The Mass Spectrometry society of Japan - The 68th Annual Conference on Mass Spectrometry, Japan

Abstract

Oral Sessions

Day 3, May 13(Wed.) 9:45-10:05 Room A (Main Hall)

Identification of Target Binder by Affinity Selection Mass Spectrometry

(Mitsubishi Tanabe Pharm.)
oTomoya Akashi, Akiko Iihara, Yuuki Watanabe

High-throughput screening (HTS) is a starting point for the drug development and necessary for the selection of the lead compound which is a prototype of drug. Due to the depletion of target molecules and the potential exists for a false positive and false negative data in enzymatic analysis, the traditional binding assay technologies “Affinity Selection Mass Spectrometry (AS-MS)” are being attracted as HTS. AS-MS technique is based on biophysical technology that pool compounds are incubated with the target of interest, binder-target complex and non-binder are separated by ultrafiltration and finally the binder is identified via LC/MS analysis. This technology can evaluate candidate compounds more rapidly than other biophysical analysis. Moreover, it monitors direct compound-target interaction in label-free, that enables to get not only inhibitor but also binder for the target and assess non-enzymatic target (e.g. membrane protein, transcriptional factor, nucleotide). AS-MS requires the development of the accurate analytical method for the detection of binders from compound library. In this presentation, the exploratory study and some case of AS-MS experienced in our company will be introduced.