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Review

Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques

Department of Chemistry, Institute for Biochemistry, University of Cologne, Zuelpicher str. 47a, D-50674 Cologne, Germany
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Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Andrea Trabocchi
Molecules 2021, 26(6), 1591; https://doi.org/10.3390/molecules26061591
Received: 31 January 2021 / Revised: 8 March 2021 / Accepted: 10 March 2021 / Published: 13 March 2021
(This article belongs to the Special Issue Bioconjugation Strategies in Drug Delivery and Molecular Imaging)
This review summarizes recent developments in conjugation techniques for the synthesis of cell-penetrating peptide (CPP)–drug conjugates targeting cancer cells. We will focus on small organic molecules as well as metal complexes that were used as cytostatic payloads. Moreover, two principle ways of coupling chemistry will be discussed direct conjugation as well as the use of bifunctional linkers. While direct conjugation of the drug to the CPP is still popular, the use of bifunctional linkers seems to gain increasing attention as it offers more advantages related to the linker chemistry. Thus, three main categories of linkers will be highlighted, forming either disulfide acid-sensitive or stimuli-sensitive bonds. All techniques will be thoroughly discussed by their pros and cons with the aim to help the reader in the choice of the optimal conjugation technique that might be used for the synthesis of a given CPP–drug conjugate View Full-Text
Keywords: cell-penetrating peptides; peptide–drug conjugates; bioconjugation; peptide synthesis; anticancer drugs cell-penetrating peptides; peptide–drug conjugates; bioconjugation; peptide synthesis; anticancer drugs
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MDPI and ACS Style

Gayraud, F.; Klußmann, M.; Neundorf, I. Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques. Molecules 2021, 26, 1591. https://doi.org/10.3390/molecules26061591

AMA Style

Gayraud F, Klußmann M, Neundorf I. Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques. Molecules. 2021; 26(6):1591. https://doi.org/10.3390/molecules26061591

Chicago/Turabian Style

Gayraud, Félix, Merlin Klußmann, and Ines Neundorf. 2021. "Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques" Molecules 26, no. 6: 1591. https://doi.org/10.3390/molecules26061591

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