2. Academic Validation
  3. 9-ING-41, a small molecule inhibitor of GSK-3beta, potentiates the effects of anticancer therapeutics in bladder cancer

9-ING-41, a small molecule inhibitor of GSK-3beta, potentiates the effects of anticancer therapeutics in bladder cancer

  • Sci Rep. 2019 Dec 27;9(1):19977. doi: 10.1038/s41598-019-56461-4.
Hiroo Kuroki 1,  Tsutomu Anraku 1,  Akira Kazama 1,  Vladimir Bilim 1 2,  Masayuki Tasaki 1,  Daniel Schmitt 3,  Andrew P Mazar 4,  Francis J Giles 3,  Andrey Ugolkov 3,  Yoshihiko Tomita 5
Affiliations

Affiliations

  • 1 Department of Urology, Molecular Oncology, Graduate School of Medical and Dental Sciences, Niigata University, Niigata, Japan.
  • 2 Kameda Daiichi Hospital, Niigata, Japan.
  • 3 Actuate Therapeutics, Fort Worth, TX, USA.
  • 4 Monopar Therapeutics, Wilmette, IL, USA.
  • 5 Department of Urology, Molecular Oncology, Graduate School of Medical and Dental Sciences, Niigata University, Niigata, Japan. ytomita@med.niigata-u.ac.jp.
PMID: 31882719 DOI: 10.1038/s41598-019-56461-4
Abstract

Glycogen synthase kinase-3 beta (GSK-3β), a serine/threonine kinase, has been identified as a potential therapeutic target in human bladder Cancer. In the present study, we investigated the antitumor effect of a small molecule GSK-3β Inhibitor, 9-ING-41, currently in clinical studies in patients with advanced Cancer, in bladder Cancer cell lines. We found that treatment with 9-ING-41 leads to cell cycle arrest, Autophagy and Apoptosis in bladder Cancer cells. The Autophagy Inhibitor chloroquine potentiated the antitumor effects of 9-ING-41 when tested in combination studies. Our findings also demonstrate that 9-ING-41 enhanced the growth inhibitory effects of gemcitabine or cisplatin when used in combination in bladder Cancer cells. Finally, we found that 9-ING-41 sensitized bladder Cancer cells to the cytotoxic effects of human immune effector cells. Our results provide a rationale for the inclusion of patients with advanced bladder Cancer in clinical studies of 9-ING-41.

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