<i>N</i>‐Methyl Scanning Mutagenesis Generates Protease‐Resistant G Protein Ligands with Improved Affinity and Selectivity

Abstract

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.