Potent transglutaminase inhibitors, aryl beta-aminoethyl ketones.

Bioorg Med Chem Lett

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

Published: February 2010

AI Article Synopsis

  • Aryl beta-aminoethyl ketones are effective blockers of tissue transglutaminase.
  • Thiophene groups and N-benzyl N-t-butyl aminoethyl structures enhance their inhibitory power.
  • These findings could pave the way for new treatments targeting tissue transglutaminase-related conditions.

Article 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.

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Source
http://dx.doi.org/10.1016/j.bmcl.2009.12.011DOI Listing

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