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Future Med Chem. 2012 Aug;4(12):1567-86. doi: 10.4155/fmc.12.76.

Peptides and peptide conjugates: therapeutics on the upward path.

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Institute of Biochemistry, Faculty of Biosciences, Pharmacy & Psychology, Universität Leipzig, Brüderstrasse 34, 04103 Leipzig, Germany.


The main benefit of natural peptides, peptide analogs and newly designed peptides as therapeutics, lies in their high selectivity and affinity, which are frequently in the nanomolar range. New drugs targeting protein-protein interactions often require larger interaction sites than small molecules can offer. Thus, many peptidic drugs are already applied in therapy at the current state. The next generation of peptide-based therapeutic agents is currently on its way from basic research to clinical studies and eventually to the pharmaceutical market. Development of more robust and long-lasting drugs owing to well-known and new stabilization strategies is yielding novel and continuously improving peptide drugs. The introduction of smart linkers that exhibit stability towards blood plasma but intracellular lability will lead to target-oriented activity, which might successfully decrease side effects. In this review, peptidic therapeutics on the market, in clinical studies and some of those in basic research are characterized. Stabilization strategies and intelligent linkers are discussed with respect to their use in peptide drug therapy.

[Indexed for MEDLINE]

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