Publications relevant to ARIAD’s programs
ARIAD’s scientific programs have been validated through extensive publications in the scientific literature. Listed below are key scientific publications of relevance to our product candidates.
mTOR Inhibition to Treat Solid Tumors & Other Malignancies
- Guertin, D.A & Sabatini, D.M. (2005) An Expanding Role for mTOR in Cancer. Trends Mol. Med. 11:353-361.
- Dancey, J.E. (2005) Inhibitors of the Mammalian Target of Rapamycin. Expert Opin. Investig. Drugs 14:313-328.
- Bjornsti, M.A. and Houghton, P.J. (2004) The mTOR Pathway: a Target for Cancer Therapy. Nat. Rev. Cancer 4:335-348.
- Mita, M.M., Mita, A. and Rowinsky, E.K. (2003) The Molecular Target of Rapamycin (mTOR) as a Therapeutic Target Against Cancer. Cancer Biology and Therapy 2:S169-S177.
Inhibition of Bcr/Abl and Src to Treat Leukemia
- O'Hare, T., Corbin, A.D. and Druker, B.J. (2006). Targeted CML Therapy: Controlling Drug Resistance, Seeking Cure. Curr. Opin. Genet. Dev. 16:92-99.
- Sausville, E.A. (2003) Is Another Bcr-Abl Inhibitor Needed for Chronic Myelogenous Leukemia? Clin. Cancer Res. 9:1233-4.
- Marcucci, G., Perrotti, D. and Caligiuri, M.A. (2003) Understanding the Molecular Basis of Imatinib Mesylate Therapy in Chronic Myelogenous Leukemia and the Related Mechanisms of Resistance. Clinical Cancer Research 9:1248-52.
Kinase Inhibitors for Cancer
- Dancey, J. and Sausville, E.A. (2003) Issues and Progress with Protein Kinase Inhibitors for Cancer Treatment. Nat. Rev. Drug Disc. 2:296-313.
- Blume-Jensen, P. and Hunter, T. (2001) Oncogenic Kinase Signalling. Nature 411:355-365.
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ARIAD Publications
ARIAD scientists have published extensively on the role of cell signaling in disease, the design of drugs to inhibit cell signaling, and on the development and use of cell-signaling regulation technology. A listing of recent publications is provided below.
Cell-signaling Inhibitors - Reviews and Commentaries
- Boyce, B.F., Xing, L., Yao, Z., Wang, Y., Shakespeare, W., Metcalf III, C., Sundaramoorthi, R., Dalgarno, D., Iuliucci, J., and Sawyer, T.K. (2006) Future Anti-Catabolic Therapeutic Targets in Bone Disease. Annals New York Acad. Sci., 1068: 447-457.
- Sawyer, T.K., Wang, Y., Shakespeare, W.C., Metcalf, C.A. III, Sundaramoorthi, R., Narula, S., and Dalgarno, D.C. (2006) Protein Kinase SMART Drug Design: Novel Phosphotyrosine and ATP Mimetic Inhibitors of Src. In Proteomics and Protein-Protein Interactions: Biology, Chemistry, Bioinformatics and Drug Design (G. Waksman, Ed.), Series on Protein Reviews, Vol. 3, Springer Publishers, pp. 219-253.
- Sawyer, T.K., Shakespeare, W.C., Wang, Y., Sundaramoorthi, R., Huang, W.-S., Metcalf, C.A. III, Thomas, M., Lawrence, B., Rozamus, L., Noehre, J., Zhu, X., Narula, S., Bohacek, R.S., Weigele, M., and Dalgarno, D.C. (2005) Protein Phosphorylation and Signal Transduction Modulation: Chemistry Perspectives for Small-Molecule Drug Discovery. Med. Chem. 1: 293-319.
- Metcalf, C.A., and Sawyer, T.K. (2004) Src Homology-2 Domains and Structure-Based, Small Molecule Library Approaches to Drug Discovery. In Drug Discovery Strategies and Methods, A. Makriyannis and D. Biegel (ed.), Marcel Dekker, New York. 23-59.
- Sawyer, T.K. (2004) Novel Oncogenic Protein Kinase Inhibitors for Cancer Therapy. Current Medicinal Chemistry: Anti-Cancer Agents 4: 449-455.
- Sawyer, T.K. (2004) Cancer Metastasis Therapeutic Targets and Drug Discovery: Emerging Small-Molecule Protein Kinase Inhibitors. Exp. Opin. Invest. Drugs 3:1-19.
- Sawyer, T.K., Bohacek, R.S., Metcalf III, C.A., Shakespeare, W.C., Wang, Y., Sundaramoorthi, R., Keenan, T., Narula, S., Weigele, M., and Dalgarno, D.C.(2003) Novel Protein Kinase Inhibitors: SMART Drug Design Technology. BioTechniques 34:S2-S15.
- Boyce, B.F., Xing, L., Shakespeare, W., Wang, Y., Dalgarno, D., Iuliucci, J., and Sawyer, T. (2003) Regulation of bone remodeling and emerging breakthrough drugs for osteoporosis and osteolytic bone metastases. Kidney Intern. 85:52-55.
- Shakespeare, W.C., Metcalf, C.A. III, Wang, Y., Sundaramoorthi, R., Keenan, T.P., Weigele, M., Bohacek R.S., Dalgarno, D.C., and Sawyer, T.K. (2003) Novel bone-targeted Src tyrosine kinase inhibitor drug discovery. Curr Opin Drug Discov Devel. 6: 729-41.
- Metcalf, C.A., van Schravendijk, M.R., Dalgarno, D.C., and Sawyer, T.K., (2002) Targeting Protein Kinases for Bone Disease: Discovery and Development of Src Inhibitors .Current Pharmaceutical Design 8: 2049-2075.
Cell-signaling Inhibitors - Primary Research Publications
- Azam, M., Nardi, V., Latek, R.R., Shakespeare, W.C., Metcalf III, C.A., Bohacek, R.S., Wang, Y., Sundaramoorthi, R., Veach, D.R., Bornmann, W.G., Clarkson, B., Dalgarno, D.C., Sawyer, T.K., and Daley, G.Q., (2006) Activity of Dual SRC-ABL Inhibitors Highlights Role of BCR/ABL Kinase Dynamics in Drug Resistance. Proc. Natl. Acad. Sci. USA, 103: 9244-9249.
- Lesslie III, D.P., Trevino, J.G., Sawyer, T.K., Shakespeare, W.C., Metcalf III, C.A., Hicklin, D.J., Ellis, L.M., and Gallick, G.E. (2006) Vascular Endothelial Growth Factor Receptor-1 Mediates Cellular Migration of Colon Carcinoma Cells Through Activation of Src Family Kinases. British J. Pharmacology, 94: 1710-1717.
- Summy, J.S., Trevino, J.G., Lesslie, D.P., Baker, C.H., Shakespeare, W.C., Wang, Y., Keats, J.A., Sundaramoorthi, R., Metcalf III, C.A., Sawyer, T.K., and Gallick, G.E., (2005) AP23846, a Novel and Highly Potent Src Family Kinase Inhibitor, Reduces VEGF and IL-8 Expression in Human Solid Tumor Cell Lines and Abrogates Downstream Angiogenic Processes. Molec. Cancer Ther. 4: 1900-1911.
- Dalgarno, D., Stehle, T., Narula, S., Schelling, P., van Schravendijk, M., Adams, S., Andrade, L., Keats, J., Ram, M., Jin, L., Grossman, T., Metcalf III, C., Shakespeare, W., Wang, Y., Keenan, T., Sundaramoorthi, R. Bohacek, R., Weigele, M., and Sawyer, T.K., (2006) Structural Basis of Src Kinase Inhibition with a New Class of Potent and Selective Trisubstituted Purine-Based Compounds. Chem. Biol. Drug Design 67: 46-57.
- Corbin, A.S., Demehri, S., Griswold, I.J., Wang, Y., Metcalf, C.A., Sundaramoorthi, R., Shakespeare, W.C., Snodgrass, J., Dalgarno, D.C., Iulliucci, J., Sawyer, T.K., Heinrich, M.C., Druker, B.J. and Deininger, M.W.N. (2005) In Vitro and In Vivo Activity of Novel ATP-based Oncogenic Protein Kinase Inhibitors AP23464 and AP23848 Against Activation Loop Mutants of KIT. Blood 106: 227-234.
- Brunton, V.G., Avizienyte, E., Fincham, V.J., Serrels, B., Metcalf, C.A., Sawyer, T.K., and Frame, M.C. (2005) Identification of Src-Specific Phosphorylation Site on FAK: Dissection of the Role of Src SH2 and Catalytic Functions and Their Consequences for Tumor Behavior. Cancer Res. 65: 1335-1342.
- O'Hare, T., Pollock R., Stoffregen, E.P., Keats, J.A., Abdullah, O.M., Moseson, E.M., Rivera, V.M., Tang, H., Metcalf, C.A., Bohacek, R.S., Wang, Y., Sundaramoorthi, R., Shakespeare, W.C., Dalgarno, D., Clackson, T., Sawyer, T.K., Deininger, M.W., and Druker, B.J. (2004) Inhibition of Wild-Type and Mutant Bcr-Abl by AP23464, a Potent ATP-based Oncogenic Protein Kinase Inhibitor: Implications for CML. Blood 104: 2532-2539.
- Sundaramoorthi, R., Shakespeare, W.C., Keenan, T.P., Metcalf, C.A. III, Wang, Y., Mani, U., Merry, T., Liu, S., Bohacek, R.S., Narula, S.S., Dalgarno, D.C., Van Schravendijk, M.R., Violette, S.M., Liou, S., Adams, S., Ram M.R., Keats, J.A., Weigele, M., and Sawyer., T.K. (2003) Bone-targeted Src kinase inhibitors: Novel pyrrolo- and pyrazolopyrimidine analogs. Bioorg. Med. Chem. Lett. 13: 3063-3066.
- Vu, C., Luke, G.P., Kawahata, N., Shakespeare, W.C., Wang, Y., Sundaramoorthi, R., Metcalf, C.A. III, Keenan, T.P., Pradeepan, S., Corpuz, E., Merry, T., Bohacek, R.S., Dalgarno, D.C., Narula, S.S., Van Schravendijk, M.R., Ram, M.K., Adams, S., Liou, S., Keats, J.A., Violette, S.M., Guan W., Weigele, M., and Sawyer, T.K. (2003) Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: Potent inhibitors of Src tyrosine kinase as novel antiresorptive agents. Bioorg. Med. Chem. Lett. 13: 3071-3074.
- Wang, Y., Metcalf, C.A. III, Shakespeare, W.C., Sundaramoorthi, R., Keenan, T.P., Bohacek, R.S., Van Schravendijk, M.R., Violette, S.M., Narula, S.S., Dalgarno, D.C., Haraldson, C., Keats, J., Liou S., Mani, U., Pradeepan, S., Ram, M., Adams, S., Weigele, M., and Sawyer, T.K.(2003) Bone-targeted 2,6,9-trisubstituted purines: Novel inhibitors of Src tyrosine kinase for the treatment of bone diseases. Bioorg. Med. Chem. Lett. (2003) 13: 3067-3070.
Cell-signaling Regulation Technologies
More than 250 scientific publications have described the use of our Cell-signaling regulation technologies in diverse areas of biological research, including many papers authored by ARIAD scientists. A complete and annotated listing of these papers can be found in the Regulation Kits section of the website.
