Tandem mass spectrometry study of p38a kinase inhibitors and related substances

D. Falck; J. Kool; M. Honing; W.M.A. Niessen

doi:10.1002/jms.3219

Tandem mass spectrometry study of p38a kinase inhibitors and related substances

D. Falck, J. Kool, M. Honing, W.M.A. Niessen

Research output: Contribution to Journal › Article › Academic › peer-review

Abstract

The p38 mitogen-activated protein kinase α (p38α) is an important drug target widely investigated for therapy of chronic inflammatory diseases. Its inhibitors are rather lipophilic and as such not very favourable lead compounds in drug discovery. Therefore, we explored various approaches to access new chemical space, create diversity, and generate lead libraries with improved solubility and reduced lipophilicity, based on known p38α inhibitors, e.g., BIRB796 and TAK-715. Compound modification strategies include incubation with human liver microsomes and bacterial cytochrome P450 mutants from Bacillus megaterium and treatment by electrochemical oxidation, H

Original language	English
Pages (from-to)	718-731
Journal	Journal of Mass Spectrometry
Volume	48
DOIs	https://doi.org/10.1002/jms.3219
Publication status	Published - 2013

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AU - Honing, M.

AU - Niessen, W.M.A.

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AB - The p38 mitogen-activated protein kinase α (p38α) is an important drug target widely investigated for therapy of chronic inflammatory diseases. Its inhibitors are rather lipophilic and as such not very favourable lead compounds in drug discovery. Therefore, we explored various approaches to access new chemical space, create diversity, and generate lead libraries with improved solubility and reduced lipophilicity, based on known p38α inhibitors, e.g., BIRB796 and TAK-715. Compound modification strategies include incubation with human liver microsomes and bacterial cytochrome P450 mutants from Bacillus megaterium and treatment by electrochemical oxidation, H

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M3 - Article

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JF - Journal of Mass Spectrometry

ER -

Tandem mass spectrometry study of p38a kinase inhibitors and related substances

Abstract

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