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444 results on '"Campiani, G."'

9. Tubulin-6j complex

Author

Brindisi, M., primary, Ulivieri, C., additional, Alfano, G., additional, Gemma, S., additional, Balaguer, F.d.A., additional, Khan, T., additional, Grillo, A., additional, Chemi, G., additional, Menchon, G., additional, Prota, A.E., additional, Olieric, N., additional, Agell, D.L., additional, Barasoain, I., additional, Diaz, J.F., additional, Nebbioso, A., additional, Conte, M.R., additional, Lopresti, L., additional, Magnano, S., additional, Amet, R., additional, Kinsella, P., additional, Zisterer, D.M., additional, Ibrahim, O., additional, O'Sullivan, J., additional, Morbidelli, L., additional, Spaccapelo, R., additional, Baldari, C., additional, Butini, S., additional, Novellino, E., additional, Campiani, G., additional, Altucci, L., additional, Steinmetz, M.O., additional, and Brogi, S., additional

Published
2018
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12. Exploiting protein fluctuation at human cholinesterase active-sites. New Perspectives

Author

FATTORUSSO, CATERINA, PERSICO, MARCO, CATALANOTTI, BRUNO, NOVELLINO, ETTORE, Campiani G, Borriello M, Leo A, Gemma S, Panico A, Ros S, Brindisi M, Agnusdei M, Fiorini I, Nacci V, Belinskaya T, Saxena A, Butini S., Stefano Alcaro, Fattorusso, Caterina, Campiani, G, Borriello, M, Leo, A, Gemma, S, Panico, A, Persico, Marco, Catalanotti, Bruno, Ros, S, Brindisi, M, Agnusdei, M, Fiorini, I, Nacci, V, Novellino, Ettore, Belinskaya, T, Saxena, A, and Butini, S.

Published
2009

16. Polypharmacology of dopamine receptor ligands

Author

Butini, S., primary, Nikolic, K., additional, Kassel, S., additional, Brückmann, H., additional, Filipic, S., additional, Agbaba, D., additional, Gemma, S., additional, Brogi, S., additional, Brindisi, M., additional, Campiani, G., additional, and Stark, H., additional

Published
2016
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18. Agonist binding, efficacy and domain closure of GluR2

Author

Frandsen, A, Pickering, DS, Vestergaard, B, Kasper, C, Nielsen, BB, Greenwood, JR, Campiani, G, Fattorusso, C, Gajhede, M, Schousboe, A, Kastrup, JS., Frandsen, A, Pickering, D, Vestergaard, B, Kasper, C, Nielsen, Bb, Greenwood, Jr, Campiani, G, Fattorusso, C, Gajhede, M, Schousboe, A, and Kastrup, Js.

Published
2005

19. The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors

Author

Butini, S., Brogi, S., Ettore Novellino, Campiani, G., Ghosh, A. K., Brindisi, M., and Gemma, S.

Subjects
Amyloid beta-Peptides, BACE-1, Alzheimer's disease, Article, Small-molecule inhibitors, Peptidomimetic inhibitors, Protease inhibitors, β-secretase, Capillary Permeability, Small Molecule Libraries, Alzheimer Disease, Blood-Brain Barrier, Drug Design, Aspartic Acid Endopeptidases, Humans, Protease Inhibitors, Peptidomimetics, Amyloid Precursor Protein Secretases
Abstract

Effective treatment of Alzheimer’s disease (AD) remains a critical unmet need in medicine. The lack of useful treatment for AD led to an intense search for novel therapies based on the amyloid hypothesis, which states that amyloid β-42 (Aβ42) plays an early and crucial role in all cases of AD. β-Secretase (also known as BACE-1 β-site APP-cleaving enzyme, Asp-2 or memapsin-2) is an aspartyl protease representing the rate limiting step in the generation of Aβ peptide fragments, therefore it could represent an important target in the steady hunt for a disease-modifying treatment. Generally, β-secretase inhibitors are grouped into two families: peptidomimetic and nonpeptidomimetic inhibitors. However, irrespective of the class, serious challenges with respect to blood–brain barrier (BBB) penetration and selectivity still remain. Discovering a small molecule inhibitor of β-secretase represents an unnerving challenge but, due to its significant potential as a therapeutic target, growing efforts in this task are evident from both academic and industrial laboratories. In this frame, the rising availability of crystal structures of β-secretase-inhibitor complexes represents an invaluable opportunity for optimization. Nevertheless, beyond the inhibitory activity, the major issue of the current research approaches is about problems associated with BBB penetration and pharmacokinetic properties. This review follows the structural evolution of the early β-secretase inhibitors and gives a snap-shot of the hottest chemical templates in the literature of the last five years, showing research progress in this field.

Published
2013

20. Sviluppo di nuovi antipsicotici atipici a struttura Pirrolobenzotiazepinica

Author

Butini S., Gemma S., Minetti P., Di Cesare M. A., Fiorini I., Nacci V., Mennini T., Cagnotto G., Mastroianni D., Scafetta N., Galletti B., S.t.a.s.i. , C.a.s.t.o.r.i.n.o.M., Pacifici L., G.h.i.r.a.r.d.i.O., Tinti O., Carminati P., Campiani G., FATTORUSSO, CATERINA, CATALANOTTI, BRUNO, Butini, S., Gemma, S., Minetti, P., Di Cesare, M. A., Fattorusso, Caterina, Catalanotti, Bruno, Fiorini, I., Nacci, V., Mennini, T., Cagnotto, G., Mastroianni, D., Scafetta, N., Galletti, B., S. t. a. s. i., C. a. s. t. o. r. i. n. o. M., Pacifici, L., G. h. i. r. a. r. d. i., O., Tinti, O., Carminati, P., and Campiani, G.

Published
2002

22. Sintesi di molecole attive nel trattamento del Cocaine-Craving

Author

Butini S., Aiello F., Trotta F., Fiorini I., Nacci V., Carnovati F., Stark J., Cagnotto A., Cervo L., Mennini T., Campiani G., FATTORUSSO, CATERINA, CATALANOTTI, BRUNO, Butini, S., Aiello, F., Trotta, F., Fattorusso, Caterina, Catalanotti, Bruno, Fiorini, I., Nacci, V., Carnovati, F., Stark, J., Cagnotto, A., Cervo, L., Mennini, T., and Campiani, G.

Published
2002

23. The stereoselective targeting of a specific enzyme-substrate complex is the molecular mechanism for the synergic inhibition of HIV-1 reverse transcriptase by (R)-(-)-PPO464: a novel generation of nonnucleoside inhibitors

Author

Maga, G, Ramunno, A, Nacci, V, Locatelli, G A, Spadari, S, Fiorini, I, Baldanti, F, Paolucci, S, Zavattoni, M, Bergamini, A, Galletti, B, Muck, S, Hubscher, U, Giorgi, G, Guiso, G, Caccia, S, Campiani, G, University of Zurich, and Campiani, G

Subjects
1307 Cell Biology, 1303 Biochemistry, 1312 Molecular Biology, 570 Life sciences, biology, 10226 Department of Molecular Mechanisms of Disease
Published
2001

24. Pyrrolo-1,5-benzoxazepines induce apoptosis in chronic myelogenous leukemia (CML) cells by bipassing the apoptotic suppressor Bcr-Abi

Author

MC GEE M., CAMPIANI G., FATTORUSSO, CATERINA, RAMUNNO A., NACCI V., LAWLER M., WILLIAMS D. C., ZISTERER D. M., MC GEE, M., Campiani, G., Fattorusso, Caterina, Ramunno, A., Nacci, V., Lawler, M., Williams, D. C., and Zisterer, D. M.

Abstract

Expression of the transforming oncogene bcr-abl in chronic myelogenous leukemia (CML) cells is reported to confer resistance against apoptosis induced by many chemotherapeutic agents such as etoposide, ara-C, and staurosporine. In the present study some members of a series of novel pyrrolo-1,5-benzoxazepines potently induce apoptosis, as shown by cell shrinkage, chromatin condensation, DNA fragmentation, and poly(ADP-ribose) polymerase (PARP) cleavage, in three CML cell lines, K562, KYO.1, and LAMA 84. Induction of apoptosis by a representative member of this series, PBOX-6, was not accompanied by either the down-regulation of Bcr-Abl or by the attenuation of its protein tyrosine kinase activity up to 24 h after treatment, when approximately 50% of the cells had undergone apoptosis. These results suggest that down-regulation of Bcr-Abl is not part of the upstream apoptotic death program activated by PBOX-6. By characterizing the mechanism in which this novel agent executes apoptosis, this study has revealed that PBOX-6 caused activation of caspase 3-like proteases in only two of the three CML cell lines. In addition, inhibition of caspase 3-like protease activity using the inhibitor z-DEVD-fmk blocked caspase 3-like protease activity but did not prevent the induction of apoptosis, suggesting that caspase 3-like proteases are not essential in the mechanism by which PBOX-6 induces apoptosis in CML cells. In conclusion, this study demonstrates that PBOX-6 can bypass Bcr-Abl-mediated suppression of apoptosis, suggesting an important potential use of these compounds in the treatment of CML.

Published
2001

25. Pyrrole 1,5-benzoaxazepines : a new class of apoptotic agents

Author

ZISTERER D. M., MC GEE M., CAMPIANI G., RAMUNNO A., FATTORUSSO, CATERINA, NACCI V., LAWLER M., WILLIAMS D. C., Zisterer, D. M., MC GEE, M., Campiani, G., Ramunno, A., Fattorusso, Caterina, Nacci, V., Lawler, M., and Williams, D. C.

Abstract

Some members of a series of novel pyrrolo-1,5-benzoxazepines (PBOXs) potently induce apoptosis in a number of human cancerous cell lines including HL-60 cells and the drug-resistant chronic myelogenous leukaemia cell line, K562. The apoptotic induction seems to be independent of the mitochondrial peripheral-type benzodiazepine receptor (PBR), which binds these PBOXs with high affinity, due to a lack of correlation between their affinities for the receptor and their apoptotic potencies and their high apoptotic activity in PBR-deficient cells. PBOX-6, a potent member of the series, induces a transient activation of c-Jun N-terminal kinase (JNK) in a dose-dependent manner, which correlates with induction of apoptosis. Expression of a cytoplasmic inhibitor of the JNK signal transduction pathway, Jip-1, prevents JNK activity and significantly reduces the extent of apoptosis induced by PBOX-6. This demonstrates the requirement for JNK in the cellular response to this apoptotic agent. In addition, PBOX-6 activates caspase-3-like proteases in K562 and HL-60 cells. The caspase-3 inhibitor, Z-Asp-Glu-Val-Asp-fluoromethylketone (z-DEVD-fmk), blocks caspase-3-like protease activity in both cell types but only prevents PBOX-6-induced apoptosis in HL-60 cells, suggesting that the requirement for caspase-3-like proteases in the apoptotic pathway is dependent on the cell type

Published
2001

26. Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors. Synthesis and Biological Evaluation of Novel Quinoxalinylethylpyridylthioureas (QXPTs) as Potent Antiviral Agents

Author

Campiani, G., Fabbrini, M., Nacci, V., Maga, Spadari, S., Bergamini, A., Faggioli, E., Uccella, I., Bolacchi, F., Marini, S., Coletta, M., Fracasso, C., Caccia, S., MORELLI, ELENA, GRECO, GIOVANNI, NOVELLINO, ETTORE, Campiani, G., Fabbrini, M., Morelli, Elena, Nacci, V., Greco, Giovanni, Novellino, Ettore, Maga, Spadari, S., Bergamini, A., Faggioli, E., Uccella, I., Bolacchi, F., Marini, S., Coletta, M., Fracasso, C., and Caccia, S.

Published
2000

29. Pyrrolobenzoxazepinone (PBO) Derivatives as Non-Nucleoside HIV-1 Reverse Transcriptase (RT) Inhibitors. Further Structure-Activity Relationship Studies and Identification of More Potent Broad Spectrum HIV-1 RT Inhibitors with Antiviral Activity

Author

Campiani G., Fabbrini M., Nacci V., Ramunno A., Maga G., Spadari S., Bergamini A., Faggioli E., Uccella I., Bolacchi F., Marini S., Coletta M., Nacca A., Caccia S., MORELLI, ELENA, GRECO, GIOVANNI, NOVELLINO, ETTORE, CALIENDO, GIUSEPPE, Campiani, G., Morelli, Elena, Fabbrini, M., Nacci, V., Greco, Giovanni, Novellino, Ettore, Ramunno, A., Maga, G., Spadari, S., Caliendo, Giuseppe, Bergamini, A., Faggioli, E., Uccella, I., Bolacchi, F., Marini, S., Coletta, M., Nacca, A., and Caccia, S.

Published
1999

30. Pyrroloquinoxaline Derivatives as a New Class of Potent and Selective 5-HT3 Receptor Agonists. Synthesis, Further Structure-Activity Relationhsips and Biological Studies

Author

Campiani G., Gemma S., Nacci V., Butini S., Hamon M., Cagnotto A., Goegan M., Cervo L., Dalla Valle F., Fracasso C., Caccia S., Mennini T., MORELLI, ELENA, NOVELLINO, ETTORE, GRECO, GIOVANNI, Campiani, G., Morelli, Elena, Gemma, S., Nacci, V., Butini, S., Hamon, M., Novellino, Ettore, Greco, Giovanni, Cagnotto, A., Goegan, M., Cervo, L., Dalla Valle, F., Fracasso, C., Caccia, S., and Mennini, T.

Published
1999

31. Old and new targets for innovative malaria compounds: the diffferent strategies of the Italian Malaria Network

Author

Basilico, N, Bosisio, E, Buelli, F, Campiani, G, Casagrande, M, Castelli, F, Coghi, P, Corbett, Y, Cortelezzi, L, D'Alessandro, S, Dell'Agli, M, Esposito, F, Fattorusso, C, Fattorusso, E, Finaurini, S, Galli, Gv, Gemma, S, Habluetzel, Annette, Lucantoni, L, Melato, S, Monti, D, Olliaro, P, OMODEO SALÈ, F, Parapini, S, Persico, M, Rizzi, M, Romeo, S, Rossi, F, Rusconi, C, Sparatore, A, Scafati, Ot, VAN DEN BOGAART, E, Taramelli, D, Vaiana, N, and Yerbanga, S.

Published
2008

36. PBOX-15, a novel microtubule targeting agent, induces apoptosis, upregulates death receptors, and potentiates TRAIL-mediated apoptosis in multiple myeloma cells

Author

Maginn, E N, primary, Browne, P V, additional, Hayden, P, additional, Vandenberghe, E, additional, MacDonagh, B, additional, Evans, P, additional, Goodyer, M, additional, Tewari, P, additional, Campiani, G, additional, Butini, S, additional, Williams, D C, additional, Zisterer, D M, additional, Lawler, M P, additional, and McElligott, A M, additional

Published
2010
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42. ChemInform Abstract: Synthesis and “in vitro” Cardiovascular Activity of 4-Aryl-2,3,3a,4- tetrahydro-1H-pyrrolo(2,1-c) (1,4)benzothiazin-1-ones and 7-Acetoxy-6- phenyl-7a,8,9,10-tetrahydropyrrolo(2,1-d) (1,5)benzothiazepin-10-one.

Author

CAMPIANI, G., primary, GAROFALO, A., additional, FIORINI, I., additional, NACCI, V., additional, BOTTA, M., additional, TAFI, A., additional, CHIARINI, A., additional, BUDRIESI, R., additional, BRUNI, G., additional, and ROMEO, M. R., additional

Published
2010
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43. ChemInform Abstract: Novel Ligands Specific for Mitochondrial Benzodiazepine Receptors: 6- Arylpyrrolo(2,1-d) (1,5)benzothiazepine Derivatives. Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies.

Author

FIORINI, I., primary, NACCI, V., additional, CIANI, S. M., additional, GAROFALO, A., additional, CAMPIANI, G., additional, SAVINI, L., additional, NOVELLINO, E., additional, GRECO, G., additional, BERNASCONI, P., additional, and MENNINI, T., additional

Published
2010
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45. ChemInform Abstract: Cardiovascular Characterization of Pyrrolo(2,1-d)(1,5)benzothiazepine Derivatives Binding Selectively to the Peripheral-Type Benzodiazepine Receptor (PBR): From Dual PBR Affinity and Calcium Antagonist Activity to Novel and Selective

Author

CAMPIANI, G., primary, FIORINI, I., additional, DE FILIPPIS, M. P., additional, CIANI, S. M., additional, GAROFALO, A., additional, NACCI, V., additional, GIORGI, G., additional, SEGA, A., additional, BOTTA, M., additional, CHIARINI, A., additional, BUDRIESI, R., additional, BRUNI, G., additional, ROMEO, M. R., additional, MANZONI, C., additional, and MENNINI, T., additional

Published
2010
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46. ChemInform Abstract: Synthesis, Biological Activity, and SARs of Pyrrolobenzoxazepine Derivatives, a New Class of Specific “Peripheral-Type” Benzodiazepine Receptor Ligands.

Author

CAMPIANI, G., primary, NACCI, V., additional, FIORINI, I., additional, DE FILIPPIS, M. P., additional, GAROFALO, A., additional, CIANI, S. M., additional, GRECO, G., additional, NOVELLINO, E., additional, WILLIAMS, D. C., additional, ZISTERER, D. M., additional, WOODS, M. J., additional, MIHAI, C., additional, MANZONI, C., additional, and MENNINI, T., additional

Published
2010
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48. Novel pyrrolo-1,5-benzoxazepine compounds display significant activity against resistant chronic myeloid leukaemia cells in vitro, in ex vivo patient samples and in vivo

Author

Bright, S A, primary, McElligott, A M, additional, O'Connell, J W, additional, O'Connor, L, additional, Carroll, P, additional, Campiani, G, additional, Deininger, M W, additional, Conneally, E, additional, Lawler, M, additional, Williams, D C, additional, and Zisterer, D M, additional

Published
2010
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50. Synthesis and 5-HT Receptors Binding Studies of Some 3-Substituted-2-(4-methyl-1-piperazinyl)-4-phenylquinolines

Author

Anzini, M., Cappelli, A., Vomero, S., Campiani, G., Alfredo Cagnotto, and Skorupska, M.

Subjects
Male, Serotonin, Rats, Inbred Strains, In Vitro Techniques, Quinolones, Ligands, Binding, Competitive, Piperazines, Rats, Paroxetine, Quipazine, Piperidines, Animals, Serotonin Antagonists
Abstract

The syntheses of some 3-substituted-2-(4-methyl-1-piperazinyl)-4-phenylquinolines are reported. The title compounds were tested for their potential activities on 5-HT receptor subtypes and 5-HT uptake site; compounds 4b-d showed micromolar affinity for 5-HT3 and 5-HT uptake site.

Published
1991

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