Abstract
The concept of topographic design of peptide neurotransmitters and hormones was pioneered by Hruby (1,2). When the design involved primarily constraint of the side chains of a peptide that has a well-defined backbone conformation, the term “topographic design on a stable template” was proposed (3). The side chain χ1 of aromatic amino acids, such as Phe, Trp, Tyr, and His, can be constrained in either the gauche (−) or gauche (+) conformation by linking the nitrogen atom to the aromatic ring through a methylene bridge (Fig. 1).
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Tourwé, D., Iterbeke, K., Kazmierski, W.M., Tóth, G. (1999). Cyclic Aromatic Amino Acids with Constrained χ1 and χ2 Dihedral Angles. In: Kazmierski, W.M. (eds) Peptidomimetics Protocols. Methods in Molecular Medicine™, vol 23. Humana Press. https://doi.org/10.1385/0-89603-517-4:321
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DOI: https://doi.org/10.1385/0-89603-517-4:321
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