GRAB-peptidomimetic

Recently, a fourth type of peptidomimetic called a GRAB-peptidomimetic (groupreplacement-assisted binding) has been identified (10). These structures might share structural-functional features of type I peptidomimetics, but they bind to an enzyme form not accessible with type I peptidomimetics. 

Recently, the importance of generating inhibitors that target receptor conformational ensembles has been pointed out (10). This method goes beyond the current docking of knovm structures to known active site con-formers and can lead to type III and GRAB peptidomimetics. 

The concept of Group Replacement Assisted Binding (GRAB) peptidomimetics derives from the discovery at Roche of the piperidine class of renin inhibitors. The non-... 

Figure 15.35. GRAB peptidomimetics in action. See color insert.

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