TMZ-BioShuttle, an Exemplary Drug Reformulation by Inverse Diels Alder Click-Chemistry

摘要

The role of solid phase peptide synthesis (SPPS) [1] and "Click chemistry" [2] continually became more and more important in the recombinant chemistry for development of modern drugs which in turn demand not solely the specificity and efficiency, but also a sufficient local concentration of the drug at the target site. Circumventing the drawbacks of new active substances, like poor diffusion across biological membranes and a restricted solubility in physiological solvents requires both transport facilitating-(CPP) and address-peptidcs (NLS) [3-5]. The nature's treasure chest harbours excellent models for the development of pharmacological substances which allow a broad therapeutic index and simultaneously cause minimal adverse reactions of the transported active substances. Manifold multi-functional proteins like HIV-Tat and Homeo Box gene products which meet the demands are well identified.