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10.18632/oncotarget.15601

http://scihub22266oqcxt.onion/10.18632/oncotarget.15601
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suck abstract from ncbi


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pmid28445950
      Oncotarget 2017 ; 8 (15 ): 24635-24643
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  • The discovery of a novel compound with potent antitumor activity: virtual screening, synthesis, biological evaluation and preliminary mechanism study #MMPMID28445950
  • Jin Y ; Li L ; Yang Z ; Liu M ; Guo H ; Shen W
  • Oncotarget 2017[Apr]; 8 (15 ): 24635-24643 PMID28445950 show ga
  • Farnesyltransferase has been regarded as a promising drug target against cancer as it is critical for membrane association of several signal transduction proteins. In this study, a novel farnesyltransferase inhibitor (IMB-1406) was identified through virtual screening. It exhibits stronger potency (IC50s: 6.92-8.99 ?M) than Sunitinib against all of the tested cancer cell lines. Preliminary studies on mechanism reveal that IMB-1406 induces apoptosis in HepG2 cells by arresting the cell cycle at the S phase, altering anti- and pro-apoptotic proteins leading to mitochondrial dysfunction and activation of caspase-3. This anti-tumor effect is most probably related to the inhibition of farnesyltransferase as indicated by molecular docking. Overall, IMB-1406 is a novel lead compound with potent antitumor activity and deserves further structural modifications.
  • |Antineoplastic Agents/*pharmacology [MESH]
  • |Cell Line, Tumor [MESH]
  • |Drug Screening Assays, Antitumor/*methods [MESH]
  • |Humans [MESH]
  • |Molecular Structure [MESH]


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