The DOI matches its Crossref record; 10 of the 10 references it cites were found in a registry or an index.
SRC: A Century of Science Brought to the Clinic
Open accessAbstract
The SRC family kinases are the largest family of nonreceptor tyrosine kinases and one of the best-studied targets for cancer therapy. SRC, arguably the oldest oncogene, has been implicated in pathways regulating proliferation, angiogenesis, invasion and metastasis, and bone metabolism. More recently, researchers have proposed that the transforming ability of SRC is linked to its ability to activate key signaling molecules in these pathways, rather than through direct activity. It has been hypothesized that blocking SRC activation may inhibit these pathways, resulting in antitumor activity. However, successfully targeting SRC in a clinical setting remains a challenge, and SRC inhibitors have only recently begun to move through clinical development. Preclinical studies have identified specific molecular "subgroups" and histologies that may be more sensitive to SRC inhibition. In addition, other studies have demonstrated synergistic interactions between SRC inhibitors and other targeted therapies and cytotoxics. In this review, we summarize SRC biology and how it has been applied to the clinical development of SRC inhibitors. The status of SRC inhibitors, including dasatinib, saracatinib, and bosutinib, which are in phase 1, 2, and 3 trials, is highlighted.
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Cites
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“Breast cancers within this subgroup express basal cell cytokeratins (CK5 and CK17), do not express estrogen (ER) or progesterone receptors (PRs) or HER2 [45,46], and are notorious for poor prognosis [47].”
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Cited by
The Blood-Testis Barrier and Its Implications for Male Contraception
Cheng, C. Y., & Mruk, D. D. (2012) · Pharmacological Reviews · doi:10.1124/pr.110.002790 · Cited by 927
Activation pathway of Src kinase reveals intermediate states as targets for drug design
Shukla, D., Meng, Y., Roux, B., & Pande, V. S. (2014) · Nature Communications · doi:10.1038/ncomms4397 · Cited by 333
Park, J. H., Vithayathil, S., Kumar, S., Sung, P.-L., Dobrolecki, L. E., Putluri, V., Bhat, V. B., Bhowmik, S. K., Gupta, V., Arora, K., et al. (2016) · Cell Reports · doi:10.1016/j.celrep.2016.02.004 · Cited by 313
Mechanisms of Taxane Resistance
Maloney, S., Spring, C., Morejon-Lasso, L., & Prosperi, J. (2020) · Cancers · doi:10.3390/cancers12113323 · Cited by 198
Src family kinases and paclitaxel sensitivity
Le, X.-F., & Bast, Jr. (2011) · Cancer Biology & Therapy · doi:10.4161/cbt.12.4.16430 · Cited by 79
Metadata
- Authors
- Aleshin, A., & Finn, R. S.
- Venue
- Neoplasia
- Publisher
- Elsevier BV
- Published
- 2010-08
- Volume
- 12
- Issue
- 8
- Pages
- 599-607
- ISSN
- 1476-5586 (ISSN-L)
- OpenAlex
- W1536452773
- Cited by
- 211
- References
- 10
- FWCI
- 16.35
- Type
- journal article
- Language
- en
- Open access
- gold
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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