Evaluation of Zone-4 Inhibitors Using Sphingosine Kinase Activity Assay
Poster Number
54
College
College of Arts and Sciences
Department
Chemistry, Physics, Geology, & the Environment
Faculty Mentor
Christian Grattan, Ph.D.
Abstract
Sphingosine kinase 1 is an enzyme that catalyzes the phosphorylation of sphingosine to form sphingosine-1-phosphate, which is known to induce cell proliferation. Research indicates that there is an overexpression of sphingosine kinase 1 in cancer cells that leads to accelerated cell growth of cancer cells. An inhibitor, Sphingosine kinase Inhibitor 1 (SKI-1) has been found to inhibit sphingosine kinase 1 in vitro, while failing to be effective in vivo. Modifications to the structure of the inhibitor yielded derivatives that may or may not exhibit inhibitory effect in vivo. Using a Sphingosine Kinase Activity Assay kit, fifteen derivatives were synthesized and tested. Two derivatives, 4A and 4B, were found to have some inhibitory effect, with luminescence values of 38,617 and 32,776, respectively. These values are higher than the average luminescence value of 13,328 that corresponds to a reaction without any inhibitor.
Course Assignment
CHEM 551, 552 – Hanna
Start Date
21-4-2017 2:15 PM
Evaluation of Zone-4 Inhibitors Using Sphingosine Kinase Activity Assay
Richardson Ballroom
Sphingosine kinase 1 is an enzyme that catalyzes the phosphorylation of sphingosine to form sphingosine-1-phosphate, which is known to induce cell proliferation. Research indicates that there is an overexpression of sphingosine kinase 1 in cancer cells that leads to accelerated cell growth of cancer cells. An inhibitor, Sphingosine kinase Inhibitor 1 (SKI-1) has been found to inhibit sphingosine kinase 1 in vitro, while failing to be effective in vivo. Modifications to the structure of the inhibitor yielded derivatives that may or may not exhibit inhibitory effect in vivo. Using a Sphingosine Kinase Activity Assay kit, fifteen derivatives were synthesized and tested. Two derivatives, 4A and 4B, were found to have some inhibitory effect, with luminescence values of 38,617 and 32,776, respectively. These values are higher than the average luminescence value of 13,328 that corresponds to a reaction without any inhibitor.
