共查询到20条相似文献,搜索用时 25 毫秒
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Sbardella G Castellano S Vicidomini C Rotili D Nebbioso A Miceli M Altucci L Mai A 《Bioorganic & medicinal chemistry letters》2008,18(9):2788-2792
Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs. 相似文献
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Massimo Ghizzoni André Boltjes Chris de Graaf Hidde J. Haisma Frank J. Dekker 《Bioorganic & medicinal chemistry》2010,18(16):5826-5834
Several lines of evidence indicate that histone acetyltransferases (HATs) are novel drug targets for treatment of diseases like, for example, cancer and inflammation. The natural product anacardic acid is a starting point for development of small molecule inhibitors of the histone acetyltransferase (HAT) p300/CBP associated factor (PCAF). In order to optimize the inhibitory potency, a binding model for PCAF inhibition by anacardic acid was proposed and new anacardic acid derivatives were designed. Ten new derivatives were synthesized using a novel synthetic route. One compound showed a twofold improved inhibitory potency for the PCAF HAT activity and a twofold improved inhibition of histone acetylation in HEP G2 cells. 相似文献
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Regulation of E2A activities by histone acetyltransferases in B lymphocyte development 总被引:4,自引:0,他引:4
Bradney C Hjelmeland M Komatsu Y Yoshida M Yao TP Zhuang Y 《The Journal of biological chemistry》2003,278(4):2370-2376
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Hess-Stumpp H 《European journal of cell biology》2005,84(2-3):109-121
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Asako Hironaka Tetsuji Kawakami Yasuharu Tanaka 《Biochemical and biophysical research communications》2009,390(2):290-100
The cyclopentenonic prostaglandin 15-deoxy-Δ12,14-PG J2 (15d-PGJ2) is a metabolite derived from PGD2. Although 15d-PGJ2 has been demonstrated to be a potent ligand for peroxisome proliferator activated receptor γ (PPARγ), the functions are not fully understood. In order to examine the effect of 15d-PGJ2 on histone acetyltransferases (HATs), several lines of cell including mouse embryonic fibroblast (MEF) cells were exposed to 15d-PGJ2. Three types of HAT, p300, CREB-binding protein (CBP), and p300/CBP-associated factor (PCAF), selectively disappeared from the soluble fraction in time- and dose-dependent manners. Inversely, HATs in the insoluble fraction increased, suggesting their conformational changes. The decrease in the soluble form of HATs resulted in the attenuation of NF-κB-, p53-, and heat shock factor-dependent reporter gene expressions, implying that the insoluble HATs are inactive. The resultant insoluble PCAF and p300 seemed to be digested by proteasome, because proteasome inhibitors caused the accumulation of insoluble HATs. Taken together, these results indicate that 15d-PGJ2 attenuates some gene expressions that require HATs. This inhibitory action of 15d-PGJ2 on the function of HATs was independent of PPARγ, because PPARγ agonists could not mimick 15d-PGJ2 and PPARγ antagonists did not inhibit 15d-PGJ2. 相似文献
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