Design of Self-Immolative Linkers for Tumour-Activated Prodrug Therapy

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Design of Self-Immolative Linkers for Tumour-Activated Prodrug Therapy

Anti-Cancer Agents in Medicinal Chemistry, 8(6): 618-637.

Author(s): I. Tranoy-Opalinski, A. Fernandes, M. Thomas, J.-P. Gesson and S Papot.

Affiliation: Universite de Poitiers, UMRCNRS 6514, SRSN, 40 avenue du Recteur Pineau, 86022 Poitiers, France.


The main drawback of most cancer chemotherapy is its relatively low ability to target tumour cells versus normal cells. As a consequence, chemotherapy is usually connected with severe side effects due to the toxicity of traditional cytostatic agents towards normal tissues. A few years ago, the site-specific activation of non-toxic prodrugs in tumours has been proposed in order to enhance the selectivity for the killing of cancer cells. Within this framework, most of the prodrugs that have been designed were three part compounds comprising trigger, linker and effector units. The main function of the linker is to release the effector unit after selective trigger activation via a spontaneous chemical breakdown. However, its structure also affects significantly many prodrug properties such as stability, pharmacokinetic, organ distribution, bioavailability or trigger activation. This review, focussed on the linker unit, is an update of our previous article published in 2002. It deals with recent advances in the design of prodrug linkers including new delivery systems such as elongated linkers or selfimmolative dendrimers.


tumour cells, cancer chemotherapy, cytostatic agents, Self-Immolative Linkers, trigger, linker.

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Article Details

Volume: 8
Issue Number: 6
First Page: 618
Last Page: 637
Page Count: 20
DOI: 10.2174/187152008785133065
Price: $58

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