A chrysin derivative suppresses skin cancer growth by inhibiting cyclin-dependent kinases

Haidan Liu, Kangdong Liu, Zunnan Huang, Chan Mi Park, N. R. Thimmegowda, Jae Hyuk Jang, In Ja Ryoo, Long He, Sun Ok Kim, Naomi Hamada, Ki Won Lee, Nak Kyun Soung, Ann M. Bode, Yifeng Yang, Xinmin Zhou, Raymond L. Erikson, Jong Seog Ahn, Joonsung Hwang, Kyoon Eon Kim, Zigang DongBo Yeon Kim

Research output: Contribution to journalArticlepeer-review

22 Scopus citations

Abstract

Background: Binding to the ATP site results in poor selectivity; therefore, development of ATP-noncompetitive inhibitors is needed. Results: A modified chrysin with anticancer activity targets Cdks and binds to a Cdk2 allosteric site, not the ATP pocket. Conclusion: Modified chrysin is a novel ATP-noncompetitive inhibitor. Significance: This pharmacophore model might provide insights for the development of new ATP-noncompetitive agents.

Original languageEnglish (US)
Pages (from-to)25924-25937
Number of pages14
JournalJournal of Biological Chemistry
Volume288
Issue number36
DOIs
StatePublished - Sep 6 2013

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