کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1358081 | 981319 | 2014 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design and synthesis of peptide-MCA substrates for a novel assay of histone methyltransferases and their inhibitors Design and synthesis of peptide-MCA substrates for a novel assay of histone methyltransferases and their inhibitors](/preview/png/1358081.png)
Histone methyltransferases (HMTs) play an important role in controlling gene expression through site-specific methylation of lysines in core and linker histones within chromatin. As the typical HMTs, G9a and Set7/9 have been intensively studied that G9a is specific to the methylation at H3K9 and H3K27 and represses transcription, while Set7/9 methylates at H3K4. In this report we prepared various peptide-MCAs (4-methylcoumaryl-7-amides) related to histone tail and protein-substrates such as p53 and estrogen receptor-α. The fluorogenic substrates are applied for the assay of HMTs and an inhibitor, for example. The most sensitive and specific MCA-substrates to G9a and Set7/9 are discovered. The peptide-MCAs corresponding to the methylation sequences are promising for screening of HMT inhibitors.
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Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 4, 15 February 2014, Pages 1268–1275