Chemical screening of an inhibitor for gibberellin receptors based on a yeast two-hybrid system

Jung-Min Yoon; Masatoshi Nakajima; Kiyoshi Mashiguchi; Seung-Hyun Park; Masato Otani; Tadao Asami

doi:10.1016/j.bmcl.2012.12.007

Chemical screening of an inhibitor for gibberellin receptors based on a yeast two-hybrid system

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1096-8. doi: 10.1016/j.bmcl.2012.12.007. Epub 2012 Dec 14.

Authors

Jung-Min Yoon¹, Masatoshi Nakajima, Kiyoshi Mashiguchi, Seung-Hyun Park, Masato Otani, Tadao Asami

Affiliation

¹ Department of Applied Biological Chemistry, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-8657, Japan.

PMID: 23298808
DOI: 10.1016/j.bmcl.2012.12.007

Abstract

We applied a yeast two-hybrid (Y2H) system to the high-throughput monitoring of two proteins' interaction, a receptor for phytohormone gibberellin (GA) and its direct signal transducer DELLA. With this system, we screened inhibitors to the interaction. As a result, we discovered a chemical, 3-(2-thienylsulfonyl)pyrazine-2-carbonitrile (TSPC), and we confirmed that TSPC is an inhibitor for GA perception by in vitro and in planta evaluations.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Gibberellins / antagonists & inhibitors*
Gibberellins / chemistry
Gibberellins / metabolism
High-Throughput Screening Assays
Plant Growth Regulators / antagonists & inhibitors
Plant Growth Regulators / chemistry
Plant Growth Regulators / metabolism
Plants, Genetically Modified
Receptors, Cell Surface / antagonists & inhibitors*
Receptors, Cell Surface / chemistry
Receptors, Cell Surface / metabolism
Signal Transduction
Two-Hybrid System Techniques

Substances

Gibberellins
Plant Growth Regulators
Receptors, Cell Surface