title: [Inhibitory effect of CXCR4 blockers on a CXCR4-expressing gastric cancer cell line in nude mice].
abstract: OBJECTIVE
  CXCR4, one of the chemokine receptors, plays a major role in cell migration in metastasis and cancer dissemination. However, it is not known whether CXCR4 is associated with tumor growth in vivo. In the present study, we investigated the inhibitory effect of CXCR4 blockers on CXCR4-expressing gastric cancer in vivo.
  
  
  METHODS
  Cells of a CXCR4-expressing gastric cancer cell line, K-MK-2, were transplanted into nude mice. A CXCR4 blocker, AMD3100 (2 mg/kg), was injected and another blocker, KRH3955 (1 mg/kg or 10 mg/kg), was administered orally. Both drugs were administered for 5 days followed by 2 days of rest. The mice were sacrificed on the 35th day following transplantation and the weights of the tumors were measured.
  
  
  RESULTS
  The mean weights of the tumors were 7.092±1.221 g in the control mice, 5.137±1.001 g in the ADM3100-injected mice, 3.895±2.120 g in mice treated with 1 mg/kg of KRH3955, and 4.257±1.169 g in mice treated with 10 mg/kg of KRH3955. The 2 CXCR4 blockers significantly inhibited the growth of gastric cancer cells transplanted into the nude mice.
  
  
  CONCLUSIONS
  The CXCR4 blockers AMD3100 and KRH3955 inhibit tumor growth in vivo. These drugs are possible candidates for personalized therapy of gastric cancer.
authors.affiliation: Dept. of Surgery, Tokyo Metropolitan Cancer and Infectious Diseases Center, Japan.
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Iwanaga
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Iwasaki
authors.forename: Manabu
authors.initials: M
authors.lastname: Ohashi
authors.forename: Ryoki
authors.initials: R
authors.lastname: Ohinata
authors.forename: Keiichi
authors.initials: K
authors.lastname: Takahashi
authors.forename: Tatsuro
authors.initials: T
authors.lastname: Yamaguchi
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Matsumoto
authors.forename: Daisuke
authors.initials: D
authors.lastname: Nakano
mesh_terms: D000818:Animals; D001596:Benzylamines / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D000080027:Cyclams; D006571:Heterocyclic Compounds / Q000627:therapeutic use*; D007093:Imidazoles / Q000627:therapeutic use*; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors*; D013274:Stomach Neoplasms / Q000188:drug therapy*; D023041:Xenograft Model Antitumor Assays
chemical_list: D001596:Benzylamines; D000080027:Cyclams; D006571:Heterocyclic Compounds; D007093:Imidazoles; C541387:N,N-dipropyl-N'-(4-((((1H-imidazol-2-yl)methyl)((1-methyl-1H-imidazol-2-yl) methyl)amino)methyl)benzyl)-N'-methylbutane-1,4-diamine; D019718:Receptors, CXCR4; C088327:plerixafor