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  • vitro
  • In vitro, MLN2238 inhibited 20S proteasome activity, preferentially binding the 20S 5 site with an IC 50 of 3.4 nM and demonstrated potent activity against cultured cancer cells in cell viability assays. (aacrjournals.org)
  • ovarian cancer
  • In the present study we have explored the sensitivity of ovarian cancer cells to TRAIL and proteasome inhibitors. (ovid.com)
  • Particularly, we have explored the capacity of proteasome inhibitors to bypass TRAIL resistance of ovarian cancer cells. (ovid.com)
  • Importantly, studies on primary ovarian cancer cells have shown that these cells are completely resistant to TRAIL and proteasome inhibitors markedly enhance the sensitivity of these cells to TRAIL. (ovid.com)
  • Given the high susceptibility of ovarian cancer cells to proteasome inhibitors, our results further support the experimental use of these compounds in the treatment of ovarian cancer. (ovid.com)
  • boronic acid
  • To assess the effects of proteasome inhibition on chemotherapy response, human colorectal cancer cells were pretreated with the dipeptide boronic acid analogue PS-341 (1 μ m ) prior to exposure to SN-38, the active metabolite of the topoisomerase I inhibitor, CPT-11. (aacrjournals.org)
  • Evidence
  • 10 Evidence from the animal model indicates a potential role for proteasome inhibitors in the treatment of graft-versus-host disease. (bloodjournal.org)
  • In a study published in the May 1, 2001, issue of Clinical Cancer Research , Sunwoo and colleagues provided evidence for proteasome inhibition of NF-κB and tumorigenesis, supporting early-phase clinical trials in solid malignancies of the upper aerodigestive tract. (aacrjournals.org)
  • This trial revealed transient tumor regression or stable disease in a subset of patients, and despite being unable to administer doses tolerated by patients with multiple myeloma, provided evidence of proteasome inhibition along with altered expression of NF-κB target genes in evaluable tumor biopsies. (aacrjournals.org)
  • approaches
  • Previous preclinical work demonstrating a role for NF-κB in the initiation and progression of head and neck squamous cell carcinomas (HNSCC), a group of highly inflammatory and aggressive malignancies of the upper aerodigestive tract, provided a rationale for investigating different approaches to proteasome inhibition in this disease. (aacrjournals.org)