Thursday, January 17, 2013
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proteins with Pictet-Spengler ligations
could be useful for creating hydrolysis-resistant biologics. The
Pictet-Spengler ligation forms a hydrolysis-resistant carbon-carbon bond
between tryptamine and an aldehyde or ketone. In a protein hydrolysis assay,
more than 90% of a stabilized fluorescent protein produced by the
Pictet-Spengler ligation remained intact after two days, whereas less than
50% of a fluorescent protein produced using another chemical method remained
intact. The ligation reaction generated a HER2
antibody-drug conjugate that maintained its target affinity. Next steps could
include using the ligation reaction to create additional hydrolysis-resistant
variants of existing biologics.
Published online Jan. 17, 2013
Patent pending; licensing
details available from the University of California, Berkeley
Office of Technology Licensing
Agarwal, P. et al. Proc.
Natl. Acad. Sci. USA; published online
Dec. 13, 2012;
Contact: Carolyn R. Bertozzi, University of California,
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