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Items: 1 to 50 of 97

1.

Octreotide Conjugates for Tumor Targeting and Imaging.

Figueras E, Martins A, Borbély A, Le Joncour V, Cordella P, Perego R, Modena D, Pagani P, Esposito S, Auciello G, Frese M, Gallinari P, Laakkonen P, Steinkühler C, Sewald N.

Pharmaceutics. 2019 May 7;11(5). pii: E220. doi: 10.3390/pharmaceutics11050220.

2.

Synthesis and Biological Evaluation of RGD⁻Cryptophycin Conjugates for Targeted Drug Delivery.

Borbély A, Figueras E, Martins A, Esposito S, Auciello G, Monteagudo E, Di Marco A, Summa V, Cordella P, Perego R, Kemker I, Frese M, Gallinari P, Steinkühler C, Sewald N.

Pharmaceutics. 2019 Apr 1;11(4). pii: E151. doi: 10.3390/pharmaceutics11040151.

3.

Synthesis and Biological Evaluation of RGD and isoDGR-Monomethyl Auristatin Conjugates Targeting Integrin αV β3.

Raposo Moreira Dias A, Bodero L, Martins A, Arosio D, Gazzola S, Belvisi L, Pignataro L, Steinkühler C, Dal Corso A, Gennari C, Piarulli U.

ChemMedChem. 2019 May 6;14(9):938-942. doi: 10.1002/cmdc.201900049. Epub 2019 Mar 22.

PMID:
30840356
4.

In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas.

Cazzamalli S, Figueras E, Pethő L, Borbély A, Steinkühler C, Neri D, Sewald N.

ACS Omega. 2018 Nov 30;3(11):14726-14731. doi: 10.1021/acsomega.8b02350. Epub 2018 Nov 2.

5.

[Telematics in ambulatory care: Exploring the nurses' perspective].

Dockweiler C, Diedrich L, Palmdorf S, Beier D, Ilic J, Kibbert M, Kirsch J, Hannemann N, Prisett F, Schmitke V, Schmidt C, Spindeler T, Sommer L, Sommer S, Stark AL, Steinkühler C, Stolte J, Hornberg C.

Pflege. 2019 Apr;32(2):87-96. doi: 10.1024/1012-5302/a000648. Epub 2018 Sep 28. German.

PMID:
30265200
6.

Control of cytokine mRNA degradation by the histone deacetylase inhibitor ITF2357 in rheumatoid arthritis fibroblast-like synoviocytes: beyond transcriptional regulation.

Angiolilli C, Kabala PA, Grabiec AM, Rossato M, Lai WS, Fossati G, Mascagni P, Steinkühler C, Blackshear PJ, Reedquist KA, Baeten DL, Radstake TRDJ.

Arthritis Res Ther. 2018 Jul 20;20(1):148. doi: 10.1186/s13075-018-1638-4.

7.

MK-4101, a Potent Inhibitor of the Hedgehog Pathway, Is Highly Active against Medulloblastoma and Basal Cell Carcinoma.

Filocamo G, Brunetti M, Colaceci F, Sasso R, Tanori M, Pasquali E, Alfonsi R, Mancuso M, Saran A, Lahm A, Di Marcotullio L, Steinkühler C, Pazzaglia S.

Mol Cancer Ther. 2016 Jun;15(6):1177-89. doi: 10.1158/1535-7163.MCT-15-0371. Epub 2016 Mar 9.

8.

Critical role of zinc finger protein 521 in the control of growth, clonogenicity and tumorigenic potential of medulloblastoma cells.

Spina R, Filocamo G, Iaccino E, Scicchitano S, Lupia M, Chiarella E, Mega T, Bernaudo F, Pelaggi D, Mesuraca M, Pazzaglia S, Semenkow S, Bar EE, Kool M, Pfister S, Bond HM, Eberhart CG, Steinkühler C, Morrone G.

Oncotarget. 2013 Aug;4(8):1280-92.

9.

Skin equivalents: a tool for the discovery and validation of pharmacodynamic biomarkers.

Paolini C, Orecchia A, Failla CM, Gallinari P, Zambruno G, Steinkühler C.

Cancer Invest. 2013 Jan;31(1):60-6. doi: 10.3109/07357907.2012.749269.

PMID:
23327193
10.

Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells.

Rotili D, Tarantino D, Nebbioso A, Paolini C, Huidobro C, Lara E, Mellini P, Lenoci A, Pezzi R, Botta G, Lahtela-Kakkonen M, Poso A, Steinkühler C, Gallinari P, De Maria R, Fraga M, Esteller M, Altucci L, Mai A.

J Med Chem. 2012 Dec 27;55(24):10937-47. doi: 10.1021/jm3011614. Epub 2012 Dec 12.

PMID:
23189967
11.

Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells.

Rotili D, Tarantino D, Carafa V, Paolini C, Schemies J, Jung M, Botta G, Di Maro S, Novellino E, Steinkühler C, De Maria R, Gallinari P, Altucci L, Mai A.

J Med Chem. 2012 Sep 27;55(18):8193-7. Epub 2012 Sep 7.

PMID:
22931526
12.

Antibody-drug conjugates in tumor therapy.

Sammet B, Steinkühler C, Sewald N.

Pharm Pat Anal. 2012 Mar;1(1):65-73. doi: 10.4155/ppa.12.4. Review.

PMID:
24236714
13.

Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.

Ontoria JM, Bufi LL, Torrisi C, Bresciani A, Giomini C, Rowley M, Serafini S, Bin H, Hao W, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5274-82. doi: 10.1016/j.bmcl.2011.07.031. Epub 2011 Jul 14.

PMID:
21803580
14.

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.

Muraglia E, Ontoria JM, Branca D, Dessole G, Bresciani A, Fonsi M, Giuliano C, Llauger Bufi L, Monteagudo E, Palumbi MC, Torrisi C, Rowley M, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5283-8. doi: 10.1016/j.bmcl.2011.07.030. Epub 2011 Jul 14.

PMID:
21802943
15.

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.

Malancona S, Altamura S, Filocamo G, Kinzel O, Hernando JI, Rowley M, Scarpelli R, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4422-8. doi: 10.1016/j.bmcl.2011.06.024. Epub 2011 Jun 16.

PMID:
21737272
16.

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.

Kinzel O, Alfieri A, Altamura S, Brunetti M, Bufali S, Colaceci F, Ferrigno F, Filocamo G, Fonsi M, Gallinari P, Malancona S, Hernando JI, Monteagudo E, Orsale MV, Palumbi MC, Pucci V, Rowley M, Sasso R, Scarpelli R, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4429-35. doi: 10.1016/j.bmcl.2011.06.023. Epub 2011 Jun 16.

PMID:
21737263
17.

Histone deacetylase and Cullin3-REN(KCTD11) ubiquitin ligase interplay regulates Hedgehog signalling through Gli acetylation.

Canettieri G, Di Marcotullio L, Greco A, Coni S, Antonucci L, Infante P, Pietrosanti L, De Smaele E, Ferretti E, Miele E, Pelloni M, De Simone G, Pedone EM, Gallinari P, Giorgi A, Steinkühler C, Vitagliano L, Pedone C, Schinin ME, Screpanti I, Gulino A.

Nat Cell Biol. 2010 Feb;12(2):132-42. doi: 10.1038/ncb2013. Epub 2010 Jan 17.

PMID:
20081843
18.

Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.

Ontoria JM, Altamura S, Di Marco A, Ferrigno F, Laufer R, Muraglia E, Palumbi MC, Rowley M, Scarpelli R, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P.

J Med Chem. 2009 Nov 12;52(21):6782-9. doi: 10.1021/jm900555u.

PMID:
19888759
19.

Loss of histone deacetylase 4 causes segregation defects during mitosis of p53-deficient human tumor cells.

Cadot B, Brunetti M, Coppari S, Fedeli S, de Rinaldis E, Dello Russo C, Gallinari P, De Francesco R, Steinkühler C, Filocamo G.

Cancer Res. 2009 Aug 1;69(15):6074-82. doi: 10.1158/0008-5472.CAN-08-2796. Epub 2009 Jul 21.

20.

Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.

Dessole G, Branca D, Ferrigno F, Kinzel O, Muraglia E, Palumbi MC, Rowley M, Serafini S, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4191-5. doi: 10.1016/j.bmcl.2009.05.112. Epub 2009 Jun 2.

PMID:
19540115
21.

Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.

Kinzel O, Llauger-Bufi L, Pescatore G, Rowley M, Schultz-Fademrecht C, Monteagudo E, Fonsi M, Gonzalez Paz O, Fiore F, Steinkühler C, Jones P.

J Med Chem. 2009 Jun 11;52(11):3453-6. doi: 10.1021/jm9004303.

PMID:
19441846
22.

Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.

Attenni B, Ontoria JM, Cruz JC, Rowley M, Schultz-Fademrecht C, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3081-4. doi: 10.1016/j.bmcl.2009.04.011. Epub 2009 Apr 9.

PMID:
19410459
23.

Smoothened antagonists: a promising new class of antitumor agents.

Gallinari P, Filocamo G, Jones P, Pazzaglia S, Steinkühler C.

Expert Opin Drug Discov. 2009 May;4(5):525-44. doi: 10.1517/17460440902852686.

PMID:
23485085
24.

HDAC2 blockade by nitric oxide and histone deacetylase inhibitors reveals a common target in Duchenne muscular dystrophy treatment.

Colussi C, Mozzetta C, Gurtner A, Illi B, Rosati J, Straino S, Ragone G, Pescatori M, Zaccagnini G, Antonini A, Minetti G, Martelli F, Piaggio G, Gallinari P, Steinkuhler C, Clementi E, Dell'Aversana C, Altucci L, Mai A, Capogrossi MC, Puri PL, Gaetano C.

Proc Natl Acad Sci U S A. 2008 Dec 9;105(49):19183-7. doi: 10.1073/pnas.0805514105. Epub 2008 Dec 1. Erratum in: Proc Natl Acad Sci U S A. 2009 Feb 3;106(5):1679. Steinkulher, Christian [corrected to Steinkuhler, Christian].

25.

Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.

Scarpelli R, Di Marco A, Ferrigno F, Laufer R, Marcucci I, Muraglia E, Ontoria JM, Rowley M, Serafini S, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6078-82. doi: 10.1016/j.bmcl.2008.10.041. Epub 2008 Oct 12.

PMID:
18952417
26.

2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.

Muraglia E, Altamura S, Branca D, Cecchetti O, Ferrigno F, Orsale MV, Palumbi MC, Rowley M, Scarpelli R, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6083-7. doi: 10.1016/j.bmcl.2008.09.076. Epub 2008 Sep 24.

PMID:
18930398
27.

Optimization of a series of potent and selective ketone histone deacetylase inhibitors.

Pescatore G, Kinzel O, Attenni B, Cecchetti O, Fiore F, Fonsi M, Rowley M, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5528-32. doi: 10.1016/j.bmcl.2008.09.003. Epub 2008 Sep 6.

PMID:
18809328
28.

Inhibition of class I histone deacetylase with an apicidin derivative prevents cardiac hypertrophy and failure.

Gallo P, Latronico MV, Gallo P, Grimaldi S, Borgia F, Todaro M, Jones P, Gallinari P, De Francesco R, Ciliberto G, Steinkühler C, Esposito G, Condorelli G.

Cardiovasc Res. 2008 Dec 1;80(3):416-24. doi: 10.1093/cvr/cvn215. Epub 2008 Aug 12.

PMID:
18697792
29.

Structural and functional analysis of the human HDAC4 catalytic domain reveals a regulatory structural zinc-binding domain.

Bottomley MJ, Lo Surdo P, Di Giovine P, Cirillo A, Scarpelli R, Ferrigno F, Jones P, Neddermann P, De Francesco R, Steinkühler C, Gallinari P, Carfí A.

J Biol Chem. 2008 Sep 26;283(39):26694-704. doi: 10.1074/jbc.M803514200. Epub 2008 Jul 8.

30.

2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors.

Jones P, Bottomley MJ, Carfí A, Cecchetti O, Ferrigno F, Lo Surdo P, Ontoria JM, Rowley M, Scarpelli R, Schultz-Fademrecht C, Steinkühler C.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3456-61. doi: 10.1016/j.bmcl.2008.02.026. Epub 2008 Feb 14.

PMID:
18440229
31.

Development and optimization of a binding assay for histone deacetylase 4 using surface plasmon resonance.

Mattu M, Di Giovine P, Steinkuhler C, De Francesco R, Altamura S, Cecchetti O, Carfì A, Barbato G.

Anal Biochem. 2008 Jun 15;377(2):267-9. doi: 10.1016/j.ab.2008.03.028. Epub 2008 Mar 22.

PMID:
18381195
32.

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.

Jones P, Altamura S, De Francesco R, Paz OG, Kinzel O, Mesiti G, Monteagudo E, Pescatore G, Rowley M, Verdirame M, Steinkühler C.

J Med Chem. 2008 Apr 24;51(8):2350-3. doi: 10.1021/jm800079s. Epub 2008 Mar 28.

PMID:
18370373
33.
34.

Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.

Jones P, Altamura S, De Francesco R, Gallinari P, Lahm A, Neddermann P, Rowley M, Serafini S, Steinkühler C.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1814-9. doi: 10.1016/j.bmcl.2008.02.025. Epub 2008 Feb 14.

PMID:
18308563
35.

PP2A regulates HDAC4 nuclear import.

Paroni G, Cernotta N, Dello Russo C, Gallinari P, Pallaoro M, Foti C, Talamo F, Orsatti L, Steinkühler C, Brancolini C.

Mol Biol Cell. 2008 Feb;19(2):655-67. Epub 2007 Nov 28.

36.

Nitric oxide modulates chromatin folding in human endothelial cells via protein phosphatase 2A activation and class II histone deacetylases nuclear shuttling.

Illi B, Dello Russo C, Colussi C, Rosati J, Pallaoro M, Spallotta F, Rotili D, Valente S, Ragone G, Martelli F, Biglioli P, Steinkuhler C, Gallinari P, Mai A, Capogrossi MC, Gaetano C.

Circ Res. 2008 Jan 4;102(1):51-8. Epub 2007 Nov 1.

PMID:
17975112
37.

Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.

Lahm A, Paolini C, Pallaoro M, Nardi MC, Jones P, Neddermann P, Sambucini S, Bottomley MJ, Lo Surdo P, Carfí A, Koch U, De Francesco R, Steinkühler C, Gallinari P.

Proc Natl Acad Sci U S A. 2007 Oct 30;104(44):17335-40. Epub 2007 Oct 23.

38.

Substrate binding to histone deacetylases as shown by the crystal structure of the HDAC8-substrate complex.

Vannini A, Volpari C, Gallinari P, Jones P, Mattu M, Carfí A, De Francesco R, Steinkühler C, Di Marco S.

EMBO Rep. 2007 Sep;8(9):879-84. Epub 2007 Aug 10.

39.

HDACs, histone deacetylation and gene transcription: from molecular biology to cancer therapeutics.

Gallinari P, Di Marco S, Jones P, Pallaoro M, Steinkühler C.

Cell Res. 2007 Mar;17(3):195-211. Review.

40.

A series of novel, potent, and selective histone deacetylase inhibitors.

Jones P, Altamura S, Chakravarty PK, Cecchetti O, De Francesco R, Gallinari P, Ingenito R, Meinke PT, Petrocchi A, Rowley M, Scarpelli R, Serafini S, Steinkühler C.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):5948-52. Epub 2006 Sep 20.

PMID:
16987657
41.

Functional and morphological recovery of dystrophic muscles in mice treated with deacetylase inhibitors.

Minetti GC, Colussi C, Adami R, Serra C, Mozzetta C, Parente V, Fortuni S, Straino S, Sampaolesi M, Di Padova M, Illi B, Gallinari P, Steinkühler C, Capogrossi MC, Sartorelli V, Bottinelli R, Gaetano C, Puri PL.

Nat Med. 2006 Oct;12(10):1147-50. Epub 2006 Sep 17.

PMID:
16980968
42.

Dissecting the biological functions of Drosophila histone deacetylases by RNA interference and transcriptional profiling.

Foglietti C, Filocamo G, Cundari E, De Rinaldis E, Lahm A, Cortese R, Steinkühler C.

J Biol Chem. 2006 Jun 30;281(26):17968-76. Epub 2006 Apr 21.

43.

The design and enzyme-bound crystal structure of indoline based peptidomimetic inhibitors of hepatitis C virus NS3 protease.

Ontoria JM, Di Marco S, Conte I, Di Francesco ME, Gardelli C, Koch U, Matassa VG, Poma M, Steinkühler C, Volpari C, Harper S.

J Med Chem. 2004 Dec 16;47(26):6443-6.

PMID:
15588076
44.

Crystal structure of a eukaryotic zinc-dependent histone deacetylase, human HDAC8, complexed with a hydroxamic acid inhibitor.

Vannini A, Volpari C, Filocamo G, Casavola EC, Brunetti M, Renzoni D, Chakravarty P, Paolini C, De Francesco R, Gallinari P, Steinkühler C, Di Marco S.

Proc Natl Acad Sci U S A. 2004 Oct 19;101(42):15064-9. Epub 2004 Oct 11.

45.
46.

Mechanism of activation of human heparanase investigated by protein engineering.

Nardella C, Lahm A, Pallaoro M, Brunetti M, Vannini A, Steinkühler C.

Biochemistry. 2004 Feb 24;43(7):1862-73.

PMID:
14967027
47.

In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor.

Trozzi C, Bartholomew L, Ceccacci A, Biasiol G, Pacini L, Altamura S, Narjes F, Muraglia E, Paonessa G, Koch U, De Francesco R, Steinkuhler C, Migliaccio G.

J Virol. 2003 Mar;77(6):3669-79.

48.

Recent developments in the discovery of hepatitis C virus serine protease inhibitors--towards a new class of antiviral agents?

Narjes F, Koch U, Steinkühler C.

Expert Opin Investig Drugs. 2003 Feb;12(2):153-63. Review.

PMID:
12556211
49.

Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.

Colarusso S, Koch U, Gerlach B, Steinkühler C, De Francesco R, Altamura S, Matassa VG, Narjes F.

J Med Chem. 2003 Jan 30;46(3):345-8.

PMID:
12540231
50.

A scintillation proximity active site binding assay for the hepatitis C virus serine protease.

Steinkühler C, Biasiol G, Cerretani M, Di Renzo L, Brunetti M, Ingallinella P, De Francesco R, Altamura S.

Anal Biochem. 2002 Aug 1;307(1):99-104.

PMID:
12137785

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