Investigating the Effects of BIBR1532 and Related Analogs on Telomerase Activity in Human Prostate Cancer Cells
Presentation Type
Poster/Portfolio
Presenter Major(s)
Cell and Molecular Biology
Mentor Information
Suganthi Sridhar
Department
Biomedical Sciences
Location
Henry Hall Atrium 60
Start Date
11-4-2012 9:00 AM
Keywords
Health, Life Science
Abstract
Unlimited cellular proliferation of cancer cells is coupled with the maintenance of telomeres in DNA. Telomerase, the enzyme that re-extends telomeres, has become an attractive target for new cancer therapeutics. BIBR1532, a mixed-type non-competitive inhibitor of telomerase, has been shown to cause growth arrest in tumor cells. Here, we tested BIBR1532 and two synthetic analogues (WS6-48, WS4-43A) for anti-proliferative activity on metastatic prostate cancer cells. Preliminary results indicate these compounds are highly active against proliferation. Their effects on inhibiting telomerase activity directly were quantified using a telomere repeat amplification protocol assay. Newly developed analogues are under preliminary testing to determine their effect upon telomerase. Available x-ray structures of telomerase domains are also being explored to asses ligand binding sites and affinities. Further studies will asses the effect these compounds have on other metastatic cancer cell lines.
Investigating the Effects of BIBR1532 and Related Analogs on Telomerase Activity in Human Prostate Cancer Cells
Henry Hall Atrium 60
Unlimited cellular proliferation of cancer cells is coupled with the maintenance of telomeres in DNA. Telomerase, the enzyme that re-extends telomeres, has become an attractive target for new cancer therapeutics. BIBR1532, a mixed-type non-competitive inhibitor of telomerase, has been shown to cause growth arrest in tumor cells. Here, we tested BIBR1532 and two synthetic analogues (WS6-48, WS4-43A) for anti-proliferative activity on metastatic prostate cancer cells. Preliminary results indicate these compounds are highly active against proliferation. Their effects on inhibiting telomerase activity directly were quantified using a telomere repeat amplification protocol assay. Newly developed analogues are under preliminary testing to determine their effect upon telomerase. Available x-ray structures of telomerase domains are also being explored to asses ligand binding sites and affinities. Further studies will asses the effect these compounds have on other metastatic cancer cell lines.