Kinase Inhibition in Kidney Cancer

NIH RePORTER · NIH · R01 · $432,423 · view on reporter.nih.gov ↗

Abstract

ABSTRACT The incidence of renal cell carcinoma (RCC) is on the rise. 65,000 new cases occur annually in the United States. Vascular endothelial growth factor receptor (VEGFR) and mammalian target of rapamycin (mTOR) inhibitors are FDA approved and commonly used treatments for advanced RCC but result in increases in overall survival by only months. At this time, the most druggable portion of the genome remains the kinome. Through unbiased, high-throughput screening we have identified and validated the therapeutic value of a novel kinase in RCC, tyrosine kinase 2 (TYK2: a member of the Janus Kinase family) and demonstrate that it plays a role in mTOR inhibitor resistance. We have characterized a signaling network in which TYK2 positively regulates the SRC family kinases (SFKs) and demonstrate that dual inhibition of mTOR and SRC with everolimus and dasatinib induces tumor regression in vivo. Based on these results we hypothesize that inhibition of the TYK2/SRC axis is a tractable therapeutic strategy in a subset of RCC, that we can define predictive markers of TYK2/SRC inhibitor response, and that defining the kinomic landscape of RCC and its response to mTOR inhibition will lead to further combinatorial targets.

Key facts

NIH application ID
9988187
Project number
5R01CA202053-05
Recipient
UNIV OF NORTH CAROLINA CHAPEL HILL
Principal Investigator
WILLIAM Y. KIM
Activity code
R01
Funding institute
NIH
Fiscal year
2020
Award amount
$432,423
Award type
5
Project period
2016-09-02 → 2021-07-31