Work

A Fast Method to Monitor Tyrosine Kinase Inhibitor Mechanisms

Year: 2024

Type: article

Abstract: High Resolution Image Download MS PowerPoint Slide Methionine residues within the kinase domain of Src serve as unique NMR probes capable of distinguishing between distinct conformational states of full-length Src, including alternative drug-inhibited forms. This approach offers a rapid method to differentiate between various inhibition mechanisms at any stage of drug development, eliminating the need to resolve the structure of Src-drug complexes. Using selectively 13 C-methyl-enriched methionine, spectra can be acquired in under an hour, while natural abundance spectra with comparable information are achievable within a few hours.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.4c02042

Authors: Alejandro Fernández, Margarida Gairí, María Teresa González, Miquel Pons

Institutions: Universitat de Barcelona, Centres Científics i Tecnològics de la Universitat de Barcelona

Language: English

Topic: Advanced NMR Techniques and Applications

Subfield: Spectroscopy

Field: Chemistry

Domain: Physical Sciences

Open Access status: hybrid

Estimated APC paid: $4,500