Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a
G9a is a histone lysine methyltransferase responsible for the methylation of histone H3 lysine 9. The discovery of A-366 arose from a unique diversity screening hit, which was optimized by incorporation of a propyl-pyrrolidine subunit to occupy the enzyme lysine channel. A-366 is a potent inhibitor...
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| Veröffentlicht in: | ACS medicinal chemistry letters 2014-02, Vol.5 (2), p.205-209 |
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| container_end_page | 209 |
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| container_title | ACS medicinal chemistry letters |
| container_volume | 5 |
| creator | Sweis, Ramzi F Pliushchev, Marina Brown, Peter J Guo, Jun Li, Fengling Maag, David Petros, Andrew M Soni, Nirupama B Tse, Chris Vedadi, Masoud Michaelides, Michael R Chiang, Gary G Pappano, William N |
| description | G9a is a histone lysine methyltransferase responsible for the methylation of histone H3 lysine 9. The discovery of A-366 arose from a unique diversity screening hit, which was optimized by incorporation of a propyl-pyrrolidine subunit to occupy the enzyme lysine channel. A-366 is a potent inhibitor of G9a (IC50: 3.3 nM) with greater than 1000-fold selectivity over 21 other methyltransferases. |
| doi_str_mv | 10.1021/ml400496h |
| format | Article |
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The discovery of A-366 arose from a unique diversity screening hit, which was optimized by incorporation of a propyl-pyrrolidine subunit to occupy the enzyme lysine channel. 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| identifier | ISSN: 1948-5875 |
| ispartof | ACS medicinal chemistry letters, 2014-02, Vol.5 (2), p.205-209 |
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| language | eng |
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| source | ACS Publications; EZB-FREE-00999 freely available EZB journals; PubMed Central |
| subjects | Letter |
| title | Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a |
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