Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs

[Image: see text] To obtain new oral drugs in the beyond rule of five space, PROTACs among others, molecular properties should be optimized in early drug discovery. Degraders call for design strategies which focus on intramolecular interaction and chameleonicity. In parallel, tailored revalidation o...

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Autores principales: Ermondi, Giuseppe, Garcia Jimenez, Diego, Rossi Sebastiano, Matteo, Caron, Giulia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8274089/
https://www.ncbi.nlm.nih.gov/pubmed/34262642
http://dx.doi.org/10.1021/acsmedchemlett.1c00298
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author Ermondi, Giuseppe
Garcia Jimenez, Diego
Rossi Sebastiano, Matteo
Caron, Giulia
author_facet Ermondi, Giuseppe
Garcia Jimenez, Diego
Rossi Sebastiano, Matteo
Caron, Giulia
author_sort Ermondi, Giuseppe
collection PubMed
description [Image: see text] To obtain new oral drugs in the beyond rule of five space, PROTACs among others, molecular properties should be optimized in early drug discovery. Degraders call for design strategies which focus on intramolecular interaction and chameleonicity. In parallel, tailored revalidation of permeability assessment and prediction methods becomes fundamental in this innovative chemical space.
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spelling pubmed-82740892021-07-13 Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs Ermondi, Giuseppe Garcia Jimenez, Diego Rossi Sebastiano, Matteo Caron, Giulia ACS Med Chem Lett [Image: see text] To obtain new oral drugs in the beyond rule of five space, PROTACs among others, molecular properties should be optimized in early drug discovery. Degraders call for design strategies which focus on intramolecular interaction and chameleonicity. In parallel, tailored revalidation of permeability assessment and prediction methods becomes fundamental in this innovative chemical space. American Chemical Society 2021-06-08 /pmc/articles/PMC8274089/ /pubmed/34262642 http://dx.doi.org/10.1021/acsmedchemlett.1c00298 Text en © 2021 The Authors. Published by American Chemical Society Permits the broadest form of re-use including for commercial purposes, provided that author attribution and integrity are maintained (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Ermondi, Giuseppe
Garcia Jimenez, Diego
Rossi Sebastiano, Matteo
Caron, Giulia
Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs
title Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs
title_full Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs
title_fullStr Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs
title_full_unstemmed Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs
title_short Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs
title_sort rational control of molecular properties is mandatory to exploit the potential of protacs as oral drugs
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8274089/
https://www.ncbi.nlm.nih.gov/pubmed/34262642
http://dx.doi.org/10.1021/acsmedchemlett.1c00298
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