7th Drug Chemistry Conference: Design, Synthesis, Production and Standardization of Drug Active Substances, Antalya, Türkiye, 14 - 17 Mart 2019, ss.18
Separase (EC 3.4.22.49) is a protease which cleaves the SSC1 subunit of the cohesin ring complex
releasing the tension of the spindle and allowing segregation of sister chromatids to opposite
centrosomal poles. Overexpression of Separase has been is defined as lagged chromosomes,
premature separation of chromatids and aneuploidy. Disrupt mitosis and cell cycle regulation can
result in aneuploidy and subsequently, cancer formation1,2
. ESPL1 (NM_012291.4) associated with the
development and progression of human breast cancer2
.
Gambogic acid isolated from Garcinia hanburyi tree, is known to can be induced to undergo apoptosis,
anti-angiogenesis and anti-metastatic. Due to these features, Gambogic acid has a potential to become
a cancer drug candidate3
.
My goal in the present research was to examine effects of the Gambogic acid on gene expression and
activity of Separase in human breast cancer MDA-MB-453 cells. It has been studied that the gene
expression level of ESPL1 with the human β-actin used as a reference to normalize data. Furthermore,
the activity of Separase in the Gambogic acid-applied cells by fluorogenic assay method using Rad21-
MCA peptide (Ac-Asp-Arg-Glu-Ile-Nle-Arg-MCA) as substrate.