Topographical mimetics

Type III Topographical mimetics Structure-based design Non-peptide protease inhibitors... 

Type III mimetics represent the Farmer definition ofpeptidomimetics in that they possess novel templates, which appear unrelated to the original peptides but contain the essential groups, positioned on a novel non-peptide scaffold to serve as topographical mimetics. Several type III peptidomimetic protease inhibitors have been characterized where direct... 

A more recent example of the use of vector maps to evaluate conformational similarity is an applicationto /3-turn mimetics by Ballet al. (434,435). This led to a recognition that many of the various turn types described in peptides based on their backbone dihedral angles lead to quite similar topographical arrangements of the side chains. A new parameter, ]8 [the dihedral angle formed by the backbone atoms C(i)-o C(2)-aC(35-Nf4)], was described (Fig. 3.42) that more readily facilitated comparison of the topography of the system. 

Figure 2.9. Conversion of (2jS,3i2)TMT -c[DPDPE] into a nonpeptide peptide mimetic based on topographical considerations.

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