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Innovative Linker Strategies for Tumor‐Targeted Drug Conjugates
Author(s) -
Dal Corso Alberto,
Pignataro Luca,
Belvisi Laura,
Gennari Cesare
Publication year - 2019
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201903127
Subject(s) - linker , conjugate , chemistry , bioorthogonal chemistry , combinatorial chemistry , cytotoxic t cell , drug , covalent bond , small molecule , drug discovery , cleavage (geology) , therapeutic modalities , biochemistry , pharmacology , computer science , biology , click chemistry , medicine , in vitro , organic chemistry , mathematical analysis , paleontology , mathematics , fracture (geology) , operating system , physical therapy
Abstract The covalent conjugation of potent cytotoxic agents to either macromolecular carriers or small molecules represents a well‐known approach to increase the therapeutic index of these drugs, thus improving treatment efficacy and minimizing side effects. In general, cytotoxic activity is displayed only upon cleavage of a specific chemical bond (linker) that connects the drug to the carrier. The perfect balance between the linker stability and its selective cleavage represents the key for success in these therapeutic approaches and the chemical toolbox to reach this goal is continuously expanding. In this Review article, we highlight recent advances on the different modalities to promote the selective release of cytotoxic agents, either by exploiting specific hallmarks of the tumor microenvironment (e.g. pH, enzyme expression) or by the application of external triggers (e.g. light and bioorthogonal reactions).

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