Advanced search
Publication Cover
Journal of Drug Targeting Volume 27, 2019 - Issue 4
Submit an article Journal homepage
368
Views
3
CrossRef citations to date
0
Altmetric
ORGINAL Article

GZD2202, a novel TrkB inhibitor, suppresses BDNF-mediated proliferation and metastasis in neuroblastoma models

Jian ZouSchool of Pharmacy, Jinan University, Guangzhou, China; View further author information
,
Zhang ZhangInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, Guangzhou, China; ;Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou, China; Correspondence[email protected]
View further author information
,
Fang XuInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, Guangzhou, China; ;Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou, China; View further author information
,
Shengyang CuiUniversity of Chinese Academy of Sciences, Beijing, China; ;Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China; View further author information
,
Chunli QiInsititute of Laboratory Animal Science, Jinan University, Guangzhou, ChinaView further author information
,
Jinfeng LuoGuangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China; View further author information
,
Zhen WangUniversity of Chinese Academy of Sciences, Beijing, China; ;Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China; View further author information
,
Xiaoyun LuInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, Guangzhou, China; ;Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou, China; View further author information
,
Zhengchao TuSchool of Pharmacy, Jinan University, Guangzhou, China; ;Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China; View further author information
,
Xiaomei RenInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, Guangzhou, China; ;Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou, China; View further author information
,
Liyan SongSchool of Pharmacy, Jinan University, Guangzhou, China; Correspondence[email protected]
View further author information
&
Ke DingInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, Guangzhou, China; ;Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou, China; Correspondence[email protected]
ORCID Iconhttp://orcid.org/0000-0001-9016-812XView further author information
ORCID Icon show all
Pages 442-450 | Received 23 Apr 2018, Accepted 05 Oct 2018, Published online: 30 Oct 2018
 
Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days

Abstract

Collective data suggest tropomyosin-related kinase B (TrkB), which is correlated with the growth, migration and poor prognosis of neuroblastoma (NB), is a potential target for NB target therapy. Several Phase I/II pan-Trk inhibitors display impressive clinical outcomes but still no drug has been approved for general use. In this paper, we report a novel structural TrkB inhibitor GZD2202, a structural derivative of our previously identified DDR1 antagonists. GZD2202 demonstrates a moderate selectivity between Trk B/C and TrkA. GZD2202 suppresses the brain-derived neurotrophic factor (BDNF) -mediated TrkB signalling pathway, proliferation, migration and invasion in SH-SY5Y-TrkB neuroblastoma cells, and causes about 36.1% growth inhibition in a SH-SY5Y-TrkB neuroblastoma xenograft model.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study was funded by National Natural Science Foundation of China (21572230, 81673285 and 81425021), Guangdong Province (2014TQ01R341, 2015A030306042, 2015A030312014, 2016A050502041 and Nanyue-Baijie Award), Guangzhou City (201805010007) and Jinan University.

Log in via your institution

Access through your institution

Log in to Taylor & Francis Online

Restore content access

Restore content access for purchases made as guest
Purchase options * Save for later

PDF download + Online access

  • 48 hours access to article PDF & online version
  • Article PDF can be downloaded
  • Article PDF can be printed
USD 65.00 Add to cart

Issue Purchase

  • 30 days online access to complete issue
  • Article PDFs can be downloaded
  • Article PDFs can be printed
USD 767.00 Add to cart

* Local tax will be added as applicable

Related Research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.