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Article

Limited Proteolysis Combined with Stable Isotope Labeling Reveals Conformational Changes in Protein (Pseudo)kinases upon Binding Small Molecules.

Journal of proteome research - 2 Oct 2015

Di Michele Michela, Stes Elisabeth, Vandermarliere Elien, Arora Rohit, Astorga-Wells Juan, Vandenbussche Jonathan, van Heerde Erika, Zubarev Roman, Bonnet Pascal, Linders Joannes T M, Jacoby Edgar, Brehmer Dirk, Martens Lennart, Gevaert Kris

Abstract excerpt

Likely due to conformational rearrangements, small molecule inhibitors may stabilize the active conformation of protein kinases and paradoxically promote tumorigenesis. We combined limited proteolysis with stable isotope labeling MS to monitor protein conformational changes upon binding of small molecules. Applying this method to the human serine/threonine kinase B-Raf, frequently mutated in cancer, we found that...

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Identifiers

PMID: 26293246
DOI: 10.1021/acs.jproteome.5b00282

Genes

KSR1
PNP

Variants

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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