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Items: 43

1.

Phase I dose escalation study of NMS-1286937, an orally available Polo-Like Kinase 1 inhibitor, in patients with advanced or metastatic solid tumors.

Weiss GJ, Jameson G, Von Hoff DD, Valsasina B, Davite C, Di Giulio C, Fiorentini F, Alzani R, Carpinelli P, Di Sanzo A, Galvani A, Isacchi A, Ramanathan RK.

Invest New Drugs. 2018 Feb;36(1):85-95. doi: 10.1007/s10637-017-0491-7. Epub 2017 Jul 20.

PMID:
28726132
2.

A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action.

Campaner E, Rustighi A, Zannini A, Cristiani A, Piazza S, Ciani Y, Kalid O, Golan G, Baloglu E, Shacham S, Valsasina B, Cucchi U, Pippione AC, Lolli ML, Giabbai B, Storici P, Carloni P, Rossetti G, Benvenuti F, Bello E, D'Incalci M, Cappuzzello E, Rosato A, Del Sal G.

Nat Commun. 2017 Jun 9;8:15772. doi: 10.1038/ncomms15772.

3.

Synthesis and biological evaluation of RGD peptidomimetic-paclitaxel conjugates bearing lysosomally cleavable linkers.

Dal Corso A, Caruso M, Belvisi L, Arosio D, Piarulli U, Albanese C, Gasparri F, Marsiglio A, Sola F, Troiani S, Valsasina B, Pignataro L, Donati D, Gennari C.

Chemistry. 2015 Apr 27;21(18):6921-9. doi: 10.1002/chem.201500158. Epub 2015 Mar 17.

PMID:
25784522
4.

Discovery of 2-(cyclohexylmethylamino)pyrimidines as a new class of reversible valosine containing protein inhibitors.

Cervi G, Magnaghi P, Asa D, Avanzi N, Badari A, Borghi D, Caruso M, Cirla A, Cozzi L, Felder E, Galvani A, Gasparri F, Lomolino A, Magnuson S, Malgesini B, Motto I, Pasi M, Rizzi S, Salom B, Sorrentino G, Troiani S, Valsasina B, O'Brien T, Isacchi A, Donati D, D'Alessio R.

J Med Chem. 2014 Dec 26;57(24):10443-54. doi: 10.1021/jm501313x. Epub 2014 Dec 12.

PMID:
25474526
5.

Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance.

Sero V, Tavanti E, Vella S, Hattinger CM, Fanelli M, Michelacci F, Versteeg R, Valsasina B, Gudeman B, Picci P, Serra M.

Invest New Drugs. 2014 Dec;32(6):1167-80. doi: 10.1007/s10637-014-0158-6. Epub 2014 Sep 7.

PMID:
25193492
6.

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death.

Magnaghi P, D'Alessio R, Valsasina B, Avanzi N, Rizzi S, Asa D, Gasparri F, Cozzi L, Cucchi U, Orrenius C, Polucci P, Ballinari D, Perrera C, Leone A, Cervi G, Casale E, Xiao Y, Wong C, Anderson DJ, Galvani A, Donati D, O'Brien T, Jackson PK, Isacchi A.

Nat Chem Biol. 2013 Sep;9(9):548-56. doi: 10.1038/nchembio.1313. Epub 2013 Jul 28.

PMID:
23892893
7.

NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.

Fogliatto G, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder E, Pesenti E, Galvani A, Mantegani S, Isacchi A.

Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14.

8.

The Polo-Like Kinase 1 (PLK1) inhibitor NMS-P937 is effective in a new model of disseminated primary CD56+ acute monoblastic leukaemia.

Casolaro A, Golay J, Albanese C, Ceruti R, Patton V, Cribioli S, Pezzoni A, Losa M, Texido G, Giussani U, Marchesi F, Amboldi N, Valsasina B, Bungaro S, Cazzaniga G, Rambaldi A, Introna M, Pesenti E, Alzani R.

PLoS One. 2013;8(3):e58424. doi: 10.1371/journal.pone.0058424. Epub 2013 Mar 8.

9.

NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies.

Valsasina B, Beria I, Alli C, Alzani R, Avanzi N, Ballinari D, Cappella P, Caruso M, Casolaro A, Ciavolella A, Cucchi U, De Ponti A, Felder E, Fiorentini F, Galvani A, Gianellini LM, Giorgini ML, Isacchi A, Lansen J, Pesenti E, Rizzi S, Rocchetti M, Sola F, Moll J.

Mol Cancer Ther. 2012 Apr;11(4):1006-16. doi: 10.1158/1535-7163.MCT-11-0765. Epub 2012 Feb 7.

10.

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.

Caruso M, Valsasina B, Ballinari D, Bertrand J, Brasca MG, Caldarelli M, Cappella P, Fiorentini F, Gianellini LM, Scolaro A, Beria I.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):96-101. doi: 10.1016/j.bmcl.2011.11.065. Epub 2011 Nov 23.

PMID:
22154349
11.

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, Fasolini M, Forte B, Fiorentini F, Pesenti E, Pezzetta D, Posteri H, Scolaro A, Re Depaolini S, Valsasina B.

Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74. doi: 10.1016/j.bmcl.2011.03.054. Epub 2011 Mar 21.

PMID:
21470862
12.

Phosphorylation of TCTP as a marker for polo-like kinase-1 activity in vivo.

Cucchi U, Gianellini LM, De Ponti A, Sola F, Alzani R, Patton V, Pezzoni A, Troiani S, Saccardo MB, Rizzi S, Giorgini ML, Cappella P, Beria I, Valsasina B.

Anticancer Res. 2010 Dec;30(12):4973-85.

PMID:
21187478
13.

4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.

Beria I, Valsasina B, Brasca MG, Ceccarelli W, Colombo M, Cribioli S, Fachin G, Ferguson RD, Fiorentini F, Gianellini LM, Giorgini ML, Moll JK, Posteri H, Pezzetta D, Roletto F, Sola F, Tesei D, Caruso M.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6489-94. doi: 10.1016/j.bmcl.2010.09.060. Epub 2010 Sep 17.

PMID:
20932759
14.

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Menichincheri M, Albanese C, Alli C, Ballinari D, Bargiotti A, Caldarelli M, Ciavolella A, Cirla A, Colombo M, Colotta F, Croci V, D'Alessio R, D'Anello M, Ermoli A, Fiorentini F, Forte B, Galvani A, Giordano P, Isacchi A, Martina K, Molinari A, Moll JK, Montagnoli A, Orsini P, Orzi F, Pesenti E, Pillan A, Roletto F, Scolaro A, Tatò M, Tibolla M, Valsasina B, Varasi M, Vianello P, Volpi D, Santocanale C, Vanotti E.

J Med Chem. 2010 Oct 28;53(20):7296-315. doi: 10.1021/jm100504d.

PMID:
20873740
15.

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.

Beria I, Ballinari D, Bertrand JA, Borghi D, Bossi RT, Brasca MG, Cappella P, Caruso M, Ceccarelli W, Ciavolella A, Cristiani C, Croci V, De Ponti A, Fachin G, Ferguson RD, Lansen J, Moll JK, Pesenti E, Posteri H, Perego R, Rocchetti M, Storici P, Volpi D, Valsasina B.

J Med Chem. 2010 May 13;53(9):3532-51. doi: 10.1021/jm901713n.

PMID:
20397705
16.

Identification of Myb-binding protein 1A (MYBBP1A) as a novel substrate for aurora B kinase.

Perrera C, Colombo R, Valsasina B, Carpinelli P, Troiani S, Modugno M, Gianellini L, Cappella P, Isacchi A, Moll J, Rusconi L.

J Biol Chem. 2010 Apr 16;285(16):11775-85. doi: 10.1074/jbc.M109.068312. Epub 2010 Feb 22.

17.

Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.

Ermoli A, Bargiotti A, Brasca MG, Ciavolella A, Colombo N, Fachin G, Isacchi A, Menichincheri M, Molinari A, Montagnoli A, Pillan A, Rainoldi S, Sirtori FR, Sola F, Thieffine S, Tibolla M, Valsasina B, Volpi D, Santocanale C, Vanotti E.

J Med Chem. 2009 Jul 23;52(14):4380-90. doi: 10.1021/jm900248g.

PMID:
19555113
18.

First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.

Menichincheri M, Bargiotti A, Berthelsen J, Bertrand JA, Bossi R, Ciavolella A, Cirla A, Cristiani C, Croci V, D'Alessio R, Fasolini M, Fiorentini F, Forte B, Isacchi A, Martina K, Molinari A, Montagnoli A, Orsini P, Orzi F, Pesenti E, Pezzetta D, Pillan A, Poggesi I, Roletto F, Scolaro A, Tatò M, Tibolla M, Valsasina B, Varasi M, Volpi D, Santocanale C, Vanotti E.

J Med Chem. 2009 Jan 22;52(2):293-307. doi: 10.1021/jm800977q. Erratum in: J Med Chem. 2009 Feb 26;52(4):1230.

PMID:
19115845
19.

A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.

Montagnoli A, Valsasina B, Croci V, Menichincheri M, Rainoldi S, Marchesi V, Tibolla M, Tenca P, Brotherton D, Albanese C, Patton V, Alzani R, Ciavolella A, Sola F, Molinari A, Volpi D, Avanzi N, Fiorentini F, Cattoni M, Healy S, Ballinari D, Pesenti E, Isacchi A, Moll J, Bensimon A, Vanotti E, Santocanale C.

Nat Chem Biol. 2008 Jun;4(6):357-65. doi: 10.1038/nchembio.90. Epub 2008 May 11.

PMID:
18469809
20.

Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships.

Vanotti E, Amici R, Bargiotti A, Berthelsen J, Bosotti R, Ciavolella A, Cirla A, Cristiani C, D'Alessio R, Forte B, Isacchi A, Martina K, Menichincheri M, Molinari A, Montagnoli A, Orsini P, Pillan A, Roletto F, Scolaro A, Tibolla M, Valsasina B, Varasi M, Volpi D, Santocanale C.

J Med Chem. 2008 Feb 14;51(3):487-501. doi: 10.1021/jm700956r. Epub 2008 Jan 18.

PMID:
18201066
21.

Identification of Mcm2 phosphorylation sites by S-phase-regulating kinases.

Montagnoli A, Valsasina B, Brotherton D, Troiani S, Rainoldi S, Tenca P, Molinari A, Santocanale C.

J Biol Chem. 2006 Apr 14;281(15):10281-90. Epub 2006 Jan 30.

22.

Searching for biomarkers of Aurora-A kinase activity: identification of in vitro substrates through a modified KESTREL approach.

Troiani S, Uggeri M, Moll J, Isacchi A, Kalisz HM, Rusconi L, Valsasina B.

J Proteome Res. 2005 Jul-Aug;4(4):1296-303.

PMID:
16083279
23.

Kinase selectivity profiling by inhibitor affinity chromatography.

Valsasina B, Kalisz HM, Isacchi A.

Expert Rev Proteomics. 2004 Oct;1(3):303-15. Review.

PMID:
15966827
24.

Structural characterization of the GSK-3beta active site using selective and non-selective ATP-mimetic inhibitors.

Bertrand JA, Thieffine S, Vulpetti A, Cristiani C, Valsasina B, Knapp S, Kalisz HM, Flocco M.

J Mol Biol. 2003 Oct 17;333(2):393-407.

PMID:
14529625
25.

Inhibitor affinity chromatography: profiling the specific reactivity of the proteome with immobilized molecules.

Lolli G, Thaler F, Valsasina B, Roletto F, Knapp S, Uggeri M, Bachi A, Matafora V, Storici P, Stewart A, Kalisz HM, Isacchi A.

Proteomics. 2003 Jul;3(7):1287-98.

PMID:
12872229
26.

A new approach to phosphoserine and phosphothreonine analysis in peptides and proteins: chemical modification, enrichment via solid-phase reversible binding, and analysis by mass spectrometry.

Thaler F, Valsasina B, Baldi R, Xie J, Stewart A, Isacchi A, Kalisz HM, Rusconi L.

Anal Bioanal Chem. 2003 Jun;376(3):366-73. Epub 2003 May 7.

PMID:
12734628
27.

The C-terminal domain of yeast Ero1p mediates membrane localization and is essential for function.

Pagani M, Pilati S, Bertoli G, Valsasina B, Sitia R.

FEBS Lett. 2001 Nov 9;508(1):117-20.

28.

Role of the Src homology 2 domains and interdomain regions in ZAP-70 phosphorylation and enzymatic activity.

Magistrelli G, Bosotti R, Valsasina B, Visco C, Perego R, Toma S, Acuto O, Isacchi A.

Eur J Biochem. 1999 Dec;266(3):1166-73.

29.

Recombinant human IL-2 is cytotoxic to oligodendrocytes after in vitro self aggregation.

Curatolo L, Valsasina B, Caccia C, Raimondi GL, Orsini G, Bianchetti A.

Cytokine. 1997 Oct;9(10):734-9.

PMID:
9344504
30.

Hydroxylamine-induced cleavage of the asparaginyl-glycine motif in the production of recombinant proteins: the case of insulin-like growth factor I.

Antorini M, Breme U, Caccia P, Grassi C, Lebrun S, Orsini G, Taylor G, Valsasina B, Marengo E, Todeschini R, Andersson C, Gellerfors P, Gustafsson JG.

Protein Expr Purif. 1997 Oct;11(1):135-47.

PMID:
9325149
31.

Characterization of a saporin isoform with lower ribosome-inhibiting activity.

Fabbrini MS, Rappocciolo E, Carpani D, Solinas M, Valsasina B, Breme U, Cavallaro U, Nykjaer A, Rovida E, Legname G, Soria MR.

Biochem J. 1997 Mar 15;322 ( Pt 3):719-27.

32.

Investigation on minor degraded derivatives of the recombinant hirudin variant HM2 from Hirudinaria manillensis isolated by isoelectric focusing in multicompartment electrolyzers.

Bossi A, Righetti PG, Visco C, Breme U, Mauriello M, Valsasina B, Orsini G, Wenisch E.

Electrophoresis. 1996 May;17(5):932-7.

PMID:
8783019
33.

Basic fibroblast growth factor stimulates hepatocyte growth factor/scatter factor secretion by human mesenchymal cells.

Roletto F, Galvani AP, Cristiani C, Valsasina B, Landonio A, Bertolero F.

J Cell Physiol. 1996 Jan;166(1):105-11.

PMID:
8557758
34.

Detection of traces of a trisulphide derivative in the preparation of a recombinant truncated interleukin-6 mutein.

Breton J, Avanzi N, Valsasina B, Sgarella L, La Fiura A, Breme U, Orsini G, Wenisch E, Righetti PG.

J Chromatogr A. 1995 Aug 11;709(1):135-46.

PMID:
7581842
35.

Structure, stability and biological properties of a N-terminally truncated form of recombinant human interleukin-6 containing a single disulfide bond.

Breton J, La Fiura A, Bertolero F, Orsini G, Valsasina B, Ziliotto R, De Filippis V, Polverino de Laureto P, Fontana A.

Eur J Biochem. 1995 Jan 15;227(1-2):573-81.

36.

Distinct role of 2-O-, N-, and 6-O-sulfate groups of heparin in the formation of the ternary complex with basic fibroblast growth factor and soluble FGF receptor-1.

Rusnati M, Coltrini D, Caccia P, Dell'Era P, Zoppetti G, Oreste P, Valsasina B, Presta M.

Biochem Biophys Res Commun. 1994 Aug 30;203(1):450-8.

PMID:
8074689
37.

Disulfide isoform intermediates in the reoxidation of recombinant human basic fibroblast growth factor.

Ruoppolo M, Nitti G, Valsasina B, Malorni A, Marino G, Pucci P.

Biochemistry. 1993 May 18;32(19):4991-6.

PMID:
8494874
38.

Novel hirudin variants from the leech Hirudinaria manillensis. Amino acid sequence, cDNA cloning and genomic organization.

Scacheri E, Nitti G, Valsasina B, Orsini G, Visco C, Ferrera M, Sawyer RT, Sarmientos P.

Eur J Biochem. 1993 May 15;214(1):295-304.

39.

Bean homologs of the mammalian glucose-regulated proteins: induction by tunicamycin and interaction with newly synthesized seed storage proteins in the endoplasmic reticulum.

D'Amico L, Valsasina B, Daminati MG, Fabbrini MS, Nitti G, Bollini R, Ceriotti A, Vitale A.

Plant J. 1992 Jul;2(4):443-55.

40.

Stabilization of recombinant human basic fibroblast growth factor by chemical modifications of cysteine residues.

Caccia P, Nitti G, Cletini O, Pucci P, Ruoppolo M, Bertolero F, Valsasina B, Roletto F, Cristiani C, Cauet G, et al.

Eur J Biochem. 1992 Mar 1;204(2):649-55.

41.

A Saporin-6 cDNA containing a precursor sequence coding for a carboxyl-terminal extension.

Benatti L, Nitti G, Solinas M, Valsasina B, Vitale A, Ceriotti A, Soria MR.

FEBS Lett. 1991 Oct 21;291(2):285-8.

42.

The signal peptide of human preproendothelin-1.

Fabbrini MS, Valsasina B, Nitti G, Benatti L, Vitale A.

FEBS Lett. 1991 Jul 29;286(1-2):91-4.

43.

Production of the HV1 variant of hirudin by recombinant DNA methodology.

de Taxis du Poet P, Scacheri E, Benatti L, Nitti G, Valsasina B, Sarmientos P.

Blood Coagul Fibrinolysis. 1991 Feb;2(1):113-20.

PMID:
1772978

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