Harnessing conformational drivers in drug design.

Conformation preferences Conformational analysis Conformational design Conformational drivers Conformational ensemble Conformer Torsional preferences

Journal

Progress in medicinal chemistry
ISSN: 0079-6468
Titre abrégé: Prog Med Chem
Pays: Netherlands
ID NLM: 0376452

Informations de publication

Date de publication:
2024
Historique:
medline: 7 10 2024
pubmed: 7 10 2024
entrez: 6 10 2024
Statut: ppublish

Résumé

This review article explores the pivotal role of conformational drivers in the discovery of drug-like molecules and illustrates their significance through real-life examples. Understanding molecular conformation is paramount to drug hunting as it can impact on- and off-target potency, metabolism, permeability, and solubility. Each conformational driver or effector is described and exemplified in a separate section. The final section is dedicated to NMR spectroscopy and illustrates its utility as an essential tool for conformational design.

Identifiants

pubmed: 39370240
pii: S0079-6468(24)00001-8
doi: 10.1016/bs.pmch.2024.07.001
pii:
doi:

Substances chimiques

Pharmaceutical Preparations 0

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

1-60

Informations de copyright

Copyright © 2024 Elsevier B.V. All rights are reserved, including those for text and data mining, AI training, and similar technologies.

Auteurs

Praful Chovatia (P)

Evotec (UK) Ltd, Milton Park, Abingdon, United Kingdom. Electronic address: praful.chovatia@evotec.com.

Angelo Sanzone (A)

Evotec (UK) Ltd, Milton Park, Abingdon, United Kingdom.

Gert-Jan Hofman (GJ)

Evotec (UK) Ltd, Milton Park, Abingdon, United Kingdom.

Ruth Dooley (R)

Evotec (UK) Ltd, Milton Park, Abingdon, United Kingdom.

Bernardo Pezzati (B)

Evotec (Verona) S.r.l., Via Fleming, Verona, Italy.

Iuni Margaret Laura Trist (IML)

Evotec (Verona) S.r.l., Via Fleming, Verona, Italy.

Gilles Ouvry (G)

NRG Therapeutics, Stevenage Bioscience Catalyst, Stevenage, United Kingdom.

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Classifications MeSH