HomeDiscoveryPubblicazioniPubblicazioni 2010

Pubblicazioni 2010

2010

 

Targeting cell division cycle 7 kinase: a new approach for cancer therapy
Montagnoli A, Moll J, Colotta F
Clin Cancer Res.
(2010), 4503-4508

Discovery of drug mode of action and drug repositioning from transcriptional responses
Iorio F, Bosotti R, Scacheri E, Belcastro V, Mithbaokar P, Ferriero R, Murino L, Tagliaferri R, Brunetti-Pierri N, Isacchi A, di Bernardo D
Proc Natl Acad Sci
(2010), 107(33), 14621-6

Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy
Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M
Mol Cancer Ther
(2010), 2243-2254

Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors
Bossi RT, Saccardo MB, Ardini E, Menichincheri M, Rusconi L, Magnaghi P, Orsini P, Avanzi N, Borgia AL, Nesi M, Bandiera T, Fogliatto G, Bertrand JA
Biochemistry
(2010), 6813-6825

Cell-based assays–Informa Life Sciences’ Fifth Annual Conference–Cell-based assays for compound screening and 3D assays
Gasparri F
IDrugs
(2010), 520-522

Cell-based assays–Informa Life Sciences’ Fifth Annual Conference–Label-free cell-based assays and high-content analysis in drug discovery
Gasparri F
IDrugs
(2010), 523-526

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity
Bindi S, Fancelli D, Alli C, Berta D, Bertrand JA, Cameron AD, Cappella P, Carpinelli P, Cervi G, Croci V, D’Anello M, Forte B, Giorgini ML, Marsiglio A, Moll J, Pesenti E, Pittalà V, Pulici M, Riccardi-Sirtori F, Roletto F, Soncini C et al
Bioorg Med Chem.
2010), 7113-7120.

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 et al.
J Med Chem.
(2010), 7296-7315

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), 6489-6494

Anaplastic Lymphoma Kinase: role in specific tumours, and development of small molecule inhibitors for cancer therapy
Ardini E, Magnaghi P, Orsini P, Galvani A, Menichincheri M.
Cancer Lett.
(2010), 81-94

Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase
Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J.
Cancer Res.
(2010), 10255-10264

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) 30(12), 4973-4985

Development of an automated modular system for the synthesis of [11C]acetate
Felicini C, Någren K, Berton A, Pascali G, Salvadori PA.
Nucl Med Commun.
(2010) 1033-1039

Destabilizing Aneuploidy by Targeting Cell Cycle and Mitotic Checkpoint Proteins in Cancer Cells.
Colombo R, Moll J
Curr Drug Targets
(2010) 11(10), 1325-1335

Targeting Genetic Instability in Cancer Cells
Colotta F
Curr Drug Targets
(2010) 11(10), 1293-1295

Miniaturizing bromodeoxyuridine incorporation enables the usage of flow cytometry for cell cycle analysis of adherent tissue culture cells for high throughput screening
Cappella P, Giorgini ML, Ernestina Re C, Ubezio P, Ciomei M, Moll J.
Cytometry A
(2010) 77(10), 953-961

Down-regulation of the nucleotide excision repair gene XPG as a new mechanism of drug resistance in human and murine cancer cells
Sabatino MA, Marabese M, Ganzinelli M, Caiola E, Geroni C, Broggini M.
Mol Cancer
(2010) 24(9), 259

Structure-based optimization of PDK1 inhibitors
Angiolini M, Banfi P, Casale E, Casuscelli F, Fiorelli C, Silvagni M, Zuccotto F, Saccardo MB
Bioorganic & Med Chem Lett
(2010) 4095-4099

Identification of Potent Pyrazolo[4,3-h]quinazoline-3-carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors
Traquandi G, Ciomei M, Ballinari D, Casale E, Colombo N, Croci V, Fiorentini F, Isacchi A, Longo A, Mercurio C, Panzeri A, Pastori W, Pevarello P, Volpi D, Roussel P, Vulpetti A, Brasca MG
J Med Chem
(2010) 53, 2171-2187

Role of glutathione transferases in the mechanism of Brostallicin activation
Pezzola S, Antonini G, Geroni C, Beria I, Colombo M, Broggini M, Mongelli N, Leboffe L, MacArthur R, Mozzi AF, Federici G, Caccuri AM
Biochemistry
(2010) 49, 226-235

Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engrafment and high-burden leukemia models
Alzani R, Pedrini O, Albanese C, Ceruti R, Casolaro A, Patton V, Colotta F, Rambaldi A, Introna M, Pesenti E, Ciomei M, Golay J
Experimental Hematology
(2010) 38, 259-269

Phase I dose-escalation study of brostallicin, a minor groove binder, in combination with cisplatin in patients with advanced solid tumors
Caponigro F, Lorusso D, Fornari G, Barone C, Merlano M, Airoldi M, Schena M, MacArthur R, Weitman S, Jannuzzo MG, Crippa S, Fiorentini F, Petroccione A, Comis S
Cancer Chemother Pharmacol
(2010) 66(2), 389-64

Efficacy of PHA-848125, a Cyclin Dependent Kinase inhibitor, on the K-RasG12DLA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging
Degrassi A, Russo M, Nanni C, Patton V, Alzani R, Giusti A, Fanti S, Ciomei M, Pesenti E, Texido G
Mol Cancer Ther
(2010) 9(3), 673-681

Optimisation of 6,6-Dimethyl Pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a Potent CDK Inhibitor Suitable for Intravenous Dosing
Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M
Bioorganic & Medicical Chemistry
(2010) 18, 1844-1853

Transcriptional analysis of an E2F gene signature as a biomarker of activity of the Cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study
Locatelli G, Bosotti R, Ciomei M, Brasca G,Calogero R, Mercurio C, Fiorentini F, Bertolotti M, Scacheri E, Scaburri A, Pesenti E, De Baere T, Soria JC, Lazar V, Isacchi A.
Mol Cancer Ther
(2010) 9(5), 1265-1273

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, Isacchi A, Moll J, Rusconi L
JBC
(2010) 285(16), 11775-11785

Through the “Gatekeeper Door”: Exploiting The Active Kinase Conformation
Zuccotto F, Ardini E, Casale E, Angiolini M
J Med Chem
(2010) 53, 2681-2694

The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound
Caporali S, Alvino E, Starace G, Ciomei M, Brasca M.G, Levati L, Garbin A, Castiglia D, Covaciu C, Bonmassar E, D’Atri S.
Pharmacol Research
(2010) 61, 437-448

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline Derivatives as a New Class of Orally and Selective Plk1 Inhibitors
Beria I, Ballinari D, Bertrand J, Borghi D, Bossi RT, Brasca MG, Cappella P, Caruso M, Ceccarelli W, Ciavolella A, Cinziani C, Croci V, DePonti A, Fachin G, Fergusson RD, Lansen J, Moll JK, Pesenti E, Posteri H, Perego R, Rocchetti M, Storici P et a
J. Med. Chem.
(2010) 53, 3532-3551