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Ref Type Journal Article
PMID (28711351)
Authors Goff D, Zhang J, Heckrodt T, Yu J, Ding P, Singh R, Holland S, Li W, Irving M
Title Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy.
Journal Vol Issue Date Pages Journal Short Title
Bioorganic & medicinal chemistry letters 27 16 2017 Aug 15 3766-3771 Bioorg Med Chem Lett
URL
Abstract Text Axl tyrosine kinase has been shown to be involved in multiple pathways contributing to tumor development, angiogenesis, and metastasis. High Axl expression has been observed in many human tumors where it appears to confer aggressive tumor behavior. Here we present several series of dual Axl-VEGF-R2 kinase inhibitors based on extensive optimization of an acyl diaminotriazole. It was hypothesized that dual inhibition of these two receptor tyrosine kinases may have a synergistic affect in inhibiting tumor angiogenesis and metastasis. One of these molecules, R916562 showed comparable activity to Sunitinib in two mouse tumor xenograft models and a mouse corneal micropocket model.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
R916562 R916562 0 0
TAK-243 TAK-243 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
R916562 AXL Inhibitor 30 VEGFR2 Inhibitor 37 R916562 is a small molecule that inhibits both Axl and Vegfr2, therefore results in synergistic inhibition of tumor angiogenesis and metastasis (PMID: 28711351).
TAK-243 MLN7243 TAK-243 (MLN7243) is an inhibitor that selectively targets the ubiquitin activating enzyme, UBA1, which may result in inhibition of ubiquitination related processes such as cell cycle progression, apoptotic regulation, and DNA damage response (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A164, PMID: 28711351).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References