PMID- 23469688
OWN - NLM
STAT- MEDLINE
DCOM- 20130408
LR  - 20130308
IS  - 0031-7144 (Print)
IS  - 0031-7144 (Linking)
VI  - 68
IP  - 2
DP  - 2013 Feb
TI  - 8-(Tosylamino)quinoline inhibits tumour progression through targeting 
      phosphoinositide-3-kinase/Akt pathway.
PG  - 146-52
AB  - We examined whether 8-(tosylamino)quinoline (8-TQ), a structural analogue of BAY 
      11-7082, is able to modulate various tumourigenic responses using various in 
      vitro and in vivo experimental conditions. 8-TQ exhibited the strongest 
      suppressive activity on the proliferation of C6, A431, HeLa and MDA-MB-231 cells 
      with IC550 values ranging from 10 to 30 microM. According to the analysis of 
      level of active caspase-3, and morphologies of C6, HeLa and MDA-MB-231 cells, it 
      was revealed that 8-TQ is able to induce apoptosis. Furthermore, this compound 
      strongly diminished the invasion of MDA-MB-231 cells, the migration of HeLa 
      cells, and the new generation of blood vessels under non-toxic conditions. 
      Reduction of the phospho-form levels of intracellular signalling enzymes by 8-TQ 
      strongly indicated that molecular signalling machineries composed of 
      phosphoinositide 3-kinase (PI3K)/phosphoinositide-dependent kinase-1 (PDK1)/Akt 
      and extracellular-signal-regulated kinase (ERK) could be targeted by 8-TQ 
      treatment. Indeed, the specific inhibitors (LY294002 and U0126) of PI3K/PDK1/Akt 
      and ERK showed similar anti-cancer properties to 8-TQ. Finally, 8-TQ 
      intraperitoneally injected suppressed the increase of tumour volume up to 40% 
      compared to vehicle-treated control. Taken together, our results clearly suggest 
      that 8-TQ might have applications as a novel anti-cancer drug or may be served as 
      a lead compound to be further optimized.
FAU - Jung, Yongwoo
AU  - Jung Y
AD  - Department of Genetic Engineering, Sungkyunkwan University, Suwon, Republic of 
      Korea.
FAU - Yi, Young-Su
AU  - Yi YS
FAU - Yoo, Dae Sung
AU  - Yoo DS
FAU - Kim, Ji Hye
AU  - Kim JH
FAU - Yang, Woo Seok
AU  - Yang WS
FAU - Lee, Jongsung
AU  - Lee J
FAU - Park, Kye Won
AU  - Park KW
FAU - Kweon, Dae-Hyuk
AU  - Kweon DH
FAU - Hong, Sungyoul
AU  - Hong S
FAU - Cho, Jae Youl
AU  - Cho JY
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Germany
TA  - Pharmazie
JT  - Die Pharmazie
JID - 9800766
RN  - 0 (8-(tosylamino)quinoline)
RN  - 0 (Angiogenesis Inhibitors)
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Quinolines)
RN  - 0 (Tosyl Compounds)
RN  - EC 2.7.1.- (Phosphatidylinositol 3-Kinases)
RN  - EC 2.7.11.1 (Oncogene Protein v-akt)
RN  - EC 3.4.24.24 (Matrix Metalloproteinase 2)
RN  - EC 3.4.24.35 (Matrix Metalloproteinase 9)
SB  - IM
MH  - Angiogenesis Inhibitors/therapeutic use
MH  - Animals
MH  - Antineoplastic Agents/*pharmacology
MH  - Blotting, Western
MH  - Cell Line, Tumor
MH  - Cell Movement/drug effects
MH  - Cell Proliferation/drug effects
MH  - Chorioallantoic Membrane/drug effects
MH  - Disease Progression
MH  - Humans
MH  - Immunoprecipitation
MH  - Male
MH  - Matrix Metalloproteinase 2/metabolism
MH  - Matrix Metalloproteinase 9/metabolism
MH  - Mice
MH  - Mice, Inbred C57BL
MH  - Microscopy, Confocal
MH  - Neoplasm Invasiveness
MH  - Neovascularization, Pathologic/drug therapy
MH  - Oncogene Protein v-akt/*physiology
MH  - Phosphatidylinositol 3-Kinases/*physiology
MH  - Quinolines/*pharmacology
MH  - Tosyl Compounds/*pharmacology
MH  - Wound Healing/drug effects
EDAT- 2013/03/09 06:00
MHDA- 2013/04/09 06:00
CRDT- 2013/03/09 06:00
PHST- 2013/03/09 06:00 [entrez]
PHST- 2013/03/09 06:00 [pubmed]
PHST- 2013/04/09 06:00 [medline]
PST - ppublish
SO  - Pharmazie. 2013 Feb;68(2):146-52.