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inhibition of histone deacetylase activity, resulting in prevention of interferon gamma-induced Janus kinase 1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation
inhibition of histone deacetylase activity, resulting in prevention of interferon gamma-induced Janus kinase 1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation
inhibition of histone deacetylase activity, resulting in prevention of interferon gamma-induced Janus kinase 1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation
inhibition of histone deacetylase activity, resulting in prevention of interferon gamma-induced Janus kinase 1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation
inhibition of histone deacetylase activity, resulting in prevention of interferon gamma-induced Janus kinase 1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation
inhibition of histone deacetylase activity, resulting in prevention of interferon gamma-induced Janus kinase 1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation
inhibition of histone deacetylase activity, resulting in prevention of interferon gamma-induced Janus kinase 1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation
SAHA, vorinostat, zolinza, broad-spectrum or pan-HDAC inhibitor
SAHA, vorinostat, zolinza, broad-spectrum or pan-HDAC inhibitor
SAHA, vorinostat, zolinza, broad-spectrum or pan-HDAC inhibitor
SAHA, vorinostat, zolinza, broad-spectrum or pan-HDAC inhibitor
SAHA, vorinostat, zolinza, broad-spectrum or pan-HDAC inhibitor
SAHA, vorinostat, zolinza, broad-spectrum or pan-HDAC inhibitor
SAHA, vorinostat, zolinza, broad-spectrum or pan-HDAC inhibitor
SAHA, synthetic inhibitor
SAHA, synthetic inhibitor
SAHA, synthetic inhibitor
SAHA, synthetic inhibitor
SAHA, synthetic inhibitor
SAHA, synthetic inhibitor
SAHA, synthetic inhibitor
SAHA; SAHA; SAHA; SAHA; SAHA
SAHA; SAHA; SAHA; SAHA; SAHA
SAHA; SAHA; SAHA; SAHA; SAHA
SAHA; SAHA; SAHA; SAHA; SAHA
SAHA; SAHA; SAHA; SAHA; SAHA
SAHA; SAHA; SAHA; SAHA; SAHA
SAHA; SAHA; SAHA; SAHA; SAHA
i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively
i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively
i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively
i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively
i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively
i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively
i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively
; complete inhibition; complete inhibition
; complete inhibition; complete inhibition
; complete inhibition; complete inhibition
; complete inhibition; complete inhibition
; complete inhibition; complete inhibition
; complete inhibition; complete inhibition
; complete inhibition; complete inhibition
-
678192, 681276, 681304, 682501, 696716, 700547, 712181, 712485, 713087, 733081, 733817
-
678192, 681276, 681304, 682501, 696716, 700547, 712181, 712485, 713087, 733081, 733817
-
678192, 681276, 681304, 682501, 696716, 700547, 712181, 712485, 713087, 733081, 733817
-
678192, 681276, 681304, 682501, 696716, 700547, 712181, 712485, 713087, 733081, 733817
-
678192, 681276, 681304, 682501, 696716, 700547, 712181, 712485, 713087, 733081, 733817
-
678192, 681276, 681304, 682501, 696716, 700547, 712181, 712485, 713087, 733081, 733817
-
678192, 681276, 681304, 682501, 696716, 700547, 712181, 712485, 713087, 733081, 733817
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
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A new amidohydrolase from Bordetella or Alcaligenes strain FB188 with similarities to histone deacetylases
2004
Hildmann, C.; Ninkovic, M.; Dietrich, R.; Wegener, D.; Riester, D.; Zimmermann, T.; Birch, O.M.; Bernegger, C.; Loidl, P.; Schwienhorst, A.
J. Bacteriol.
186
2328-2339
Catalytic activity and inhibition of human histone deacetylase 8 is dependent on the identity of the active site metal ion
2006
Gantt, S.L.; Gattis, S.G.; Fierke, C.A.
Biochemistry
45
6170-6178
Requirement of histone deacetylase activity for signaling by STAT1
2004
Klampfer, L.; Huang, J.; Swaby, L.A.; Augenlicht, L.
J. Biol. Chem.
279
30358-30368
Novel Inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates
2005
Suzuki, T.; Nagano, Y.; Kouketsu, A.; Matsuura, A.; Maruyama, S.; Kurotaki, M.; Nakagawa, H.; Miyata, N.
J. Med. Chem.
48
1019-1032
Design and synthesis of a potent histone deacetylase inhibitor
2007
Liu, T.; Kapustin, G.; Etzkorn, F.A.
J. Med. Chem.
50
2003-2006
Crystal structure of a eukaryotic zinc-dependent histone deacetylase, human HDAC8, complexed with a hydroxamic acid inhibitor
2004
Vannini, A.; Volpari, C.; Filocamo, G.; Casavola, E.C.; Brunetti, M.; Renzoni, D.; Chakravarty, P.; Paolini, C.; De Francesco, R.; Gallinari, P.; Steinkuhler, C.; Di Marco, S.
Proc. Natl. Acad. Sci. USA
101
15064-15069
Structural studies of human histone deacetylase 8 and its site-specific variants complexed with substrate and inhibitors
2008
Dowling, D.P.; Gantt, S.L.; Gattis, S.G.; Fierke, C.A.; Christianson, D.W.
Biochemistry
47
13554-13563
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities
2008
Mai, A.; Perrone, A.; Nebbioso, A.; Rotili, D.; Valente, S.; Tardugno, M.; Massa, S.; De Bellis, F.; Altucci, L.
Bioorg. Med. Chem. Lett.
18
2530-2535
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: Design, synthesis, SAR studies, and in vivo antitumor activity
2009
Wang, H.; Yu, N.; Song, H.; Chen, D.; Zou, Y.; Deng, W.; Lye, P.L.; Chang, J.; Ng, M.; Sun, E.T.; Sangthongpitag, K.; Wang, X.; Wu, X.; Khng, H.H.; Fang, L.; Goh, S.K.; Ong, W.C.; Bonday, Z.; Stuenkel, W.; Poulsen, A.; Entzeroth, M.
Bioorg. Med. Chem. Lett.
19
1403-1408
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group
2008
Chen, P.C.; Patil, V.; Guerrant, W.; Green, P.; Oyelere, A.K.
Bioorg. Med. Chem.
16
4839-4853
Isoform-specific histone deacetylase inhibitors: The next step?
2009
Balasubramanian, S.; Verner, E.; Buggy, J.J.
Cancer Lett.
280
211-221
Synthesis, structural characterization and biological evaluation of N-protected cyclopropylethylcarbamates as potential histone deacetylase inhibitor
2008
Jung, J.C.; Moon, H.I.; Oh, S.
Chem. Biol. Drug Des.
72
592-595
Modulation of histone deacetylase activity by dietary isothiocyanates and allyl sulfides: studies with sulforaphane and garlic organosulfur compounds
2009
Nian, H.; Delage, B.; Ho, E.; Dashwood, R.H.
Environ. Mol. Mutagen.
50
213-221
Design, synthesis, biological evaluation, and structural characterization of potent histone deacetylase inhibitors based on cyclic alpha/beta-tetrapeptide architectures
2009
Montero, A.; Beierle, J.M.; Olsen, C.A.; Ghadiri, M.R.
J. Am. Chem. Soc.
131
3033-3041
Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity
2008
Schuetz, A.; Min, J.; Allali-Hassani, A.; Schapira, M.; Shuen, M.; Loppnau, P.; Mazitschek, R.; Kwiatkowski, N.P.; Lewis, T.A.; Maglathin, R.L.; McLean, T.H.; Bochkarev, A.; Plotnikov, A.N.; Vedadi, M.; Arrowsmith, C.H.
J. Biol. Chem.
283
11355-11363
Simple inhibitors of histone deacetylase activity that combine features of short-chain fatty acid and hydroxamic acid inhibitors
2008
Tischler, J.L.; Abuaita, B.; Cuthpert, S.C.; Fage, C.; Murphy, K.; Saxe, A.; Furr, E.B.; Hedrick, J.; Meyers, J.; Snare, D.; Zand, A.R.
J. Enzyme Inhib. Med. Chem.
23
549-555
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo
2008
Jones, P.; Altamura, S.; De Francesco, R.; Paz, O.G.; Kinzel, O.; Mesiti, G.; Monteagudo, E.; Pescatore, G.; Rowley, M.; Verdirame, M.; Steinkuehler, C.
J. Med. Chem.
51
2350-2353
Residues in the 11 A channel of histone deacetylase 1 promote catalytic activity: implications for designing isoform-selective histone deacetylase inhibitors
2008
Weerasinghe, S.V.; Estiu, G.; Wiest, O.; Pflum, M.K.
J. Med. Chem.
51
5542-5551
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum
2009
Patel, V.; Mazitschek, R.; Coleman, B.; Nguyen, C.; Urgaonkar, S.; Cortese, J.; Barker, R.H.; Greenberg, E.; Tang, W.; Bradner, J.E.; Schreiber, S.L.; Duraisingh, M.T.; Wirth, D.F.; Clardy, J.
J. Med. Chem.
52
2185-2187
Enhanced histone deacetylase enzyme activity in primary myelofibrosis
2008
Wang, J.C.; Chen, C.; Dumlao, T.; Naik, S.; Chang, T.; Xiao, Y.Y.; Sominsky, I.; Burton, J.
Leuk. Lymphoma
49
2321-2327
Specific activity of class II histone deacetylases in human breast cancer cells
2008
Duong, V.; Bret, C.; Altucci, L.; Mai, A.; Duraffourd, C.; Loubersac, J.; Harmand, P.O.; Bonnet, S.; Valente, S.; Maudelonde, T.; Cavailles, V.; Boulle, N.
Mol. Cancer Res.
6
1908-1919
Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold
2009
Bowers, A.A.; West, N.; Newkirk, T.L.; Troutman-Youngman, A.E.; Schreiber, S.L.; Wiest, O.; Bradner, J.E.; Williams, R.M.
Org. Lett.
11
1301-1304
Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor
2009
Hoffman, H.E.; Jiraskova, J.; Cigler, P.; Sanda, M.; Schraml, J.; Konvalinka, J.
J. Med. Chem.
52
6032-6041
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity
2010
Chetan, B.; Bunha, M.; Jagrat, M.; Sinha, B.N.; Saiko, P.; Graser, G.; Szekeres, T.; Raman, G.; Rajendran, P.; Moorthy, D.; Basu, A.; Jayaprakash, V.
Bioorg. Med. Chem. Lett.
20
3906-3910
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies
2009
Bora-Tatar, G.; Dayangac-Erden, D.; Demir, A.S.; Dalkara, S.; Yelekci, K.; Erdem-Yurter, H.
Bioorg. Med. Chem.
17
5219-5228
Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel histone deacetylases (HDACs) inhibitors
2010
Zhang, Y.; Feng, J.; Liu, C.; Zhang, L.; Jiao, J.; Fang, H.; Su, L.; Zhang, X.; Zhang, J.; Li, M.; Wang, B.; Xu, W.
Bioorg. Med. Chem.
18
1761-1772
Type-specific roles of histone deacetylase (HDAC) overexpression in ovarian carcinoma: HDAC1 enhances cell proliferation and HDAC3 stimulates cell migration with downregulation of E-cadherin
2010
Hayashi, A.; Horiuchi, A.; Kikuchi, N.; Hayashi, T.; Fuseya, C.; Suzuki, A.; Konishi, I.; Shiozawa, T.
Int. J. Cancer
127
1332-1346
Activation and inhibition of histone deacetylase 8 by monovalent cations
2010
Gantt, S.L.; Joseph, C.G.; Fierke, C.A.
J. Biol. Chem.
285
6036-6043
Inhibition of histone deacetylase 10 induces thioredoxin-interacting protein and causes accumulation of reactive oxygen species in SNU-620 human gastric cancer cells
2010
Lee, J.; Jeong, E.; Choi, M.; Kim, S.; Park, J.; Song, S.; Park, J.; Bang, Y.; Kim, T.
Mol. Cells
30
107-112
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis
2010
Hutt, D.M.; Herman, D.; Rodrigues, A.P.; Noel, S.; Pilewski, J.M.; Matteson, J.; Hoch, B.; Kellner, W.; Kelly, J.W.; Schmidt, A.; Thomas, P.J.; Matsumura, Y.; Skach, W.R.; Gentzsch, M.; Riordan, J.R.; Sorscher, E.J.; Okiyoneda, T.; Yates, J.R.; Lukacs, G.L.; Frizzell, R.A.; Manning, G.; Gottesfeld, J.M.; Balc, B.a.l.c.h.
Nat. Chem. Biol.
6
25-33
Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors
2012
Guan, P.; Sun, F.; Hou, X.; Wang, F.; Yi, F.; Xu, W.; Fang, H.
Bioorg. Med. Chem.
20
3865-3872
Kinetic method for the large-scale analysis of the binding mechanism of histone deacetylase inhibitors
2014
Meyners, C.; Baud, M.G.; Fuchter, M.J.; Meyer-Almes, F.J.
Anal. Biochem.
460
39-46
Functional characterization of Candida albicans Hos2 histone deacetylase
2013
Karthikeyan, G.; Paul-Satyaseela, M.; Dhatchana Moorthy, N.; Gopalaswamy, R.; Narayanan, S.
F1000Res.
2
238
Characterization of the regulation and function of zinc-dependent histone deacetylases during rodent liver regeneration
2013
Huang, J.; Barr, E.; Rudnick, D.A.
Hepatology
57
1742-1751
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response
2012
Wong, J.C.; Tang, G.; Wu, X.; Liang, C.; Zhang, Z.; Guo, L.; Peng, Z.; Zhang, W.; Lin, X.; Wang, Z.; Mei, J.; Chen, J.; Pan, S.; Zhang, N.; Liu, Y.; Zhou, M.; Feng, L.; Zhao, W.; Li, S.; Zhang, C.; Zhang, M.; Rong, Y.; Jin, T.G.; Zhang, X.; Ren, S.; Ji, Y.; Zhao, R.; She, J.; Ren, Y.; Xu, C.; Chen, D.; Cai, J.; Shan, S.
J. Med. Chem.
55
8903-8925
Roles of human UDP-glucuronosyltransferases in clearance and homeostasis of endogenous substrates, and functional implications
2015
Bock, K.W.
Biochem. Pharmacol.
96
77-82
Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
2015
Cholewinski, G.; Iwaszkiewicz-Grzes, D.; Prejs, M.; Glowacka, A.; Dzierzbicka, K.
J. Enzyme Inhib. Med. Chem.
30
550-563