The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Overriding Imatinib Resistance with a Novel ABL Kinase Inhibitor
Abstract
Resistance to the ABL kinase inhibitor imatinib (STI571 or Gleevec) in chronic myeloid leukemia (CML) occurs through selection for tumor cells harboring BCR-ABL kinase domain point mutations that interfere with drug binding. Crystallographic studies predict that most imatinib-resistant mutants should remain sensitive to inhibitors that bind ABL with less stringent conformational requirements. BMS-354825 is an orally bioavailable ABL kinase inhibitor with two-log increased potency relative to imatinib that retains activity against 14 of 15 imatinib-resistant BCR-ABL mutants. BMS-354825 prolongs survival of mice with BCR-ABL–driven disease and inhibits proliferation of BCR-ABL–positive bone marrow progenitor cells from patients with imatinib-sensitive and imatinib-resistant CML. These data illustrate how molecular insight into kinase inhibitor resistance can guide the design of second-generation targeted therapies.
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Cites
Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification
Gorre, M. E., Mohammed, M., Ellwood, K., Hsu, N., Paquette, R., Rao, P. N., & Sawyers, C. L. (2001) · Science · doi:10.1126/science.1062538 · Cited by 3,104
Self-citationDeng, M., & Daley, G. Q. (2001) · Blood · doi:10.1182/blood.v97.11.3491 · Cited by 50
Cited by
Cancer drug resistance: an evolving paradigm
Holohan, C., Van Schaeybroeck, S., Longley, D. B., & Johnston, P. G. (2013) · Nature Reviews Cancer · doi:10.1038/nrc3599 · Cited by 4,681
EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib
Kobayashi, S., Boggon, T. J., Dayaram, T., Jänne, P. A., Kocher, O., Meyerson, M., Johnson, B. E., Eck, M. J., Tenen, D. G., & Halmos, B. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa044238 · Cited by 3,964
Pao, W., Miller, V. A., Politi, K. A., Riely, G. J., Somwar, R., Zakowski, M. F., Kris, M. G., & Varmus, H. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020073 · Cited by 3,527
“The new drugs bind to ABL in an ‘‘open’’ conformation, as opposed to imatinib, which binds ABL in a ‘‘closed’’ conformation [12,13].”
BackgroundDasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias
Talpaz, M., Shah, N. P., Kantarjian, H., Donato, N., Nicoll, J., Paquette, R., Cortes, J., O'Brien, S., Nicaise, C., Bleickardt, E., et al. (2006) · New England Journal of Medicine · doi:10.1056/nejmoa055229 · Cited by 1,760
Self-citationSteeg, P. S. (2016) · Nature Reviews Cancer · doi:10.1038/nrc.2016.25 · Cited by 1,363
Metadata
- Authors
- Shah, N. P., Tran, C., Lee, F. Y., Chen, P., Norris, D., & Sawyers, C. L.
- Venue
- Science
- Published
- 2004-07-16
- Volume
- 305
- Issue
- 5682
- Pages
- 399-401
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2092606584
- Cited by
- 1,796
- References
- 2
- FWCI
- 92.85
- Type
- journal article
- Language
- en
- Open access
- closed
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