Drug Screening in Human Cells by NMR Spectroscopy Allows the Early Assessment of Drug Potency.
drug design
drug screening
in-cell NMR spectroscopy
structural biology
sulfonamide
Journal
Angewandte Chemie (International ed. in English)
ISSN: 1521-3773
Titre abrégé: Angew Chem Int Ed Engl
Pays: Germany
ID NLM: 0370543
Informations de publication
Date de publication:
16 04 2020
16 04 2020
Historique:
received:
21
10
2019
revised:
09
12
2019
pubmed:
6
2
2020
medline:
16
3
2021
entrez:
6
2
2020
Statut:
ppublish
Résumé
Structure-based drug development is often hampered by the lack of in vivo activity of promising compounds screened in vitro, due to low membrane permeability or poor intracellular binding selectivity. Herein, we show that ligand screening can be performed in living human cells by "intracellular protein-observed" NMR spectroscopy, without requiring enzymatic activity measurements or other cellular assays. Quantitative binding information is obtained by fast, inexpensive
Identifiants
pubmed: 32022355
doi: 10.1002/anie.201913436
pmc: PMC7187179
doi:
Substances chimiques
Carbonic Anhydrase Inhibitors
0
Ligands
0
Pharmaceutical Preparations
0
Sulfonamides
0
Carbonic Anhydrases
EC 4.2.1.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
6535-6539Informations de copyright
© 2020 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.
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