title: RGD-modified angiogenesis inhibitor HM-3 dose: dual function during cancer treatment.
abstract: In the present study, we have undertaken pharmacodynamic studies of HM-3 in vitro and in vivo. A dual function of HM-3 with various doses was observed. HM-3 at low dose revealed obvious anticancer activity. In contrast, HM-3 at high dose had a tendency to promote tumorigenesis and tumor metastasis. Microarray analysis demonstrated that HM-3 at high dose could up-regulate the transcription of AKT1 and MEK1, which resulted in the promotion of tumorigenesis and metastasis. Therefore, the dose of angiogenesis inhibitors plays a critical role in cancer treatment. In order to achieve the ideal effect of angiogenesis inhibitor drugs on cancer treatment, a ful exploration of administration dose, frequency, and period for this kind of drugs is highly desired.
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, PR China. xuhanmei@cpu.edu.cn
authors.forename: Hanmei
authors.initials: H
authors.lastname: Xu
authors.forename: Li
authors.initials: L
authors.lastname: Pan
authors.forename: Yinling
authors.initials: Y
authors.lastname: Ren
authors.forename: Yongjing
authors.initials: Y
authors.lastname: Yang
authors.forename: Xiaofeng
authors.initials: X
authors.lastname: Huang
authors.forename: Zhendong
authors.initials: Z
authors.lastname: Liu
mesh_terms: D020533:Angiogenesis Inhibitors / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D002460:Cell Line; D002465:Cell Movement / Q000187:drug effects; D005260:Female; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D008810:Mice, Inbred C57BL; D008819:Mice, Nude; D019950:Mitogen-Activated Protein Kinase 1 / Q000235:genetics; D048052:Mitogen-Activated Protein Kinase 3 / Q000235:genetics; D009369:Neoplasms / Q000098:blood supply* / Q000188:drug therapy* / Q000473:pathology; D009842:Oligopeptides / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D009924:Organ Culture Techniques; D010455:Peptides / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D051057:Proto-Oncogene Proteins c-akt / Q000235:genetics
chemical_list: D020533:Angiogenesis Inhibitors; D009842:Oligopeptides; D010455:Peptides; C047981:arginyl-glycyl-aspartic acid; D051057:Proto-Oncogene Proteins c-akt; D019950:Mitogen-Activated Protein Kinase 1; D048052:Mitogen-Activated Protein Kinase 3