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NMR screening for lead compounds using tryptophan-mutated proteins.

Title data

Rothweiler, Ulli ; Czarna, Anna ; Weber, Lutz ; Popowicz, Grzegorz M. ; Brongel, Kinga ; Kowalska, Kaja ; Orth, Michael ; Stemmann, Olaf ; Holak, Tad A.:
NMR screening for lead compounds using tryptophan-mutated proteins.
In: Journal of Medicinal Chemistry. Vol. 51 (28 August 2008) Issue 16 . - pp. 5035-5042.
ISSN 0022-2623
DOI: https://doi.org/10.1021/jm8002813

Official URL: Volltext

Abstract in another language

NMR-based drug screening methods provide the most reliable characterization of binding propensities of ligands to their target proteins. They are, however, one of the least effective methods in terms of the amount of protein required and the time needed for acquiring an NMR experiment. We show here that the introduction of tryptophan to proteins permits rapid screening by monitoring a simple 1D proton NMR signal of the NH side chain ((N)H(epsilon)) of the tryptophan. The method could also provide quantitative characterization of the antagonist-protein and antagonist-protein-protein interactions in the form of KDs and fractions of the released proteins from their mutual binding. We illustrate the method with the lead compounds that block the Mdm2-p53 interaction and by studying inhibitors that bind to cyclin-dependent kinase 2 (CDK2).

Further data

Item Type: Article in a journal
Refereed: Yes
Institutions of the University: Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Biology > Chair Genetics > Chair Genetics - Univ.-Prof. Dr. Olaf Stemmann
Profile Fields > Advanced Fields > Molecular Biosciences
Research Institutions > Research Centres > Bayreuth Center for Molecular Biosciences - BZMB
Faculties
Faculties > Faculty of Biology, Chemistry and Earth Sciences
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Biology
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Biology > Chair Genetics
Profile Fields
Profile Fields > Advanced Fields
Research Institutions
Research Institutions > Research Centres
Result of work at the UBT: No
DDC Subjects: 500 Science > 570 Life sciences, biology
Date Deposited: 26 Mar 2015 10:22
Last Modified: 26 Mar 2015 10:22
URI: https://eref.uni-bayreuth.de/id/eprint/8537