Small-molecule inhibitors of histone acetyltransferase activity: Identification and biological properties (508 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2006 Nov 16; 49(23): 6897-6907.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 5.115, 5-year impact factor: 5.504
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-33750989910&partnerID=40&md5=2d11e2bb1daaf2c6978d13baf41b41f1
Keywords: 4 Hydroxy 2 Pentyl 3 Quinolinecarboxylic Acid, Alpha Tubulin, Anacardic Acid, Cell Extract, Curcumin, Enzyme Inhibitor, Histone Acetyltransferase, Histone Acetyltransferase Gcn5, Histone Acetyltransferase Inhibitor, Mb 3, Quinoline Derivative, Unclassified Drug, Acetylation, Antifungal Activity, Apoptosis, Article, Catalysis, Cell Cycle Arrest, Cell Cycle G1 Phase, Cell Differentiation, Cell Strain U937, Controlled Study, Deletion Mutant, Enzyme Activity, Enzyme Inhibition, Fungus Growth, Genetic Transcription, Granulocyte, Human, Human Cell, Nonhuman, Reference Value, Reporter Gene, Saccharomyces Cerevisiae, Antineoplastic Agents, Saccharomyces Cerevisiae Proteins, Structure-Activity Relationship, Trans-Activation (genetics), U937 Cells,
Affiliations:
*** IBB - CNR ***
Dipartimento di Studi Farmaceutici, Istituto Pasteur-Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Roma, Italy
Dipartimento di Genetica e Biologia Molecolare, Università degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Roma, Italy
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy
Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. De Crecchio 7, 80138 Napoli, Italy
Centro di Oncogenomica AIRC, CEINGE Biotecnologia Avanzata, Napoli, Italy
References:
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Kouzarides, T., Histone acetylases and deacetylases in cell proliferation (1999) Curr. Opin. Genet. Dev., 9, pp. 40-48
Strahl, B.D., Allis, C.D., The language of covalent histone modifications (2000) Nature, 403, pp. 41-45
Pazin, M.J., Kadonaga, J.T., What's up and down with histone deacetylation and transcription? (1997) Cell, 89, pp. 325-328
Glass, C.K., Rosenfeld, M.G., The coregulator exchange in transcriptional functions of nuclear receptors (2000) Genes Dev., 14, pp. 121-141
Luger, K., Mader, A.W., Richmond, R.K., Sargent, D.F., Richmond, T.J., Crystal structure of the nucleosome core particle at 2.8 Å resolution (1998) Nature, 389, pp. 251-260
Urnov, F.D., Wolffe, A., Chromatin organization and human disease (2000) Emerging Ther. Targets, 4, pp. 665-685
Fischle, W., Wang, Y., Allis, C.D., Histone and chromatin crosstalk (2003) Curr. Opin. Cell Biol., 15, pp. 172-183
Akey, C.W., Luger, K., Histone chaperones and nucleosome assembly (2003) Curr. Opin. Struct. Biol., 13, pp. 6-14
Roth, S.Y., Denu, J.M., Allis, C.D., Histone acetyltransferases (2001) Annu. Rev. Biochem., 70, pp. 81-120
Sterner, D.E., Berger, S.L., Acetylation of histones and transcription-related factors (2000) Microbiol. Mol. Biol. Rev., 64, pp. 435-459
Marmorstein, R., Structure of histone acetyltransferases (2001) J. Mol. Biol., 311, pp. 433-444
Schiltz, R.L., Mizzen, C.A., Vassilev, A., Cook, R.G., Allis, C.D., Nakatani, Y., Overlapping but distinct patterns of histone acetylation by the human coactivators p300 and PCAF within nucleosomal substrates (1999) J. Biol. Chem., 274, pp. 1189-1192
Lau, O.D., Courtney, A.D., Vassilev, A., Marzilli, L.A., Cotter, R.J., Nakatani, Y., Cole, P.A., p300/CBP-associated factor histone acetyltransferase processing of a peptide substrate. Kinetic analysis of the catalytic mechanism (2000) J. Biol. Chem., 275, pp. 21953-21959
Grant, P.A., Duggan, L., Cote, J., Roberts, S.M., Brownell, J.E., Candau, R., Ohba, R., Workman, J.L., Yeast Gcn5 functions in two multisubunit complexes to acetylate nucleosomal histones: Characterization of an Ada complex and the SAGA (Spt/Ada) complex (1997) Genes Dev., 11, pp. 1640-1650
Grant, P.A., Eberharter, A., John, S., Cook, R.G., Turner, B.M., Workman, J.L., Expanded lysine acetylation specificity of Gcn5 in native complexes (1999) J. Biol. Chem., 274, pp. 5895-5900
Liu, Y., Colosimo, A.L., Yang, X.-J., Liao, D., Adenovirus E1B 55-kilodalton oncoprotein inhibits p53 acetylation by PCAF (2000) Mol. Cell Biol., 20, pp. 5540-5553
Hubbert, C., Guardiola, A., Shao, R., Kawaguchi, Y., Ito, A., Nixon, A., Yoshida, M., Yao, T.P., HDAC6 is a microtubule-associated deacetylase (2002) Nature, 417, pp. 455-458
Mai, A., Massa, S., Rotili, D., Cerbara, I., Valente, S., Pezzi, R., Simeoni, S., Ragno, R., Histone deacetylation in epigenetics: An attractive target for anticancer therapy (2005) Med. Res. Rev., 25, pp. 261-309
Minucci, S., Pelicci, P.G., Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer (2006) Nat. Rev. Cancer, 6, pp. 38-51
Muraoka, M., Konishi, M., Kikuchi-Yanoshita, R., Tanaka, K., Shitara, N., Chong, J.M., Iwama, T., Miyaki, M., p300 gene alterations in colorectal and gastic carcinomas (1996) Oncogene, 12, pp. 1565-1569
Phillips, A.C., Vousden, K.H., Acetyltransferases and tumor suppression (2000) Breast Cancer Res., 2, pp. 244-246
Anzick, S.L., Kononen, J., Walker, R.L., Azorsa, D.O., Tanner, M.M., Guan, X.Y., Sauter, G., Meltzer, P.S., AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer (1997) Science, 277, pp. 965-969
Sakakura, C., Hagiwara, A., Yasuoka, R., Fujita, Y., Nakanishi, M., Masuda, K., Kimura, A., Yamagishi, H., Amplification and overexpression of the AIB1 nuclear receptor co-activator gene in primary gastric cancers (2000) Int. J. Cancer, 89, pp. 217-223
Aguiar, R.C., Chase, A., Coulthard, S., Macdonald, D.H., Carapeti, M., Reiter, A., Sohal, J., Cross, N.C., Abnormalities of chromosome band 8p11 in leukaemia: Two clinical syndromes can be distinguished on the basis of MOZ involvement (1997) Blood, 90, pp. 3130-3135
Panagopoulos, I., Fioretos, T., Isaksson, M., Isaksson, M., Samuelsson, U., Billstrom, R., Strombeck, B., Johansson, B., Fusion of the MORF and CBP genes in acute myeloid leukemia with the t(10
p13) (2001) Hum. Mol. Genet., 10, pp. 395-404
Puri, P.L., Sartorelli, V., Yang, X.J., Hamamori, Y., Ogryzko, V.V., Howard, B.H., Kedes, L., Levrero, M., Differential roles of p300 and PCAF acetyltransferases in muscle differentiation (1997) Mol. Cell, 1, pp. 35-45
Lehrmann, H., Pritchard, L.L., Harel-Bellan, A., Histone acetyltransferases and deacetylases in the control of cell proliferation and differentiation (2002) Adv. Cancer Res., 86, pp. 41-65
Zheng, Y., Thompson, P.R., Cebrat, M., Wang, L., Devlin, M., Alani, R.M., Cole, P.A., Selective HAT inhibitors as mechanistic tools for protein acetylation (2004) Methods Enzymol., 376, pp. 188-199
Lau, O.D., Kundu, T.K., Soccio, R.E., Ait-Si-Ali, S., Khalil, E.M., Vassilev, A., Wolffe, A.P., Cole, P.A., HATs off: Selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF (2000) Mol. Cell, 5, pp. 589-595
Balasubramanyam, K., Swaminathan, V., Ranganathan, A., Kundu, T.K., Small molecule modulators of histone acetyltransferase p300 (2003) J. Biol. Chem., 278, pp. 19134-19140
Biel, M., Kretsovali, A., Karatzali, E., Papamatheakis, J., Giannis, A., Design, synthesis and biological evaluation of a small molecule inhibitor of the histone acetyltransferase GCN5 (2004) Angew. Chem., Int. Ed., 43, pp. 3974-3976
Stimson, L., Rowlands, M.G., Newbatt, Y.M., Smith, N.F., Raynaud, F.I., Rogers, P., Bavetsias, V., Aherne, G.W., Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity (2005) Mol. Cancer Ther., 4, pp. 1521-1532
Massa, S., Mai, A., Sbardella, G., Esposito, M., Ragno, R., Loidl, P., Brosch, G., 3-(4-Aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors (2001) J. Med. Chem., 44, pp. 2069-2072
Ragno, R., Mai, A., Massa, S., Cerbara, I., Valente, S., Bottoni, P., Scatena, R., Brosch, G., 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies (2004) J. Med. Chem., 47, pp. 1351-1359
Georgakopoulos, T., Thireos, G., Two distinct yeast transcriptional activators require the function of the GCN5 protein to promote normal levels of transcription (1992) EMBO J., 11, pp. 4145-4152
Warrell Jr., R.P., Frankel, S.R., Miller Jr., W.H., Scheinberg, D.A., Itri, L.M., Hittelman, W.N., Vyas, R., Jakubowski, A.N., (1991) Engl. J. Med., 324, p. 1385
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Shute, R.E., Dunlap, B., Rich, D.H., Analogues of the cytostatic and antimitogenic agents chlamydocin and HC-toxin: Synthesis and biological activity of chloromethyl ketone and diazomethyl ketone functionalized cyclic tetrapeptides (1987) J. Med. Chem., 30, pp. 71-78
Diana, G.D., McKinlay, M.A., Otto, M.J., Akullian, V., Oglesby, C., [[(4,5-Dihydro-2-oxazolyl)phenoxy]alkyl]isoxazoles. Inhibitors of picornavirus uncoating (1985) J. Med. Chem., 28, pp. 1906-1910
Ornaghi, P., Rotili, D., Sbardella, G., Mai, A., Filetici, P., A novel Gcn5p inhibitor represses cell growth, gene transcription and histone acetylation in budding yeast (2005) Biochem. Pharmacol., 70, pp. 911-917
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J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2006 Nov 16; 49(23): 6897-6907.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 5.115, 5-year impact factor: 5.504
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-33750989910&partnerID=40&md5=2d11e2bb1daaf2c6978d13baf41b41f1
Keywords: 4 Hydroxy 2 Pentyl 3 Quinolinecarboxylic Acid, Alpha Tubulin, Anacardic Acid, Cell Extract, Curcumin, Enzyme Inhibitor, Histone Acetyltransferase, Histone Acetyltransferase Gcn5, Histone Acetyltransferase Inhibitor, Mb 3, Quinoline Derivative, Unclassified Drug, Acetylation, Antifungal Activity, Apoptosis, Article, Catalysis, Cell Cycle Arrest, Cell Cycle G1 Phase, Cell Differentiation, Cell Strain U937, Controlled Study, Deletion Mutant, Enzyme Activity, Enzyme Inhibition, Fungus Growth, Genetic Transcription, Granulocyte, Human, Human Cell, Nonhuman, Reference Value, Reporter Gene, Saccharomyces Cerevisiae, Antineoplastic Agents, Saccharomyces Cerevisiae Proteins, Structure-Activity Relationship, Trans-Activation (genetics), U937 Cells,
Affiliations:
*** IBB - CNR ***
Dipartimento di Studi Farmaceutici, Istituto Pasteur-Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Roma, Italy
Dipartimento di Genetica e Biologia Molecolare, Università degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Roma, Italy
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy
Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. De Crecchio 7, 80138 Napoli, Italy
Centro di Oncogenomica AIRC, CEINGE Biotecnologia Avanzata, Napoli, Italy
References:
Davie, J.R., Covalent modifications of histones: Expression from chromatin templates (1998) Curr. Opin. Genet. Dev., 8, pp. 173-17
Kouzarides, T., Histone acetylases and deacetylases in cell proliferation (1999) Curr. Opin. Genet. Dev., 9, pp. 40-48
Strahl, B.D., Allis, C.D., The language of covalent histone modifications (2000) Nature, 403, pp. 41-45
Pazin, M.J., Kadonaga, J.T., What's up and down with histone deacetylation and transcription? (1997) Cell, 89, pp. 325-328
Glass, C.K., Rosenfeld, M.G., The coregulator exchange in transcriptional functions of nuclear receptors (2000) Genes Dev., 14, pp. 121-141
Luger, K., Mader, A.W., Richmond, R.K., Sargent, D.F., Richmond, T.J., Crystal structure of the nucleosome core particle at 2.8 Å resolution (1998) Nature, 389, pp. 251-260
Urnov, F.D., Wolffe, A., Chromatin organization and human disease (2000) Emerging Ther. Targets, 4, pp. 665-685
Fischle, W., Wang, Y., Allis, C.D., Histone and chromatin crosstalk (2003) Curr. Opin. Cell Biol., 15, pp. 172-183
Akey, C.W., Luger, K., Histone chaperones and nucleosome assembly (2003) Curr. Opin. Struct. Biol., 13, pp. 6-14
Roth, S.Y., Denu, J.M., Allis, C.D., Histone acetyltransferases (2001) Annu. Rev. Biochem., 70, pp. 81-120
Sterner, D.E., Berger, S.L., Acetylation of histones and transcription-related factors (2000) Microbiol. Mol. Biol. Rev., 64, pp. 435-459
Marmorstein, R., Structure of histone acetyltransferases (2001) J. Mol. Biol., 311, pp. 433-444
Schiltz, R.L., Mizzen, C.A., Vassilev, A., Cook, R.G., Allis, C.D., Nakatani, Y., Overlapping but distinct patterns of histone acetylation by the human coactivators p300 and PCAF within nucleosomal substrates (1999) J. Biol. Chem., 274, pp. 1189-1192
Lau, O.D., Courtney, A.D., Vassilev, A., Marzilli, L.A., Cotter, R.J., Nakatani, Y., Cole, P.A., p300/CBP-associated factor histone acetyltransferase processing of a peptide substrate. Kinetic analysis of the catalytic mechanism (2000) J. Biol. Chem., 275, pp. 21953-21959
Grant, P.A., Duggan, L., Cote, J., Roberts, S.M., Brownell, J.E., Candau, R., Ohba, R., Workman, J.L., Yeast Gcn5 functions in two multisubunit complexes to acetylate nucleosomal histones: Characterization of an Ada complex and the SAGA (Spt/Ada) complex (1997) Genes Dev., 11, pp. 1640-1650
Grant, P.A., Eberharter, A., John, S., Cook, R.G., Turner, B.M., Workman, J.L., Expanded lysine acetylation specificity of Gcn5 in native complexes (1999) J. Biol. Chem., 274, pp. 5895-5900
Liu, Y., Colosimo, A.L., Yang, X.-J., Liao, D., Adenovirus E1B 55-kilodalton oncoprotein inhibits p53 acetylation by PCAF (2000) Mol. Cell Biol., 20, pp. 5540-5553
Hubbert, C., Guardiola, A., Shao, R., Kawaguchi, Y., Ito, A., Nixon, A., Yoshida, M., Yao, T.P., HDAC6 is a microtubule-associated deacetylase (2002) Nature, 417, pp. 455-458
Mai, A., Massa, S., Rotili, D., Cerbara, I., Valente, S., Pezzi, R., Simeoni, S., Ragno, R., Histone deacetylation in epigenetics: An attractive target for anticancer therapy (2005) Med. Res. Rev., 25, pp. 261-309
Minucci, S., Pelicci, P.G., Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer (2006) Nat. Rev. Cancer, 6, pp. 38-51
Muraoka, M., Konishi, M., Kikuchi-Yanoshita, R., Tanaka, K., Shitara, N., Chong, J.M., Iwama, T., Miyaki, M., p300 gene alterations in colorectal and gastic carcinomas (1996) Oncogene, 12, pp. 1565-1569
Phillips, A.C., Vousden, K.H., Acetyltransferases and tumor suppression (2000) Breast Cancer Res., 2, pp. 244-246
Anzick, S.L., Kononen, J., Walker, R.L., Azorsa, D.O., Tanner, M.M., Guan, X.Y., Sauter, G., Meltzer, P.S., AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer (1997) Science, 277, pp. 965-969
Sakakura, C., Hagiwara, A., Yasuoka, R., Fujita, Y., Nakanishi, M., Masuda, K., Kimura, A., Yamagishi, H., Amplification and overexpression of the AIB1 nuclear receptor co-activator gene in primary gastric cancers (2000) Int. J. Cancer, 89, pp. 217-223
Aguiar, R.C., Chase, A., Coulthard, S., Macdonald, D.H., Carapeti, M., Reiter, A., Sohal, J., Cross, N.C., Abnormalities of chromosome band 8p11 in leukaemia: Two clinical syndromes can be distinguished on the basis of MOZ involvement (1997) Blood, 90, pp. 3130-3135
Panagopoulos, I., Fioretos, T., Isaksson, M., Isaksson, M., Samuelsson, U., Billstrom, R., Strombeck, B., Johansson, B., Fusion of the MORF and CBP genes in acute myeloid leukemia with the t(10
p13) (2001) Hum. Mol. Genet., 10, pp. 395-404
Puri, P.L., Sartorelli, V., Yang, X.J., Hamamori, Y., Ogryzko, V.V., Howard, B.H., Kedes, L., Levrero, M., Differential roles of p300 and PCAF acetyltransferases in muscle differentiation (1997) Mol. Cell, 1, pp. 35-45
Lehrmann, H., Pritchard, L.L., Harel-Bellan, A., Histone acetyltransferases and deacetylases in the control of cell proliferation and differentiation (2002) Adv. Cancer Res., 86, pp. 41-65
Zheng, Y., Thompson, P.R., Cebrat, M., Wang, L., Devlin, M., Alani, R.M., Cole, P.A., Selective HAT inhibitors as mechanistic tools for protein acetylation (2004) Methods Enzymol., 376, pp. 188-199
Lau, O.D., Kundu, T.K., Soccio, R.E., Ait-Si-Ali, S., Khalil, E.M., Vassilev, A., Wolffe, A.P., Cole, P.A., HATs off: Selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF (2000) Mol. Cell, 5, pp. 589-595
Balasubramanyam, K., Swaminathan, V., Ranganathan, A., Kundu, T.K., Small molecule modulators of histone acetyltransferase p300 (2003) J. Biol. Chem., 278, pp. 19134-19140
Biel, M., Kretsovali, A., Karatzali, E., Papamatheakis, J., Giannis, A., Design, synthesis and biological evaluation of a small molecule inhibitor of the histone acetyltransferase GCN5 (2004) Angew. Chem., Int. Ed., 43, pp. 3974-3976
Stimson, L., Rowlands, M.G., Newbatt, Y.M., Smith, N.F., Raynaud, F.I., Rogers, P., Bavetsias, V., Aherne, G.W., Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity (2005) Mol. Cancer Ther., 4, pp. 1521-1532
Massa, S., Mai, A., Sbardella, G., Esposito, M., Ragno, R., Loidl, P., Brosch, G., 3-(4-Aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors (2001) J. Med. Chem., 44, pp. 2069-2072
Ragno, R., Mai, A., Massa, S., Cerbara, I., Valente, S., Bottoni, P., Scatena, R., Brosch, G., 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies (2004) J. Med. Chem., 47, pp. 1351-1359
Georgakopoulos, T., Thireos, G., Two distinct yeast transcriptional activators require the function of the GCN5 protein to promote normal levels of transcription (1992) EMBO J., 11, pp. 4145-4152
Warrell Jr., R.P., Frankel, S.R., Miller Jr., W.H., Scheinberg, D.A., Itri, L.M., Hittelman, W.N., Vyas, R., Jakubowski, A.N., (1991) Engl. J. Med., 324, p. 1385
Man, J.W., Ahn, S.H., Park, S.H., Wang, S.Y., Bae, G.U., Seo, D.W., Known, H.K., Lee, H.W., Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin (2000) Cancer Res., 60, pp. 6068-6074
Shute, R.E., Dunlap, B., Rich, D.H., Analogues of the cytostatic and antimitogenic agents chlamydocin and HC-toxin: Synthesis and biological activity of chloromethyl ketone and diazomethyl ketone functionalized cyclic tetrapeptides (1987) J. Med. Chem., 30, pp. 71-78
Diana, G.D., McKinlay, M.A., Otto, M.J., Akullian, V., Oglesby, C., [[(4,5-Dihydro-2-oxazolyl)phenoxy]alkyl]isoxazoles. Inhibitors of picornavirus uncoating (1985) J. Med. Chem., 28, pp. 1906-1910
Ornaghi, P., Rotili, D., Sbardella, G., Mai, A., Filetici, P., A novel Gcn5p inhibitor represses cell growth, gene transcription and histone acetylation in budding yeast (2005) Biochem. Pharmacol., 70, pp. 911-917
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Small-molecule inhibitors of histone acetyltransferase activity: Identification and biological properties
Starting from a yeast phenotypic screening performed on 21 compounds, we described the identification of two small molecules ( 9 and 18) able to significantly reduce the S. cerevisiae cell growth, thus miming the effect of GCN5 deletion mutant. Tested on a GCN5-dependent gene transcription assay, compounds 9 and 18 gave a high reduction of the reporter activity. In S. cerevisiae histone H3 terminal tails assay, the H3 acetylation levels were highly reduced by treatment with 0.6-1 mM 9, while 18 was effective only at 1.5 mM. In human leukemia U937 cell line, at 1 mM 9 and 18 showed effects on cell cycle ( arrest in G1 phase, 9), apoptosis ( 9), and granulocytic differentiation ( 18). When tested on U937 cell nuclear extracts to evaluate their histone acetyltransferase ( HAT) inhibitory action, both compounds were able to reduce the enzyme activity when used at 500 AM. Another quinoline, compound 22, was synthesized with the aim to improve the activity observed with 9 and 18. Tested in the HAT assay, 22 was able to reduce the HAT catalytic action at 50 and 25 AM, thereby being comparable to anacardic acid, curcumin, and MB- 3 used as references. Finally, in U937 cells, compounds 9 and 18 used at 2.5 mM were able to reduce the extent of the acetylation levels of histone H3 ( 9) and alpha-tubulin ( 9 and 18). In the same assay, 22 at lower concentration ( 100 AM) showed the same hypoacetylating effects with both histone and non-histone substrates.
Starting from a yeast phenotypic screening performed on 21 compounds, we described the identification of two small molecules ( 9 and 18) able to significantly reduce the S. cerevisiae cell growth, thus miming the effect of GCN5 deletion mutant. Tested on a GCN5-dependent gene transcription assay, compounds 9 and 18 gave a high reduction of the reporter activity. In S. cerevisiae histone H3 terminal tails assay, the H3 acetylation levels were highly reduced by treatment with 0.6-1 mM 9, while 18 was effective only at 1.5 mM. In human leukemia U937 cell line, at 1 mM 9 and 18 showed effects on cell cycle ( arrest in G1 phase, 9), apoptosis ( 9), and granulocytic differentiation ( 18). When tested on U937 cell nuclear extracts to evaluate their histone acetyltransferase ( HAT) inhibitory action, both compounds were able to reduce the enzyme activity when used at 500 AM. Another quinoline, compound 22, was synthesized with the aim to improve the activity observed with 9 and 18. Tested in the HAT assay, 22 was able to reduce the HAT catalytic action at 50 and 25 AM, thereby being comparable to anacardic acid, curcumin, and MB- 3 used as references. Finally, in U937 cells, compounds 9 and 18 used at 2.5 mM were able to reduce the extent of the acetylation levels of histone H3 ( 9) and alpha-tubulin ( 9 and 18). In the same assay, 22 at lower concentration ( 100 AM) showed the same hypoacetylating effects with both histone and non-histone substrates.
Small-molecule inhibitors of histone acetyltransferase activity: Identification and biological properties
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Small-molecule inhibitors of histone acetyltransferase activity: Identification and biological properties
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* Molecular mechanism of the inhibition of cytochrome c aggregation by Phe-Gly (509 views)
Arch Bioch Bioph (ISSN: 0003-9861, 0003-9861linking), 2005 Mar 1; 435(1): 182-189.
Impact Factor: 3.152
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Paesano N, Marzocco S, Vicidomini C, Saturnino C, Autore G, De Martino G, Sbardella G
* Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS (433 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 Feb 1; 15(3): 539-543.
Impact Factor: 2.478
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Mischiati C, Sereni A, Finotti A, Breda L, Cortesi R, Nastruzzi C, Romanelli A, Saviano M, Bianchi N, Pedone C, Borgatti M, Gambari R
* Complexation to cationic microspheres of double-stranded peptide nucleic acid-DNA chimeras exhibiting decoy activity (361 views)
Journal Of Biomedical Science (ISSN: 1021-7770), 2004 Sep; 11(5): 697-704.
Impact Factor: 1.567
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De Luca S, Ulhaq S, Dixon M J, EssexJ, Bradley M
* Solid-phase synthesis of a focused library of trypanothione reductase inhibitors (375 views)
Tetrahedron Lett (ISSN: 0040-4039), 2003 Apr 7; 44(15): 3195-3197.
Impact Factor: 2.326
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Leosco D, Iaccarino G, Cipolletta E, De Santis D, Pisani E, Trimarco V, Ferrara N, Abete P, Sorriento D, Rengo F, Trimarco B
* Exercise restores β-adrenergic vasorelaxation in aged rat carotid arteries (332 views)
Am J Physiol Heart Circ Physiol American Journal Of Physiology Heart And Circulatory Physiology (ISSN: 0363-6135), 2003; 285(154-1): H369-H369.
Impact Factor: 3.658
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Borgatti M, Romanelli A, Saviano M, Pedone C, Lampronti I, Breda L, Nastruzzi C, Bianchi N, Mischiati C, Gambari R
* Resistance of decoy PNA-DNA chimeras to enzymatic degradation in cellular extracts and serum (372 views)
Oncology Research (ISSN: 0965-0407), 2003; 13(5): 279-287.
Impact Factor: 1.794
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Caliendo G, Fiorino F, Grieco P, Perissutti E, De Luca S, Giuliano A, Santelli G, Califano D, Severino B, Santagada V
Synthesis and biological activity of pseudopeptides inhibitors of Ras farnesyl transferase containing unconventional amino acids (533 views)
Farmaco (ISSN: 0014-827x), 1999 Nov; 54(11-12): 785-790.
Impact Factor: 0.406
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Morisco C, Cuocolo A, Romano M, Nappi A, Iaccarino G, Volpe M, Salvatore M, Trimarco B
Influence of digitalis on left ventricular functional response to exercise in congestive heart failure (399 views)
Am J Cardiol (ISSN: 0002-9149), 1996 Mar 1; 77(7): 480-485.
Impact Factor: 2.402
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Wink DA, Hanbauer I, Grisham MB, Laval F, Nims RW, Laval J, Cook J, Pacelli R, Liebmann J, Krishna M, Ford PC, Mitchell JB
Chemical biology of nitric oxide: Regulation and protective and toxic mechanisms (661 views)
Current Topics In Cellular Regulation (ISSN: 0070-2137), 1996; 34: 159-187.
Impact Factor: 4.375
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Morisco C, Argenziano L, Sarno D, Cuocolo A, Romano M, Trimarco B
The practical aspects of treatment in heart failure (343 views)
Ann Ital Med Int (ISSN: 0393-9340), 1993 Oct; 8Suppl: 14S-19S.
Impact Factor: 0
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* Interference of Polydatin/Resveratrol in the ACE2: Spike Recognition during COVID-19 Infection. A Focus on Their Potential Mechanism of Action through Computational and Biochemical Assays (15 views)
Biomolecules (ISSN: 2218-273xlinking), 2021 Jul 16; 11(7): N/D-N/D.
Impact Factor: 4.57
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Gogliettino M, Cocca E, Sandomenico A, Gratino L, Iaccarino E, Calvanese L, Rossi M, Palmieri G
* Selective inhibition of acylpeptide hydrolase in SAOS-2 osteosarcoma cells: is this enzyme a viable anticancer target? (20 views)
Mol Biol Rep (ISSN: 0301-4851linking), 2021 Feb; 48(2): 1505-1519.
Impact Factor: 2.316
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Supuran CT, Alterio V, Di Fiore A, D'Ambrosio K, Carta F, Monti SM, De Simone G
* Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: Three for the price of one (530 views)
Med Res Rev (ISSN: 1098-1128electronic, 0198-6325linking), 2018 Sep; 38(6): 1799-1836.
Impact Factor: 8.29
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De Simone G, D'Ambrosio K
* Recent Advances in the Development of New Therapeutic Tools Against Major Parasitic Diseases (255 views)
Curr Med Chem (ISSN: 0929-8673linking, 1875-533xelectronic), 2018; 25(39): 5238-5238.
Impact Factor: 4.63
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Marchiori MF, Riul TB, Oliveira Bortot L, Andrade P, Junqueira GG, Foca G, Doti N, Ruvo M, Dias-baruffi M, Carvalho I, Campo VL
* Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion (1018 views)
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Impact Factor: 2.881
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Deplano A, Morgillo CM, Demurtas M, Bjorklund E, Cipriano M, Svensson M, Hashemian S, Smaldone G, Pedone E, Luque FJ, Cabiddu MG, Novellino E, Fowler CJ, Catalanotti B, Onnis V
* Novel propanamides as fatty acid amide hydrolase inhibitors (326 views)
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Impact Factor: 4.816
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Pirone L, Ripoll-rozada J, Leone M, Ronca R, Lombardo F, Fiorentino G, Andersen JF, Pereira PJB, Arcà B, Pedone E
* Functional analyses yield detailedinsight into the mechanism of thrombin inhibition by the antihemostatic salivary protein cE5 from Anopheles gambiae (367 views) (PDF 190 views)
Jbc Papers (ISSN: 0021-9258linking, 1083-351x), 2017 Jul 28; 292(30): 12632-12642.
Impact Factor: 4.125
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Saccà F, Puorro G, Brunetti A, Capasso G, Cervo A, Cocozza S, De Leva M, Marsili A, Pane C, Quarantelli M, Russo CV, Trepiccione F, De Michele G, Filla A, Morra VB
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J Neurol (ISSN: 0340-5354, 1432-1459, 0340-5354print), 2015 Jan; 262(1): 149-153.
Impact Factor: 3.408
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Merlo S, Basile L, Giuffrida ML, Sortino MA, Guccione S, Copani A
* Identification of 5-Methoxyflavone as a Novel DNA Polymerase-Beta Inhibitor and Neuroprotective Agent against Beta-Amyloid Toxicity (323 views)
J Nat Prod (ISSN: 0163-3864), 2015; 78(11): 2704-2711.
Impact Factor: 3.662
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Sandomenico A, Celentano V, D'Andrea LD, Palmieri G, Ruvo M
* Screening of beta-hairpin peptide-engrafted 1, 2, 3-triazoles to identify APEH enzyme inhibitors (411 views)
Rsc Adv (ISSN: 2046-2069), 2015; 5(13): 9965-9972.
Impact Factor: 3.289
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Petretta M, Cuocolo A
Letter by Petretta and Cuocolo regarding article, "Four-variable risk model in men and women with heart failure" (299 views)
Circ-Heart Fail (ISSN: 1941-3289), 2014 Mar 1; 7(2): 380-380.
Impact Factor: 5.867
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D'Ambrosio K, Lopez M, Dathan NA, Ouahrani-bettache S, Köhler S, Ascione G, Monti SM, Winum JY, De Simone G
* Structural basis for the rational design of new anti-Brucella agents: The crystal structure of the C366S mutant of l-histidinol dehydrogenase from Brucella suis (453 views)
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Impact Factor: 2.963
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Rami M, Dubois L, Parvathaneni NK, Alterio V, van Kuijk SJ, Monti SM, Lambin P, De Simone G, Supuran CT, Winum JY
* Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates (546 views)
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Impact Factor: 5.48
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Squeglia F, Romano M, Ruggiero A, Vitagliano L, De Simone A, Berisio R
* Carbohydrate recognition by RpfB from mycobacterium tuberculosis unveiled by crystallographic and molecular dynamics analyses (441 views)
Biophysical Journal (ISSN: 0006-3495, 1542-0086), 2013 Jun 4; 104(11): 2530-2539.
Impact Factor: 3.832
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Monti SM, De Simone G, Dathan NA, Ludwig M, Vullo D, Scozzafava A, Capasso C, Supuran CT
* Kinetic And Anion Inhibition Studies Of A Beta-Carbonic Anhydrase (fbica 1) From The C-4 Plant Flaveria Bidentis (440 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2013 Mar 15; 23(6): 1626-1630.
Impact Factor: 2.331
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Calce E, Monfregola L, Sandomenico A, Saviano M, De Luca S
* Fluorescence study for selecting specific ligands toward HER2 receptor: An example of receptor fragment approach (438 views)
Eur J Med Chem (ISSN: 0223-5234, 1768-3254, 1768-3254electronic), 2013 Mar; 61: 116-121.
Impact Factor: 3.432
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Ruggiero A, Marchant J, Squeglia F, Makarov V, De Simone A, Berisio R
* Molecular determinants of inactivation of the resuscitation promoting factor B from Mycobacterium tuberculosis (408 views)
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Impact Factor: 2.983
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Scalia M, Satriano C, Greca R, Stella AM, Rizzarelli E, Spina-Purrello V
* PARP-1 inhibitors DPQ and PJ-34 negatively modulate proinflammatory commitment of human glioblastoma cells (422 views)
Neurochemical Research (ISSN: 1573-6903, 0364-3190), 2013 Jan; 38(1): 50-58.
Impact Factor: 2.551
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Berisio R
* Editorial: cell processes in bacterial diseases (409 views)
Protein Pept Lett (ISSN: 0929-8665, 1875-5305), 2012 Oct; 19(10): 1011-1012.
Impact Factor: 1.994
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Kaprelyants AS, Mukamolova GV, Ruggiero A, Makarov VA, Demina GR, Shleeva MO, Potapov VD, Shramko PA
* Resuscitation-promoting Factors (Rpf): In Search of Inhibitors (495 views)
Protein Pept Lett (ISSN: 0929-8665, 1875-5305), 2012 Oct; 19(10): 1026-1034.
Impact Factor: 1.994
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Santoro AM, Lo Giudice MC, D'Urso A, Lauceri R, Purrello R, Milardi D
* Cationic porphyrins are reversible proteasome inhibitors (446 views)
J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 2012 Jun 27; 134(25): 10451-10457.
Impact Factor: 10.677
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De Simone G, Supuran CT
* (In)organic anions as carbonic anhydrase inhibitors (378 views)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 2012 Jun; 111: 117-129.
Impact Factor: 3.197
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Sandomenico A, Russo A, Palmieri G, Bergamo P, Gogliettino M, Falcigno L, Ruvo M
* Small peptide inhibitors of acetyl-peptide hydrolase having an uncommon mechanism of inhibition and a stable bent conformation (520 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012 Mar 8; 55(5): 2102-2111.
Impact Factor: 5.614
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De Simone G
* Editorial: Zinc Metallo-Enzymes As Target For Drug Design (423 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2012 Feb; 19(6): 820-1012.
Impact Factor: 4.07
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Galdiero S, Vitiello M, Finamore E, Mansi R, Galdiero M, Morelli G, Tesauro D
* Activation of monocytic cells by immunostimulatory lipids conjugated to peptide antigens (405 views)
Molecular Biosystems (ISSN: 1742-206x), 2012; 8(12): 3166-3177.
Impact Factor: 3.35
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Folgiero V, Di Carlo SE, Bossi G, Spugnini E, Di Benedetto A, Bon G, Milella M, Fabi A, Accardo A, Morelli G, Mottolese M, Falcioni R
* Inhibition of p85, the non-catalytic subunit of phosphatidylinositol 3-kinase, exerts potent antitumor activity in human breast cancer cells (516 views)
Cell Death & (ISSN: 2041-4889, 2041-4889electronic), 2012; 3(12): N/D-N/D.
Impact Factor: 6.044
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Castellano I, Merlino A
* γ-glutamyltranspeptidases: Sequence, structure, biochemical properties, and biotechnological applications (422 views)
Cell Mol Life Sci (ISSN: 1420-682x), 2012; 69(20): 3381-3394.
Impact Factor: 5.615
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Janda E, Palmieri C, Pisano A, Pontoriero M, Iaccino E, Falcone C, Fiume G, Gaspari M, Nevolo M, Di Salle E, Rossi A, De Laurentiis A, Greco A, Di Napoli D, Verheij E, Britti D, Lavecchia L, Quinto I, Scala G
* Btk regulation in human and mouse B cells via protein kinase C phosphorylation of IBtkγ (451 views)
Blood (ISSN: 0006-4971, 0006-6497, 0390-6078), 2011 Jun 16; 117(24): 6520-6531.
Impact Factor: 9.898
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Milite C, Castellano S, Benedetti R, Tosco A, Ciliberti C, Vicidomini C, Boully L, Franci G, Altucci L, Mai A, Sbardella G
* Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs) (360 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2011 Jun 15; 19(12): 3690-3701.
Impact Factor: 2.921
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Langella E, Pierre S, Ghattas W, Giorgi M, Réglier M, Saviano M, Esposito L, Hardré R
* Probing The Peptidylglycine Alpha-Hydroxylating Monooxygenase Active Site With Novel 4-Phenyl-3-Butenoic Acid Based Inhibitors (420 views)
Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2010 Sep 3; 5(9): 1568-1576.
Impact Factor: 3.306
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Giuffrida ML, Caraci F, Pignataro B, Cataldo S, De Bona P, Bruno V, Molinaro G, Pappalardo G, Messina A, Palmigiano A, Garozzo D, Nicoletti F, Rizzarelli E, Copani A
* Beta-Amyloid Monomers Are Neuroprotective (659 views)
J Neurosci (ISSN: 1529-2401, 0270-6474), 2009 Sep 26; 29(34): 10582-10587.
Impact Factor: 3.669
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Alterio V, Hilvo M, Di Fiore A, Supuran CT, Pan P, Parkkila S, Scaloni A, Pastorek J, Pastorekova S, Pedone C, Scozzafava A, Monti SM, De Simone G
* Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (561 views)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 2009 Sep 22; 106(38): 16233-16238.
Impact Factor: 9.432
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De Simone G, Scozzafava A, Supuran CT
* Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (352 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
Impact Factor: 2.473
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Di Fiore A, Monti SM, Hilvo M, Parkkila S, Romano V, Scaloni A, Pedone C, Scozzafava A, Supuran CT, De Simone G
* Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide (527 views)
Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
Impact Factor: 3.085
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Chiechio S, Zammataro M, Morales ME, Busceti CL, Drago F, Th Gereau RW, Copani A, Nicoletti F
* Epigenetic modulation of mGlu2 receptors by histone deacetylase inhibitors in the treatment of inflammatory pain (452 views)
Mol Pharmacol (ISSN: 0026-895x), 2009; 75(5): 1014-1020.
Impact Factor: 4.531
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Woo LWL, Fischer DS, Sharland CM, Trusselle M, Foster PA, Chander SK, Di Fiore A, Supuran CT, De Simone G, Purohit A, Reed MJ, Potter BVL
* Anticancer steroid sulfatase inhibitors: synthesis of a potent fluorinated second-generation agent, in vitro and in vivo activities, molecular modeling, and protein crystallography (644 views)
Mol Cancer Ther (ISSN: 1535-7163, 1538-8514electronic), 2008 Sep; 7(8): 2435-2444.
Impact Factor: 5.003
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Sbardella G, Castellano S, Vicidomini C, Rotili D, Nebbioso A, Miceli M, Altucci L, Mai A
* Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases (313 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 May 1; 18(9): 2788-2792.
Impact Factor: 2.531
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Ragno R, Simeoni S, Castellano S, Vicidomini C, Mai A, Caroli A, Tramontano A, Bonaccini C, Trojer P, Bauer I, Brosch G, Sbardella G
* Small molecule inhibitors of histone arginine methyltransferases: Homology modeling, molecular docking, binding mode analysis, and biological evaluations (752 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2007 Mar 22; 50(6): 1241-1253.
Impact Factor: 4.895
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Di Fiore A, Scozzafava A, Winum JY, Montero JL, Pedone C, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: binding of an antiglaucoma glycosyl-sulfanilamide derivative to human isoform II and its consequences for the drug design of enzyme inhibitors incorporating sugar moieties (410 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Mar 15; 17(6): 1726-1731.
Impact Factor: 2.604
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Menchise V, De Simone G, Di Fiore A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystallographic studies for the binding of 5-amino-1, 3, 4-thiadiazole-2-sulfonamide and 5-(4-amino-3-chloro-5-fluorophenylsulfonamido)1, 3, 4-thiadiazole-2-sulfon amide to human isoform II (310 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Dec 15; 16(24): 6204-6208.
Impact Factor: 2.538
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Cappiello M, Alterio V, Amodeo P, Del Corso A, Scaloni A, Pedone C, Moschini R, De Donatis GM, De Simone G, Mura U
* A new spot test for sulfhydryl-containing compounds (450 views)
Anal Biochem, 2006 Mar 14; 79(1-2): 610-611.
Impact Factor: 2.305
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Cappiello M, Alterio V, Amodeo P, Del Corso A, Scaloni A, Pedone C, Moschini R, De Donatis GM, De Simone G, Mura U
* Metal ion substitution in the catalytic site greatly affects the binding of sulfhydryl-containing compounds to leucyl aminopeptidase (723 views)
Biochemistry (ISSN: 0006-2960, 1520-4995, 1520-4995electronic), 2006 Mar 14; 45(10): 3226-3234.
Impact Factor: 3.633
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Cuocolo A, Acampa W, Varrone A, Salvatore M
* Highlights of the Annual Congress of the European Association of Nuclear Medicine, Istanbul, 2005: The incremental value of nuclear medicine for patient management and care (584 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2006 Mar; 33(3): 360-381.
Impact Factor: 4.041
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Grasso G, D'Agata R, Rizzarelli E, Spoto G, D'Andrea LD, Pedone C, Picardi A, Romanelli A, Fragai M, Yeo KJ
* Activity of anchored human matrix metalloproteinase-1 catalytic domain on Au(111) surfaces monitored by ESI-MS (575 views)
J Mass Spectrom (ISSN: 1076-5174, 1096-9888), 2005 Dec; 40(12): 1565-1571.
Impact Factor: 3.574
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Naddeo M, Vitagliano L, Russo A, Gotte G, D'Alessio G, Sorrentino S
* Interactions of the cytotoxic RNase A dimers with the cytosolic ribonuclease inhibitor (362 views)
Febs Lett (ISSN: 0014-5793, 0014-5793print, 1873-3468electronic), 2005 May 9; 579(12): 2663-2668.
Impact Factor: 3.415
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Cozzolino R, Palladino P, Rossi F, Cali G, Benedetti E, Laccetti P
* Antineoplastic cyclic astin analogues kill tumour cells via caspase-mediated induction of apoptosis (524 views)
Carcinogenesis (ISSN: 0143-3334), 2005 Apr; 26(4): 733-739.
Impact Factor: 5.108
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La Rosa C, Milardi D, Amato E, Pappalardo M, Grasso D
* Molecular mechanism of the inhibition of cytochrome c aggregation by Phe-Gly (509 views)
Arch Bioch Bioph (ISSN: 0003-9861, 0003-9861linking), 2005 Mar 1; 435(1): 182-189.
Impact Factor: 3.152
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Paesano N, Marzocco S, Vicidomini C, Saturnino C, Autore G, De Martino G, Sbardella G
* Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS (433 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 Feb 1; 15(3): 539-543.
Impact Factor: 2.478
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Mischiati C, Sereni A, Finotti A, Breda L, Cortesi R, Nastruzzi C, Romanelli A, Saviano M, Bianchi N, Pedone C, Borgatti M, Gambari R
* Complexation to cationic microspheres of double-stranded peptide nucleic acid-DNA chimeras exhibiting decoy activity (361 views)
Journal Of Biomedical Science (ISSN: 1021-7770), 2004 Sep; 11(5): 697-704.
Impact Factor: 1.567
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De Luca S, Ulhaq S, Dixon M J, EssexJ, Bradley M
* Solid-phase synthesis of a focused library of trypanothione reductase inhibitors (375 views)
Tetrahedron Lett (ISSN: 0040-4039), 2003 Apr 7; 44(15): 3195-3197.
Impact Factor: 2.326
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Leosco D, Iaccarino G, Cipolletta E, De Santis D, Pisani E, Trimarco V, Ferrara N, Abete P, Sorriento D, Rengo F, Trimarco B
* Exercise restores β-adrenergic vasorelaxation in aged rat carotid arteries (332 views)
Am J Physiol Heart Circ Physiol American Journal Of Physiology Heart And Circulatory Physiology (ISSN: 0363-6135), 2003; 285(154-1): H369-H369.
Impact Factor: 3.658
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Borgatti M, Romanelli A, Saviano M, Pedone C, Lampronti I, Breda L, Nastruzzi C, Bianchi N, Mischiati C, Gambari R
* Resistance of decoy PNA-DNA chimeras to enzymatic degradation in cellular extracts and serum (372 views)
Oncology Research (ISSN: 0965-0407), 2003; 13(5): 279-287.
Impact Factor: 1.794
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Caliendo G, Fiorino F, Grieco P, Perissutti E, De Luca S, Giuliano A, Santelli G, Califano D, Severino B, Santagada V
Synthesis and biological activity of pseudopeptides inhibitors of Ras farnesyl transferase containing unconventional amino acids (533 views)
Farmaco (ISSN: 0014-827x), 1999 Nov; 54(11-12): 785-790.
Impact Factor: 0.406
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Morisco C, Cuocolo A, Romano M, Nappi A, Iaccarino G, Volpe M, Salvatore M, Trimarco B
Influence of digitalis on left ventricular functional response to exercise in congestive heart failure (399 views)
Am J Cardiol (ISSN: 0002-9149), 1996 Mar 1; 77(7): 480-485.
Impact Factor: 2.402
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Wink DA, Hanbauer I, Grisham MB, Laval F, Nims RW, Laval J, Cook J, Pacelli R, Liebmann J, Krishna M, Ford PC, Mitchell JB
Chemical biology of nitric oxide: Regulation and protective and toxic mechanisms (661 views)
Current Topics In Cellular Regulation (ISSN: 0070-2137), 1996; 34: 159-187.
Impact Factor: 4.375
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Morisco C, Argenziano L, Sarno D, Cuocolo A, Romano M, Trimarco B
The practical aspects of treatment in heart failure (343 views)
Ann Ital Med Int (ISSN: 0393-9340), 1993 Oct; 8Suppl: 14S-19S.
Impact Factor: 0
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56 Records (55 excluding Abstracts).
Total impact factor: 215.101 (209.057 excluding Abstracts).
Total 5 year impact factor: 205.229 (199.185 excluding Abstracts).
Total impact factor: 215.101 (209.057 excluding Abstracts).
Total 5 year impact factor: 205.229 (199.185 excluding Abstracts).
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