Structure-activity relationships of neuropeptide Y (NPY)

Neuropeptide Y (NPY) is a 36-peptide amide, which inter alia plays a central role in blood pressure regulation. Highly active, potential lead structures for the development of drugs were shortened and cyclised analogues of NPY. Y₁ and Y₂-receptor binding assays and biological assays with the synthetic NPY analogues were carried out. Spectroscopic conformational investigations (CD, 2D-NMR) and molecular dynamics simulation supported the SAR studies.

Molecular dynamics simulation of neuropeptide Y (model for Y₂-receptor affinity)

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M. C. Michel, W. Gaida, A G. Beck-Sickinger, H. A Wieland, H. Doods, H. Dürr, G.
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A G. Beck-Sickinger, E. Hoffmann, K Paulini, H.-D. Reisig, K-D. Willim, and G.
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A. G. Beck–Sickinger, H.A Wieland, H. Wittneben, K-D. Willim, K Rudolf, and G.
Jung (1994). Complete L-Alanine Scan of Neuropeptide Y Reveals Ligands Binding to Y₁ and Y₂ Receptors with Distinguished Conformations, Eur. J. Biochem. 225,947-958.

L.J.M. Cross, A. G. Beck-Sickinger, M. Bienert, W. Gaida, G. Jung, E. Krause, and M.
Ennis (1996). Structure Activity Studies of Mast Cell Activation and Hypotension Induced by Neuropeptide Y (NPY), Centrally Truncated and C-terminal NPY Analogues, Brit. J. Pharmacol. 117, 325-332.