caa a22 4500 445879033 CHVBK 20180317145536.0 cr unu---uuuuu 170323e20110501xx s 000 0 eng 10.1007/s11030-010-9299-5 doi (NATIONALLICENCE)springer-10.1007/s11030-010-9299-5 Chemical biology of Histone acetyltransferase natural compounds modulators [Elektronische Daten] [Fabrizio Piaz, Antonio Vassallo, Osmany Rubio, Sabrina Castellano, Gianluca Sbardella, Nunziatina De Tommasi] Histone acetyltransferases (HATs) are a class of epigenetic enzymes crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells, thus being a promising target for therapeutic development. Nonetheless, differently from histone deacetylases (HDACs) inhibitors, there is still paucity of small-molecule modulators of HAT activity. After a decline during past decade, natural products and their derivatives could be once again a valuable tool in the lead discovery process and meet such need of Novel Chemical Entities (NCEs). In this review, we will provide a comprehensive summary on the discovery of small-molecule HAT modulators from naturally occurring molecular scaffolds. Springer Science+Business Media B.V., 2010 Histone acetyltransferases nationallicence Natural compounds nationallicence Polyisoprenylated benzophenone derivatives nationallicence Anacardic acid nationallicence Polyphenols nationallicence ATF2 : Activated transcription factor 2 nationallicence bZip : Basic-zipper nationallicence CBP : CREB-binding protein nationallicence CTPB : N-(4-chloro-3-trifluoromethyl-phenyl)-2-ethoxy-6-pentadecyl-benzamide nationallicence DMSO : Dimethyl sulfoxide nationallicence EGCG : (−)-Epigallocatechin gallate nationallicence ER : Estrogen receptor nationallicence FAT : Transcription factor acetyltransferase nationallicence GCN5 : General control of nitrogen metabolism-5 protein nationallicence H2A : Histone H2A nationallicence H2B : Histone H2B nationallicence H3 : Histone H3 nationallicence H4 : Histone H4 nationallicence HAT : Histone acetyltransferase nationallicence HDAC : Histone deacetylase nationallicence HeLa : Human uterine cervical carcinoma cells, after the name of Henrietta Lacks, a patient at Johns Hopkins Hospital, Baltimore nationallicence HMT : Histone methyltransferase nationallicence IG : Isogarcinol nationallicence IP-10 : Human interferon-inducible protein 10 nationallicence MCF-7 : Michigan Cancer Foundation-7 nationallicence MIP-2 : Macrophage-inflammatory protein-2 nationallicence MYST : MOZ, YBF2/SAS3, SAS2, TIP60 N-acetyltransferase nationallicence MOZ : Monocytic leukaemia zinc-finger protein nationallicence NF−κB : Nuclear factor-kappa B nationallicence NOS2 : Nitric oxide synthase 2 nationallicence p300/CBP : E1A binding protein p300/CREB-binding protein nationallicence p300HD : p300 HAT domain nationallicence PBDs : Polyisoprenylated benzophenone derivatives nationallicence PBL : Peripheral blood lymphocytes nationallicence PC : Prostate cancer nationallicence PCAF : p300/CBP-associated factor nationallicence SDS-PAGE : Sodium dodecyl sulfate - Polyacrylamide gel electrophoresis nationallicence SGR : Sanguinarine nationallicence SIRT : Sirtuin nationallicence SNL : Solanum nigrum L nationallicence SPR : Surface plasmon resonance nationallicence SRC1 : Steroid receptor coactivator 1 nationallicence SRC2 : Steroid receptor coactivator 2 nationallicence TAFII250 : TBP associated factor II250 nationallicence TBP : TATA-binding protein nationallicence TNF : Tumor necrosis factor nationallicence Piaz Fabrizio Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut Vassallo Antonio Dipartimento di Chimica, Università degli Studi della Basilicata, Viale dell'Ateneo Lucano, 85100, Potenza (PZ), Italy aut Rubio Osmany Universidad de La Habana, Havana, Cuba aut Castellano Sabrina Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut Sbardella Gianluca Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut De Tommasi Nunziatina Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut Molecular Diversity Springer Netherlands 15/2(2011-05-01), 401-416 1381-1991 15:2<401 2011 15 11030 https://doi.org/10.1007/s11030-010-9299-5 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s11030-010-9299-5 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Piaz Fabrizio Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut NATIONALLICENCE 700 1- Vassallo Antonio Dipartimento di Chimica, Università degli Studi della Basilicata, Viale dell'Ateneo Lucano, 85100, Potenza (PZ), Italy aut NATIONALLICENCE 700 1- Rubio Osmany Universidad de La Habana, Havana, Cuba aut NATIONALLICENCE 700 1- Castellano Sabrina Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut NATIONALLICENCE 700 1- Sbardella Gianluca Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut NATIONALLICENCE 700 1- De Tommasi Nunziatina Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy aut NATIONALLICENCE 773 0- Molecular Diversity Springer Netherlands 15/2(2011-05-01), 401-416 1381-1991 15:2<401 2011 15 11030 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer