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Review

Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry

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Univ. Lille, Inserm, Institut Pasteur Lille, U1177-Drugs and Molecules for Living Systems, F-59000 Lille, France
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Univ. Lille, CNRS, Inserm, CHU Lille, Institut Pasteur de Lille, US 41-UMS 2014-PLBS, F-59000 Lille, France
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Authors to whom correspondence should be addressed.
Academic Editor: Kyle Hadden
Molecules 2021, 26(19), 6083; https://doi.org/10.3390/molecules26196083
Received: 23 July 2021 / Revised: 19 September 2021 / Accepted: 5 October 2021 / Published: 8 October 2021
(This article belongs to the Special Issue The Chemical Biology Research in France)
Chemical biology and drug discovery are two scientific activities that pursue different goals but complement each other. The former is an interventional science that aims at understanding living systems through the modulation of its molecular components with compounds designed for this purpose. The latter is the art of designing drug candidates, i.e., molecules that act on selected molecular components of human beings and display, as a candidate treatment, the best reachable risk benefit ratio. In chemical biology, the compound is the means to understand biology, whereas in drug discovery, the compound is the goal. The toolbox they share includes biological and chemical analytic technologies, cell and whole-body imaging, and exploring the chemical space through state-of-the-art design and synthesis tools. In this article, we examine several tools shared by drug discovery and chemical biology through selected examples taken from research projects conducted in our institute in the last decade. These examples illustrate the design of chemical probes and tools to identify and validate new targets, to quantify target engagement in vitro and in vivo, to discover hits and to optimize pharmacokinetic properties with the control of compound concentration both spatially and temporally in the various biophases of a biological system. View Full-Text
Keywords: drug discovery; hit to lead optimization; target engagement; target validation; kinetic target guided synthesis; fragment; early ADME drug discovery; hit to lead optimization; target engagement; target validation; kinetic target guided synthesis; fragment; early ADME
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MDPI and ACS Style

Deprez, B.; Bosc, D.; Charton, J.; Couturier, C.; Deprez-Poulain, R.; Flipo, M.; Leroux, F.; Villemagne, B.; Willand, N. Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry. Molecules 2021, 26, 6083. https://doi.org/10.3390/molecules26196083

AMA Style

Deprez B, Bosc D, Charton J, Couturier C, Deprez-Poulain R, Flipo M, Leroux F, Villemagne B, Willand N. Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry. Molecules. 2021; 26(19):6083. https://doi.org/10.3390/molecules26196083

Chicago/Turabian Style

Deprez, Benoit, Damien Bosc, Julie Charton, Cyril Couturier, Rebecca Deprez-Poulain, Marion Flipo, Florence Leroux, Baptiste Villemagne, and Nicolas Willand. 2021. "Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry" Molecules 26, no. 19: 6083. https://doi.org/10.3390/molecules26196083

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