Organic compounds -- part of the class 532-570 series – Organic compounds – Oxygen containing
Reexamination Certificate
2008-07-22
2008-07-22
Witherspoon, Sikarl A (Department: 1621)
Organic compounds -- part of the class 532-570 series
Organic compounds
Oxygen containing
C514S685000
Reexamination Certificate
active
07402706
ABSTRACT:
In this patent we describe the purification of prenylated benzophenones from the fruit rinds ofGarciniaspecies and its evaluation as an inhibitor for Histone acetyltransferases p300 and PCAF. We have found that prenylated benzophenones are potent HAT inhibitors of p300 (IC50-1 μM) and pCAF (IC50-15 μM). The inhibitors significantly repress the p300 HAT dependent transcriptional activation from in vitro assembled chromatin template but had no effect on transcription from DNA. These results suggest that the compounds could be specific to HATs. Thus these compounds should be useful as biological switching molecule for evaluating the role of p300 and PCAF in cellular functions and may be useful as new chemical entities for the development of anticancer drugs.
REFERENCES:
Fuller et al. Guttiferone F, the first Prenylated Benzophenone fromAllanblackia stuhlmannii. Journal of Natural Products, 1999, vol. 62, pp. 130-132.
Roux et al. Structure- Activity Relationship of Polyisoprenyl Benzophenones fromGarcinia pyriferaon the Tubulin-Microtuble System. Journal of Natural Products, 2000, vol. 63, pp. 1070-1076.
Rao et al. Camboginol and Cambogin. Tetrahedron Letters, 1980, vol. 21 (20), pp. 1975-1978.
Krishnamurthy et al. Crystal and Molecular Structure of Isogarcinol. Tetrahedron Letters, 1982, vol. 23 (21), pp. 2233-2236.
Balasubramanyam Karanam
Mantelingu Kempegowda
Mohammad Altaf
Radhika A. Varier
Swaminathan Venkatesh
Hamre Schumann Mueller & Larson P.C.
Jawaharlal Nehru Centre for Advanced Scientific Research
Witherspoon Sikarl A
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