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N ‐Methyl Scanning Mutagenesis Generates Protease‐Resistant G Protein Ligands with Improved Affinity and Selectivity
Author(s) -
Fiacco Stephen V.,
Roberts Richard W.
Publication year - 2008
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200800208
Subject(s) - scissile bond , chemistry , protease , selectivity , stereochemistry , mutagenesis , alkaline protease , biochemistry , enzyme , mutation , gene , catalysis
Scanning for bioavailability : N ‐methyl incorporation does not have to be at the scissile bond to dramatically enhance protease resistance. N ‐methyl scanning around the scissile bond has yielded compounds that are also more selective and bind with higher affinity.