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Article: Target Identification of Kinase Inhibitor Alisertib (MLN8237) Using DNA-Programmed Affinity Labeling

TitleTarget Identification of Kinase Inhibitor Alisertib (MLN8237) Using DNA-Programmed Affinity Labeling
Authors
Issue Date2017
PublisherWiley - VCH Verlag GmbH & Co. KGaA. The Journal's web site is located at http://www.wiley-vch.de/home/chemistry
Citation
Chemistry: A European Journal, 2017, v. 23 n. 45, p. 10906-10914 How to Cite?
AbstractAccurate identification of the molecular targets of bioactive small molecules is a highly important yet challenging task in biomedical research. Previously, a method named DPAL (DNA-programmed affinity labeling) for labeling and identifying the cellular targets of small molecules and nucleic acids was developed. Herein, DPAL is applied for the target identification of Alisertib (MLN8237), which is a highly specific aurora kinase A (AKA) inhibitor and a drug candidate being tested in clinical trials for cancer treatment. Apart from the well-established target of AKA, several potential new targets of MLN8237 were identified. Among them, p38 mitogen-activated protein kinase (p38) and laminin receptor (LAMR) were validated to be implicated in the anticancer activities of MLN8237. Interestingly, these new targets were not identified with non-DNA-based affinity probes. This work may facilitate an understanding of the molecular basis of the efficacy and side effects of MLN8237 as a clinical drug candidate. On the other hand, this work has also demonstrated that the method of DPAL could be a useful tool for target identification of bioactive small molecules.
Persistent Identifierhttp://hdl.handle.net/10722/243008
ISSN
2019 Impact Factor: 4.857
2015 SCImago Journal Rankings: 2.323
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorWang, D-
dc.contributor.authorCao, Y-
dc.contributor.authorZheng, L-
dc.contributor.authorChen, L-
dc.contributor.authorChen, X-
dc.contributor.authorHong, Z-
dc.contributor.authorZhu, Z-
dc.contributor.authorLi, X-
dc.contributor.authorChai, Y-
dc.date.accessioned2017-08-25T02:48:39Z-
dc.date.available2017-08-25T02:48:39Z-
dc.date.issued2017-
dc.identifier.citationChemistry: A European Journal, 2017, v. 23 n. 45, p. 10906-10914-
dc.identifier.issn0947-6539-
dc.identifier.urihttp://hdl.handle.net/10722/243008-
dc.description.abstractAccurate identification of the molecular targets of bioactive small molecules is a highly important yet challenging task in biomedical research. Previously, a method named DPAL (DNA-programmed affinity labeling) for labeling and identifying the cellular targets of small molecules and nucleic acids was developed. Herein, DPAL is applied for the target identification of Alisertib (MLN8237), which is a highly specific aurora kinase A (AKA) inhibitor and a drug candidate being tested in clinical trials for cancer treatment. Apart from the well-established target of AKA, several potential new targets of MLN8237 were identified. Among them, p38 mitogen-activated protein kinase (p38) and laminin receptor (LAMR) were validated to be implicated in the anticancer activities of MLN8237. Interestingly, these new targets were not identified with non-DNA-based affinity probes. This work may facilitate an understanding of the molecular basis of the efficacy and side effects of MLN8237 as a clinical drug candidate. On the other hand, this work has also demonstrated that the method of DPAL could be a useful tool for target identification of bioactive small molecules.-
dc.languageeng-
dc.publisherWiley - VCH Verlag GmbH & Co. KGaA. The Journal's web site is located at http://www.wiley-vch.de/home/chemistry-
dc.relation.ispartofChemistry: A European Journal-
dc.rightsPreprint This is the pre-peer reviewed version of the following article: [FULL CITE], which has been published in final form at [Link to final article]. Authors are not required to remove preprints posted prior to acceptance of the submitted version. Postprint This is the peer reviewed version of the following article: [FULL CITE], which has been published in final form at [Link to final article using the DOI]. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving: http://olabout.wiley.com/WileyCDA/Section/id-828039.html#terms-
dc.titleTarget Identification of Kinase Inhibitor Alisertib (MLN8237) Using DNA-Programmed Affinity Labeling-
dc.typeArticle-
dc.identifier.emailLi, X: xiaoyuli@hku.hk-
dc.identifier.authorityLi, X=rp02080-
dc.identifier.doi10.1002/chem.201702033-
dc.identifier.scopuseid_2-s2.0-85026301832-
dc.identifier.hkuros274706-
dc.identifier.volume23-
dc.identifier.issue45-
dc.identifier.spage10906-
dc.identifier.epage10914-
dc.identifier.isiWOS:000407397300029-
dc.publisher.placeGermany-

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