Geoffrey W. Krystal

TL;DR: STI571 efficiently blocked SCF-mediated activation of mitogen-activated protein kinase and Akt, but did not affect insulin-like growth factor-1 or serum-mediated mitogen -activated protein Kinase or Akt activation.

TL;DR: Six indolinone tyrosine kinase inhibitors were characterized for their ability to inhibit Kit kinase and for their effects on the growth of small cell lung cancer (SCLC) cell lines, suggesting that these compounds exhibit reasonable selectivity for inhibition of Kit-mediated proliferation.

TL;DR: A novel role for gene methylation that helped discriminate high BCL-2–expressing SCLCs is uncovered, suggesting that a substantial fraction of patients with SCLC could benefit from venetoclax.

TL;DR: It is demonstrated that SU5416 can inhibit SCLC growth by directly inhibiting tumor cell proliferation and by inhibited angiogenesis, in part by inhibiting Kit-mediated VEGF expression, which suggests that kinase inhibitors that target both Kit and VEGFR could play an important role in the treatment of SCLc, as well as other malignancies that express Kit.

TL;DR: The data suggest that growth inhibition and chemosensitization of SCLC by A12 is directly correlated with the ability to inhibit PI3K-Akt signaling, with those cell lines showing constitutive PI3k-Akk signaling displaying a high level of resistance to IGF-1R targeted therapy.