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Structural comparison between type I and type II antagonists: possible implications in the drug design of AT1
P Roumelioti1, T Tselios, K Alexopoulos
1Department of Chemistry, University of Patras, Greece.
Abstract:
Analogues of sarilesin (type I AT1 antagonists), and sarmesin (type II AT1 antagonists) with homoserine (hSer) at position 8 were prepared and bioassayed. The presence of a Tyr4-Ile5-His6 bend found in sarmesin but not in sarilesin was identified. The obtained results coupled with conformational analysis studies, using a combination of NMR spectroscopy and computational chemistry, propose important conformational and stereoelectronic properties for agonist and antagonist activity at AT1 receptors.
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