A novel blood glucose–lowering compound

September 15, 2017

Silkworms help researchers identify and analyze a new drug candidate

Collaborative research between RIKEN CSRS, Gunma University and the National Agriculture and Food Research Organization (NARO) has led to the identification of a compound that lowers blood glucose.

The researchers began the work by focusing on GPBA, a type of G protein–coupled receptor (GPCR) involved in the stimulation of insulin secretion. In order to consistently produce the large amounts of GPBA needed for their work, they constructed a transgenic silkworm with a human GPBA genes and developed a screening system to allow them to identify a particular compound that would activate GPBA by using GPBA overexpressing transgenic silkworm cell membranes. The system was applied to 10,625 chemical compounds in the RIKEN Natural Compound Depository (NPDepo) and returned one compound. This compound was confirmed to induce lower blood glucose level using a mice glucose tolerance test.

This compound is expected to support research on the stimulation of insulin secretion and the development of anti-diabetes drugs.

Original article
European Journal of Pharmacology doi:10.1016/j.ejphar.2017.08.017
R. Enomoto, A. Kurosawa, Y. Nikaido, M. Mashiko, T. Saheki, N. Nakajima, S. Kuroiwa, M. Otobe, M. Ohsaki, K. Tooyama, Y. Inoue, N. Kuwabara, O. Kikuchi, T. Kitamura, I. Kojima, Y. Nakagawa, T. Saito, H. Osada, M. Futahashi, H. Sezutsu, S. Takeda,
"A novel partial agonist of GPB A reduces blood glucose level in a murine glucose tolerance test".
European Journal of Pharmacology doi:10.1016/j.ejphar.2015.10.025
Y. Nikaido, A. Kurosawa, H. Saikawa, S. Kuroiwa, C. Suzuki, N. Kuwabara, H. Hoshino, H. Obata, S. Saito, T. Saito, H. Osada, I. Kobayashi, H. Sezutsu, S. Takeda,
"In vivo and in vitro evaluation of novel μ-opioid receptor a gonist compounds".
Hiroyuki Osada
Group Director
Chemical Resource Development Research Unit, RIKEN CSRS
Shigeki Takeda
Faculty of Science and Technology Division of Molecular Science, Gunma University