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SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2012 Oct 04; Vol. 3 (12), pp. 1024-8. Date of Electronic Publication: 2012 Oct 04 (Print Publication: 2012). - Publication Year :
- 2012
-
Abstract
- We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and better physical and calculated properties. Transglutaminase selectivity profiling and in vitro ADME properties of selected compounds are also reported.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 3
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24900424
- Full Text :
- https://doi.org/10.1021/ml300241m