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

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Apr 21st, 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.