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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/222479
A fast method to monitor tyrosine kinase inhibitors mechanisms
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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 13C-methyl-enriched methionine, spectra can be acquired in under an hour, while natural abundance spectra with comparable information are achievable within a few hours.
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FERNÁNDEZ, Alejandro, et al. A fast method to monitor tyrosine kinase inhibitors mechanisms. Journal of Medicinal Chemistry. 2024. Vol. 67, num. 20571-20579. ISSN 0022-2623. [consulted: 14 of June of 2026]. Available at: https://hdl.handle.net/2445/222479