2. Academic Validation
  3. Molecular Inhibitor of QSOX1 Suppresses Tumor Growth In Vivo

Molecular Inhibitor of QSOX1 Suppresses Tumor Growth In Vivo

  • Mol Cancer Ther. 2020 Jan;19(1):112-122. doi: 10.1158/1535-7163.MCT-19-0233.
Amber L Fifield 1,  Paul D Hanavan 2,  Douglas O Faigel 3,  Eduard Sergienko 4,  Andrey Bobkov 4,  Nathalie Meurice 5,  Joachim L Petit 5,  Alysia Polito 5,  Thomas R Caulfield 6 7 8 9 10,  Erik P Castle 11,  John A Copland 8,  Debabrata Mukhopadhyay 12,  Krishnendu Pal 12,  Shamit K Dutta 12,  Huijun Luo 13,  Thai H Ho 14,  Douglas F Lake 15
Affiliations

Affiliations

  • 1 School of Life Sciences, Arizona State University, Tempe, Arizona.
  • 2 RenBio, Inc., New York, New York.
  • 3 Division of Gastroenterology and Hepatology, Department of Internal Medicine, Mayo Clinic, Phoenix, Arizona.
  • 4 Assay Development, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California.
  • 5 Hematology/Oncology, Mayo Clinic, Scottsdale, Arizona.
  • 6 Department of Neuroscience, Mayo Clinic, Jacksonville, Florida.
  • 7 Mayo Graduate School, Neurobiology of Disease, Mayo Clinic, Jacksonville, Florida.
  • 8 Department of Cancer Biology, Mayo Clinic, Jacksonville, Florida.
  • 9 Health Sciences Research, Division of Biomedical Statistics & Informatics, Mayo Clinic, Jacksonville, Florida.
  • 10 Center for Individualized Medicine, Mayo Clinic, Jacksonville, Florida.
  • 11 Department of Urology, Mayo Clinic, Phoenix, Arizona.
  • 12 Department of Biochemistry and Molecular Biology, Mayo Clinic, Jacksonville, Florida.
  • 13 Division of Hematology/Oncology, Mayo Clinic, Phoenix, Arizona.
  • 14 Division of Hematology/Oncology, Mayo Clinic, Phoenix, Arizona. Ho.Thai@mayo.edu Douglas.Lake@asu.edu.
  • 15 School of Life Sciences, Arizona State University, Tempe, Arizona. Ho.Thai@mayo.edu Douglas.Lake@asu.edu.
PMID: 31575656 DOI: 10.1158/1535-7163.MCT-19-0233
Abstract

Quiescin sulfhydryl oxidase 1 (QSOX1) is an Enzyme overexpressed by many different tumor types. QSOX1 catalyzes the formation of disulfide bonds in proteins. Because short hairpin knockdowns (KD) of QSOX1 have been shown to suppress tumor growth and invasion in vitro and in vivo, we hypothesized that chemical compounds inhibiting QSOX1 enzymatic activity would also suppress tumor growth, invasion, and metastasis. High throughput screening using a QSOX1-based enzymatic assay revealed multiple potential QSOX1 inhibitors. One of the inhibitors, known as "SBI-183," suppresses tumor cell growth in a Matrigel-based spheroid assay and inhibits invasion in a modified Boyden chamber, but does not affect viability of nonmalignant cells. Oral administration of SBI-183 inhibits tumor growth in 2 independent human xenograft mouse models of renal cell carcinoma. We conclude that SBI-183 warrants further exploration as a useful tool for understanding QSOX1 biology and as a potential novel Anticancer agent in tumors that overexpress QSOX1.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-165245
    QSOX1抑制剂
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