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Page 1
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.
Menichincheri M, Ardini E, Magnaghi P, Avanzi N, Banfi P, Bossi R, Buffa L, Canevari G, Ceriani L, Colombo M, Corti L, Donati D, Fasolini M, Felder E, Fiorelli C, Fiorentini F, Galvani A, Isacchi A, Borgia AL, Marchionni C, Nesi M, Orrenius C, Panzeri A, Pesenti E, Rusconi L, Saccardo MB, Vanotti E, Perrone E, Orsini P. Menichincheri M, et al. Among authors: saccardo mb. J Med Chem. 2016 Apr 14;59(7):3392-408. doi: 10.1021/acs.jmedchem.6b00064. Epub 2016 Mar 30. J Med Chem. 2016. PMID: 27003761
Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications.
Ardini E, Menichincheri M, Banfi P, Bosotti R, De Ponti C, Pulci R, Ballinari D, Ciomei M, Texido G, Degrassi A, Avanzi N, Amboldi N, Saccardo MB, Casero D, Orsini P, Bandiera T, Mologni L, Anderson D, Wei G, Harris J, Vernier JM, Li G, Felder E, Donati D, Isacchi A, Pesenti E, Magnaghi P, Galvani A. Ardini E, et al. Among authors: saccardo mb. Mol Cancer Ther. 2016 Apr;15(4):628-39. doi: 10.1158/1535-7163.MCT-15-0758. Epub 2016 Mar 3. Mol Cancer Ther. 2016. PMID: 26939704
The TPM3-NTRK1 rearrangement is a recurring event in colorectal carcinoma and is associated with tumor sensitivity to TRKA kinase inhibition.
Ardini E, Bosotti R, Borgia AL, De Ponti C, Somaschini A, Cammarota R, Amboldi N, Raddrizzani L, Milani A, Magnaghi P, Ballinari D, Casero D, Gasparri F, Banfi P, Avanzi N, Saccardo MB, Alzani R, Bandiera T, Felder E, Donati D, Pesenti E, Sartore-Bianchi A, Gambacorta M, Pierotti MA, Siena S, Veronese S, Galvani A, Isacchi A. Ardini E, et al. Among authors: saccardo mb. Mol Oncol. 2014 Dec;8(8):1495-507. doi: 10.1016/j.molonc.2014.06.001. Epub 2014 Jun 12. Mol Oncol. 2014. PMID: 24962792 Free PMC article.
Correction to Discovery of Entrectinib: A New 3-Aminoindazole as a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.
Menichincheri M, Ardini E, Magnaghi P, Avanzi N, Banfi P, Bossi R, Buffa L, Canevari G, Ceriani L, Colombo M, Corti L, Donati D, Fasolini M, Felder E, Fiorelli C, Fiorentini F, Galvani A, Isacchi A, Borgia AL, Marchionni C, Nesi M, Orrenius C, Panzeri A, Pesenti E, Rusconi L, Saccardo MB, Vanotti E, Perrone E, Orsini P. Menichincheri M, et al. Among authors: saccardo mb. J Med Chem. 2019 Sep 12;62(17):8364. doi: 10.1021/acs.jmedchem.9b01259. Epub 2019 Aug 19. J Med Chem. 2019. PMID: 31424209 No abstract available.
Structure-based optimization of potent PDK1 inhibitors.
Angiolini M, Banfi P, Casale E, Casuscelli F, Fiorelli C, Saccardo MB, Silvagni M, Zuccotto F. Angiolini M, et al. Among authors: saccardo mb. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4095-9. doi: 10.1016/j.bmcl.2010.05.070. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20621725
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. Cucchi U, et al. Among authors: saccardo mb. Anticancer Res. 2010 Dec;30(12):4973-85. Anticancer Res. 2010. PMID: 21187478