2. Academic Validation
  3. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo

GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo

  • Cancer Lett. 2016 May 28;375(1):172-178. doi: 10.1016/j.canlet.2016.02.017.
Zhang Zhang 1,  Xiaomei Ren 2,  Xiaoyun Lu 2,  Deping Wang 2,  Xianjing Hu 3,  Yi Zheng 2,  Liyan Song 3,  Hongwen Pang 2,  Rongmin Yu 4,  Ke Ding 5
Affiliations

Affiliations

  • 1 School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou 510530, China.
  • 2 State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou 510530, China.
  • 3 School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.
  • 4 School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China. Electronic address: tyrm@jnu.edu.cn.
  • 5 School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou 510530, China. Electronic address: ding_ke@gibh.ac.cn.
PMID: 26940138 DOI: 10.1016/j.canlet.2016.02.017
Abstract

Platelet-derived growth factor receptors (PDGFRα/β) play critical roles in the autocrine-stimulated growth and recruitment of cancer-associated fibroblasts (CAFs) of human lung Cancer cells. We have identified GZD856 as a new PDGFR Inhibitor that potently inhibits PDGFRα/β kinase activity and blocks this signaling pathway in lung Cancer cells both in vitro and in vivo. GZD856 strongly suppresses the proliferation of PDGFRα-amplified H1703 (PDGFRβ(-)) human lung Cancer cells and demonstrates significant in vivo antitumor efficacy in a xenograft mouse model. Although GZD856 displays only limited in vitro antiproliferative efficiency against PDGFRα(-)/PDGFRβ(+) A549 lung Cancer cells, it efficiently inhibits the in vivo growth and metastasis of A549 Cancer cells in xenograft and orthotopic models, respectively. The promising in vivo antitumor activity of GZD856 in A549 models may result from its suppression of PDGFR-related microenvironment factors, such as recruitment of CAFs and collagen content in stromal cells. GZD856 may be considered as a promising new candidate for anti-lung Cancer drug development.

Keywords

GZD856; Lung cancer; Metastasis; PDGFRα/β inhibitor; Stromal.

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