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Applicant:
Jawaharlal Nehru Centre for Advanced Scientific Research (JNCASR) Bengaluru 
Title:
Polyisoprenylated Benzophenones and Their Isomers as Inhibitors of Histone Acetyltransferases and Uses Thereof  
Inventor(s):
Tapas Kumar Kundu, Balasubramanyam Karanam, Mantelingu Kempegowda, Mohammad Altaf, Swaminathan Venkatesh, Radhika Ashish Varier 
Applicant:
Jawaharlal Nehru Centre for Advanced Scientific Research (JNCASR) Bengaluru 
Application type:
Applied - 2004-11-04 
Application Number:
PCT/IB04/052294 
Applied at:
International 
Entered by:
Jawaharlal Nehru Centre for Advanced Scientific Research (JNCASR) Bengaluru 
Abstract:
The present invention we describe the purification of prenylated benzophenones from the fruit rinds of Garcinia species and its evaluation as an inhibitor for Histone acetyltransferases p300 and PCAF. We have found that prenylated benzophenones are potent histone acetyltransferases (HAT) inhibitors of p300 (IC50-1μM) and PCAF (IC50-15μM). The inhibitors significantly repress the p300 HAT dependent transcriptional activation from invitro assembled chromatin template but had no effect on transcription from DNA. These results suggest that the compounds could be sepecific to HATs. Thus these compounds should be useful as the biological switching molecular for evaluating the role of p300 and PCAF in cellular functions and may be useful as new chemical entities for the developement of anticancer drugs. 

 
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