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Intracellular targets of antitumor therapy: an increased complexity in the rational drug design

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Abstract

We discuss herein a paradigm of an intracellular target as a critical aspect in modern design of antitumor therapeutics. The key problems such as an uncertainty of target identification (due to binding of ligands to a variety of biomacromolecules), multiplicity of targets, and complexity of cell death signaling pathways were highlighted. Nevertheless, the idea of the preferred (the most affine) targeting by a drug candidate (specifically, the structure of the drug–target complexes) makes it possible to proceed from an empirical screening of chemical libraries to rational drug design by determining the molecular mechanisms of cytotoxicity.

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Correspondence to V. B. Tsvetkov.

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Dedicated to Academician of the Russian Academy of Sciences N. S. Zefirov on the occasion of his 80th birthday.

Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 9, pp. 2269–2272, September, 2015.

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Tsvetkov, V.B., Shtil, A.A. Intracellular targets of antitumor therapy: an increased complexity in the rational drug design. Russ Chem Bull 64, 2269–2272 (2015). https://doi.org/10.1007/s11172-015-1151-8

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  • DOI: https://doi.org/10.1007/s11172-015-1151-8

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