期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 14, 页码 6639-6643出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm300677j
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资金
- Wellcome Trust
- Commonwealth Scholarship Commission in the United Kingdom
- Biotechnology and Biological Research Council (U.K.)
- European Research Council
- Canadian Institutes for Health Research
- Canadian Foundation for Innovation
- Genome Canada through the Ontario Genomics Institute
- GlaxoSmithKline
- Karolinska Institutet
- Knut and Alice Wallenberg Foundation
- Ontario Innovation Trust
- Ontario Ministry for Research and Innovation
- Merck Co., Inc.
- Novartis Research Foundation
- Swedish Agency for Innovation Systems
- Swedish Foundation for Strategic Research
The JmjC oxygenases catalyze the N-demethylation of N-epsilon-methyl lysine residues in histones and are current therapeutic targets. A set of human 2-oxoglutarate analogues were screened using a unified assay platform for JmjC demethylases and related oxygenases. Results led to the finding that daminozide (N-(dimethylamino)succinamic acid, 160 Da), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily. Kinetic and crystallographic studies reveal that daminozide chelates the active site metal via its hydrazide carbonyl and dimethylamino groups.
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