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Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques

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...

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Detalles Bibliográficos
Autores principales: Gayraud, Félix, Klußmann, Merlin, Neundorf, Ines
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7998868/
https://www.ncbi.nlm.nih.gov/pubmed/33805680
http://dx.doi.org/10.3390/molecules26061591
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author Gayraud, Félix
Klußmann, Merlin
Neundorf, Ines
author_facet Gayraud, Félix
Klußmann, Merlin
Neundorf, Ines
author_sort Gayraud, Félix
collection PubMed
description 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
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spelling pubmed-79988682021-03-28 Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques Gayraud, Félix Klußmann, Merlin Neundorf, Ines Molecules Review 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 MDPI 2021-03-13 /pmc/articles/PMC7998868/ /pubmed/33805680 http://dx.doi.org/10.3390/molecules26061591 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Gayraud, Félix
Klußmann, Merlin
Neundorf, Ines
Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques
title Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques
title_full Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques
title_fullStr Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques
title_full_unstemmed Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques
title_short Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques
title_sort recent advances and trends in chemical cpp–drug conjugation techniques
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7998868/
https://www.ncbi.nlm.nih.gov/pubmed/33805680
http://dx.doi.org/10.3390/molecules26061591
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