title: PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells.
abstract: Growth factor signalling pathways transduce extra-cellular physiological cues to guide cells to maintain critical cellular functions, including cell proliferation, survival and metabolism. Dysregulation of certain growth factor signalling pathways has been shown as a major route to promote tumourigenesis. Glioma is a type of aggressive malignant tumour with no effective systematic therapy so far. Overexpression or hyperactivation of IGF-1R has been observed to be tightly associated with glioma progression and poor prognosis. Here, we examined the biological effects of a specific IGF-1R inhibitor, PQ401, on suppressing U87MG glioma cell growth and migration. Specifically, we observed that PQ401 not only induced cellular apoptosis in U87MG cells and subsequently reduced cell viability and proliferation but also attenuated cell mobility in vitro. More importantly, through a mouse xenograft model, we observed that administration of PQ401 on mice led to suppression of glioma tumour growth in vivo. In summary, our study suggests that PQ401 may serve as a promising leading drug for treating glioma patients with elevated IGF-1R signalling.
authors.affiliation: a Department of Neurosurgery , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Zhou
authors.affiliation: a Department of Neurosurgery , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Xinli
authors.initials: X
authors.lastname: Zhao
authors.affiliation: a Department of Neurosurgery , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Xiangsheng
authors.initials: X
authors.lastname: Li
authors.affiliation: b Department of Pharmacy , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Guanfang
authors.initials: G
authors.lastname: Ping
authors.affiliation: b Department of Pharmacy , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Sujuan
authors.initials: S
authors.lastname: Pei
authors.affiliation: b Department of Pharmacy , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Ming
authors.initials: M
authors.lastname: Chen
authors.affiliation: a Department of Neurosurgery , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Zhongwei
authors.initials: Z
authors.lastname: Wang
authors.affiliation: a Department of Neurosurgery , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Wenke
authors.initials: W
authors.lastname: Zhou
authors.affiliation: a Department of Neurosurgery , First Affiliated Hospital of Xinxiang Medical College , Weihui , Henan , P. R. China.
authors.forename: Baozhe
authors.initials: B
authors.lastname: Jin
mesh_terms: D000634:Aminoquinolines / Q000494:pharmacology*; D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D001932:Brain Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology*; D002465:Cell Movement / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects*; D005434:Flow Cytometry; D005910:Glioma / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology*; D006801:Humans; D007124:Immunoenzyme Techniques; D008297:Male; D051379:Mice; D016688:Mice, Inbred NOD; D016513:Mice, SCID; D010671:Phenylurea Compounds / Q000494:pharmacology*; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors*; D014407:Tumor Cells, Cultured; D023041:Xenograft Model Antitumor Assays
chemical_list: D000634:Aminoquinolines; C569479:PQ 401; D010671:Phenylurea Compounds; D017526:Receptor, IGF Type 1
keywords: Glioma; IGF1-R; Migration; PQ401; Proliferation; U87MG