Open Access. Powered by Scholars. Published by Universities.®
Pharmacy and Pharmaceutical Sciences Commons™
Open Access. Powered by Scholars. Published by Universities.®
Articles 1 - 1 of 1
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
Discovery And Mechanistic Study Of Novel Pbd-Targeted Inhibitors Of Plk1 For Prostate Cancer Treatment, Danda Pani Chapagai
Discovery And Mechanistic Study Of Novel Pbd-Targeted Inhibitors Of Plk1 For Prostate Cancer Treatment, Danda Pani Chapagai
Theses and Dissertations
Polo-like kinase 1 (PLK1) is a central player in regulating entry into and progression through mitosis. Inhibition of sub-cellular localization and kinase activity of PLK1 through the Polo-box domain (PBD) is emerging as a viable alternative to ATP binding site directed drugs for which the development of resistant mutants and inhibition of closely related members of the PLK family (tumor suppressor roles) are primary concerns. I describe related novel non-peptidic PBD binding inhibitors, termed abbapolins, identified through successful application of the REPLACE strategy and demonstrate their potent antiproliferative activity in prostate tumors and other cell lines. Furthermore, the abbapolins show …