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References

  • 1
    Cohen P. (2002) Protein kinases–the major drug targets of the twenty-first century? Nat Rev Drug Discov;1:309315.
  • 2
    Ottmann O.G., Druker B.J., Sawyers C.L., Goldman J.M., Reiffers J., Silver R.T., Tura S. et al. (2002) A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias. Blood;100:19651971.
  • 3
    Sawyers C.L., Hochhaus A., Feldman E., Goldman J.M., Miller C.B., Ottmann O.G., Schiffer C.A. et al. (2002) Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study. Blood;99:35303539.
  • 4
    Gorre M.E., Mohammed M., Ellwood K., Hsu N., Paquette R., Rao P.N., Sawyers C.L. (2001) Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science;293:876880.
  • 5
    Shah N.P., Nicoll J.M., Nagar B., Gorre M.E., Paquette R.L., Kuriyan J., Sawyers C.L. (2002) Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell;2:117125.
  • 6
    von Bubnoff N., Schneller F., Peschel C., Duyster J. (2002) BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: a prospective study. Lancet;359:487491.
  • 7
    Noble M.E., Endicott J.A., Johnson L.N. (2004) Protein kinase inhibitors: insights into drug design from structure. Science;303:18001805.
  • 8
    Tamborini E., Pricl S., Negri T., Lagonigro M.S., Miselli F., Greco A., Gronchi A., Casali P.G., Ferrone M., Fermeglia M., Carbone A., Pierotti M.A., Pilotti S. (2006) Functional analyses and molecular modeling of two c-Kit mutations responsible for imatinib secondary resistance in GIST patients. Oncogene;25:61406146.
  • 9
    Pao W., Miller V.A., Politi K.A., Riely G.J., Somwar R., Zakowski M.F., Kris M.G., Varmus H. (2005) Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med;2:e73.
  • 10
    von Bubnoff N., Sandherr M., Schlimok G., Andreesen R., Peschel C., Duyster J. (2005) Myeloid blast crisis evolving during imatinib treatment of an FIP1L1-PDGFR alpha-positive chronic myeloproliferative disease with prominent eosinophilia. Leukemia;19:286287.
  • 11
    Azam M., Nardi V., Shakespeare W.C., Metcalf C.A. III, Bohacek R.S., Wang Y., Sundaramoorthi R., Sliz P., Veach D.R., Bornmann W.G., Clarkson B., Dalgarno D.C., Sawyer T.K., Daley G.Q. (2006) Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proc Natl Acad Sci USA;103:92449249.
  • 12
    Azam M., Seeliger M.A., Gray N.S., Kuriyan J., Daley G.Q. (2008) Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol;15:11091118.
  • 13
    O'Hare T., Walters D.K., Stoffregen E.P., Jia T., Manley P.W., Mestan J., Cowan-Jacob S.W., Lee F. Y., Heinrich M.C., Deininger M.W., Druker B. J. (2005) In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res;65:45004505.
  • 14
    Shah N.P., Tran C., Lee F.Y., Chen P., Norris D., Sawyers C.L. (2004) Overriding imatinib resistance with a novel ABL kinase inhibitor. Science;305:399401.
  • 15
    Weisberg E., Manley P.W., Breitenstein W., Bruggen J., Cowan-Jacob S.W., Ray A., Huntly B. et al. (2005) Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell;7:129141.
  • 16
    Seeliger M.A., Ranjitkar P., Kasap C., Shan Y., Shaw D.E., Shah N.P., Kuriyan J., Maly D.J. (2009) Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations. Cancer Res;69:23842392.
  • 17
    Weisberg E., Choi H.G., Ray A., Barrett R., Zhang J., Sim T., Zhou W. et al. (2010) Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants. Blood;115:42064216.
  • 18
    Wetzel S., Klein K., Renner S., Rauh D., Oprea T.I., Mutzel P., Waldmann H. (2009) Interactive exploration of chemical space with Scaffold Hunter. Nat Chem Biol;5:581583.
  • 19
    Bemis G.W., Murcko M.A. (1996) The properties of known drugs. 1. Molecular frameworks. J Med Chem;39:28872893.
  • 20
    Huang N., Shoichet B.K., Irwin J.J. (2006) Benchmarking sets for molecular docking. J Med Chem;49:67896801.
  • 21
    Halgren T.A., Murphy R.B., Friesner R.A., Beard H.S., Frye L.L., Pollard W.T., Banks J.L. (2004) Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening. J Med Chem;47:17501759.
  • 22
    Friesner R.A., Banks J.L., Murphy R.B., Halgren T.A., Klicic J.J., Mainz D.T., Repasky M.P., Knoll E.H., Shelley M., Perry J.K., Shaw D.E., Francis P., Shenkin P.S. (2004) Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy. J Med Chem;47:17391749.
  • 23
    Rosen J., Lovgren A., Kogej T., Muresan S., Gottfries J., Backlund A. (2009) ChemGPS-NP(Web): chemical space navigation online. J Comput Aided Mol Des;23:253259.
  • 24
    Engh R.A., Bossemeyer D. (2002) Structural aspects of protein kinase control-role of conformational flexibility. Pharmacol Ther;93:99111.
  • 25
    Schindler T., Bornmann W., Pellicena P., Miller W.T., Clarkson B., Kuriyan J. (2000) Structural mechanism for STI-571 inhibition of abelson tyrosine kinase. Science;289:19381942.
  • 26
    Zuccotto F., Ardini E., Casale E., Angiolini M. (2010) Through the “gatekeeper door”: exploiting the active kinase conformation. J Med Chem;53:26812694.
  • 27
    Brooijmans N., Humblet C. (2010) Chemical space sampling in virtual screening by different crystal structures. Chem Biol Drug Des;76:472479.
  • 28
    Andersson C.D., Chen B.Y., Linusson A. (2010) Multivariate assessment of virtual screening experiments. J Chemom;24:757767.
  • 29
    Mysinger M.M., Carchia M., Irwin J.J., Shoichet B.K. (2012) Directory of useful decoys, enhanced (DUD-E): better ligands and decoys for better benchmarking. J Med Chem;55:65826594.
  • 30
    Rohrer S.G., Baumann K. (2009) Maximum unbiased validation (MUV) data sets for virtual screening based on PubChem bioactivity data. J Chem Inf Model;49:169184.
  • 31
    Posy S.L., Hermsmeier M.A., Vaccaro W., Ott K.H., Todderud G., Lippy J.S., Trainor G.L., Loughney D.A., Johnson S.R. (2010) Trends in kinase selectivity: insights for target class-focused library screening. J Med Chem;54:5466.
  • 32
    Modugno M., Casale E., Soncini C., Rosettani P., Colombo R., Lupi R., Rusconi L., Fancelli D., Carpinelli P., Cameron A.D., Isacchi A., Moll J. (2007) Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358. Cancer Res;67:79877990.
  • 33
    Zhou T., Parillon L., Li F., Wang Y., Keats J., Lamore S., Xu Q., Shakespeare W., Dalgarno D., Zhu X. (2007) Crystal structure of the T315I mutant of AbI kinase. Chem Biol Drug Des;70:171181.
  • 34
    Chan W.W., Wise S.C., Kaufman M.D., Ahn Y.M., Ensinger C.L., Haack T., Hood M.M. et al. (2011) Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell;19:556568.
  • 35
    Zhou T., Commodore L., Huang W.S., Wang Y., Thomas M., Keats J., Xu Q., Rivera V.M., Shakespeare W.C., Clackson T., Dalgarno D.C., Zhu X. (2011) Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance. Chem Biol Drug Des;77:111.