Potent transglutaminase inhibitors, aryl beta-aminoethyl ketones

Shoichiro Ozaki; Etsuko Ebisui; Kozo Hamada; Jun-Ichi Goto; Akinobu Z Suzuki; Akiko Terauchi; Katsuhiko Mikoshiba

doi:10.1016/j.bmcl.2009.12.011

Potent transglutaminase inhibitors, aryl beta-aminoethyl ketones

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1141-4. doi: 10.1016/j.bmcl.2009.12.011. Epub 2009 Dec 22.

Authors

Shoichiro Ozaki¹, Etsuko Ebisui, Kozo Hamada, Jun-Ichi Goto, Akinobu Z Suzuki, Akiko Terauchi, Katsuhiko Mikoshiba

Affiliation

¹ Laboratory for Developmental Neurobiology, Brain Science Institute, Institute of Physical and Chemical Research (RIKEN), 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.

PMID: 20053561
DOI: 10.1016/j.bmcl.2009.12.011

Abstract

Aryl beta-aminoethyl ketones were discovered as potent inhibitors of tissue transglutaminase. Heteroaryl-like thiophene groups and N-benzyl N-t-butyl aminoethyl group are critical to the strong inhibitory activity of aryl beta-aminoethyl ketones.

Publication types

Comparative Study

MeSH terms

Animals
Guinea Pigs
Ketones / chemistry*
Ketones / metabolism
Ketones / pharmacology
Liver / drug effects
Liver / enzymology
Transglutaminases / antagonists & inhibitors*
Transglutaminases / metabolism

Substances

Ketones
Transglutaminases