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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 …
Function Of Gpr68 In Normal Hematopoiesis And Malignant Hematopoietic Diseases, Xiaofei He
Function Of Gpr68 In Normal Hematopoiesis And Malignant Hematopoietic Diseases, Xiaofei He
Theses and Dissertations
G protein-coupled receptor 68 (GPR68), as a proton-sensing receptor, is involved in numerous physiological processes. However, its specific functions in normal hematopoiesis and malignant hematopoietic diseases were unknown. Using a genetic loss of function approach (i.e. whole-body Gpr68-/- mouse model), B lymphocytes were reduced under stressed conditions, such as aging and hematopoietic regeneration. However, hematopoietic stem cells (HSC) from Gpr68-/- mice exhibited comparable function as HSC from wild type mice either under steady-state or upon stress. To determine whether the unaltered HSC function of Gpr68-/- mice was due to compensatory effects of Gpr68 in nonhematopoietic cells, a …