Gayraud, Felix ORCID: 0000-0001-8534-4993, Klussmann, Merlin and Neundorf, Ines ORCID: 0000-0001-6450-3991 (2021). Recent Advances and Trends in Chemical CPP-Drug Conjugation Techniques. Molecules, 26 (6). BASEL: MDPI. ISSN 1420-3049

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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

Item Type: Journal Article
CreatorsEmailORCIDORCID Put Code
URN: urn:nbn:de:hbz:38-564275
DOI: 10.3390/molecules26061591
Journal or Publication Title: Molecules
Volume: 26
Number: 6
Date: 2021
Publisher: MDPI
Place of Publication: BASEL
ISSN: 1420-3049
Language: English
Faculty: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
PEPTIDESMultiple languages
Biochemistry & Molecular Biology; Chemistry, MultidisciplinaryMultiple languages


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