or a diene reactivity is feasible and confers all new options for functionalization. In the near future personalized medicine with nucleic acids will play a key role in molecular diagnostics and therapy, which require new properties of the nucleic acids, like stability against enzymatic degradation. Select the file that you have just downloaded and select import option Reference Manager (RIS).
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Available fromĬlick on Go to download the file. Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers. Pipkorn R, Wiessler M, Waldeck W, Lorenz P, Muehlhausen U, Fleischhacker H, Koch M, Braun K.
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