The DOI matches its Crossref record; 24 of the 24 references it cites were found in a registry or an index.
An Orally Administered Multitarget Tyrosine Kinase Inhibitor, SU11248, Is a Novel Potent Inhibitor of Thyroid Oncogenic RET/Papillary Thyroid Cancer Kinases
Abstract
Context: The oncogenic RET/PTC tyrosine kinase causes papillary thyroid cancer (PTC). The use of inhibitors specific for RET/PTC may be useful for targeted therapy of PTC. Objective: The objective of the study was to evaluate the efficacies of the recently developed kinase inhibitors SU11248, SU5416, and SU6668 in inhibition of RET/PTC. Design: SU11248, SU5416, and SU6668 were synthesized, and their inhibitory potencies were evaluated using an in vitro RET/PTC kinase assay. The inhibitory effects of the compounds on RET/PTC were evaluated by quantifying the autophosphorylation of RET/PTC, signal transducer and activator of transcription (STAT)-3 activation, and the morphological reversal of RET/PTC-transformed cells. Results: An in vitro kinase assay revealed that SU5416, SU6668, and SU11248 inhibited phosphorylation of the synthetic tyrosine kinase substrate peptide E4Y by RET/PTC3 in a dose-dependent manner with IC50 of approximately 944 nm for SU5416, 562 nm for SU6668, and 224 nm for SU11248. Thus, SU11248 effectively inhibits the kinase activity of RET/PTC3. RET/PTC-mediated Y705 phosphorylation of STAT3 was inhibited by addition of SU11248, and the inhibitory effects of SU11248 on the tyrosine phosphorylation and transcriptional activation of STAT3 were very closely correlated with decreased autophosphorylation of RET/PTC. SU11248 caused a complete morphological reversion of transformed NIH-RET/PTC3 cells and inhibited the growth of TPC-1 cells that have an endogenous RET/PTC1. Conclusion: SU11248 is a highly effective tyrosine kinase inhibitor of the RET/PTC oncogenic kinase.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
1 retracted
Melillo, R. M., Castellone, M. D., Guarino, V., De Falco, V., Cirafici, A. M., Salvatore, G., Caiazzo, F., Basolo, F., Giannini, R., Kruhoffer, M., et al. (2016) · Journal of Clinical Investigation · doi:10.1172/jci87345 · Cited by 306
RetractedHansen, M. B., Nielsen, S. E., & Berg, K. (1989) · Journal of Immunological Methods · doi:10.1016/0022-1759(89)90397-9 · Cited by 3,507
Mendel, D. B., Laird, A., Xin, X., Louie, S. G., Christensen, J. G., Li, G., Schreck, R., Abrams, T. J., Ngai, T. J., Lee, L. B., et al. (2003) · PubMed · Cited by 1,961
Motzer, R. J., Michaelson, M. D., Redman, B. G., Hudes, G. R., Wilding, G., Figlin, R. A., Ginsberg, M. S., Kim, S. T., Baum, C. M., DePrimo, S. E., et al. (2006) · Journal of Clinical Oncology · doi:10.1200/jco.2005.02.2574 · Cited by 1,634
Faivre, S., Delbaldo, C., Vera, K., Robert, C., Lozahic, S., Lassau, N., Bello, C., Deprimo, S., Brega, N., Massimini, G., et al. (2006) · Journal of Clinical Oncology · doi:10.1200/jco.2005.02.2194 · Cited by 1,164
Grieco, M., Santoro, M., Berlingieri, M. T., Melillo, R. M., Donghi, R., Bongarzone, I., Pierotti, M. A., Della Ports, G., Fusco, A., & Vecchiot, G. (1990) · Cell · doi:10.1016/0092-8674(90)90659-3 · Cited by 959
SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo
O'Farrell, A.-M., Abrams, T. J., Yuen, H. A., Ngai, T. J., Louie, S. G., Yee, K. W. H., Wong, L. M., Hong, W., Lee, L. B., Town, A., et al. (2003) · Blood · doi:10.1182/blood-2002-07-2307 · Cited by 864
Carlomagno, F., Vitagliano, D., Guida, T., Ciardiello, F., Tortora, G., Vecchio, G., Ryan, A. J., Fontanini, G., Fusco, A., & Santoro, M. M. (2002) · PubMed · Cited by 569
Sawka, A. M., Thephamongkhol, K., Brouwers, M., Thabane, L., Browman, G., & Gerstein, H. C. (2004) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2003-031167 · Cited by 432
The RET proto-oncogene in human cancers
Jhiang, S. M. (2000) · Oncogene · doi:10.1038/sj.onc.1203857 · Cited by 298
Cited by
Cardiotoxicity associated with tyrosine kinase inhibitor sunitinib
Chu, T. F., Rupnick, M. A., Kerkela, R., Dallabrida, S. M., Zurakowski, D., Nguyen, L., Woulfe, K., Pravda, E., Cassiola, F., Desai, J., et al. (2007) · The Lancet · doi:10.1016/s0140-6736(07)61865-0 · Cited by 1,083
Possible molecular mechanisms involved in the toxicity of angiogenesis inhibition
Verheul, H. M. W., & Pinedo, H. M. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2152 · Cited by 503
Houk, B. E., Bello, C. L., Poland, B., Rosen, L. S., Demetri, G. D., & Motzer, R. J. (2010) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-009-1170-y · Cited by 477
New therapeutic approaches for metastatic thyroid carcinoma
Baudin, E., & Schlumberger, M. (2007) · The Lancet Oncology · doi:10.1016/s1470-2045(07)70034-7 · Cited by 143
The Structure of Clinical Translation: Efficiency, Information, and Ethics
Kimmelman, J., & London, A. J. (2015) · Hastings Center Report · doi:10.1002/hast.433 · Cited by 85
Metadata
- Authors
- Kim, D. W., Jo, Y. S., Jung, H. S., Chung, H. K., Song, J. H., Park, K. C., Park, S. H., Hwang, J. H., Rha, S. Y., Kweon, G. R., Lee, S.-J., Jo, K.-W., & Shong, M.
- Venue
- The Journal of Clinical Endocrinology & Metabolism
- Publisher
- The Endocrine Society
- Published
- 2006-10-01
- Volume
- 91
- Issue
- 10
- Pages
- 4070-4076
- ISSN
- 0021-972X (ISSN-L)
- 1945-7197
- OpenAlex
- W2031614751
- Cited by
- 279
- References
- 24
- FWCI
- 18.56
- Type
- journal article
- Language
- en
- Open access
- closed
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: An Orally Administered Multitarget Tyrosine Kinase Inhibitor, SU11248, Is a Novel Potent Inhibitor of Thyroid Oncogenic RET/Papillary Thyroid Cancer Kinases. https://app.cochat.ai/papers/10.1210/jc.2005-2845
- The paper
- Kim, D. W., Jo, Y. S., Jung, H. S., Chung, H. K., Song, J. H., Park, K. C., Park, S. H., Hwang, J. H., Rha, S. Y., Kweon, G. R., Lee, S.-J., Jo, K.-W., & Shong, M. (2006). An Orally Administered Multitarget Tyrosine Kinase Inhibitor, SU11248, Is a Novel Potent Inhibitor of Thyroid Oncogenic RET/Papillary Thyroid Cancer Kinases. The Journal of Clinical Endocrinology & Metabolism. https://doi.org/10.1210/jc.2005-2845
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
