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Superimposition of potent non-peptide AT1receptor antagonists with angiotensin II

✍ Scribed by Efthimia Theodoropoulou; Thomas Mavromoustakos; Dimitris Panagiotopoulos; John M. Matsoukas; Julian Smith

Publisher: Springer Netherlands
Year: 1996
Tongue: English
Weight: 542 KB
Volume: 3
Category: Article
ISSN: 1573-3149
DOI: 10.1007/bf00128109

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✦ Synopsis

The model of angiotensin II (ANG II) developed in our laboratory using a combination of NMR, fluorescence data and molecular graphics [Matsoukas, J.M. et al., J. Biol. Chem., 269 (1994) 5303] served as a template for a systematic superimposition of potent AT~ receptor antagonists with ANG II. The key amino acids in this model, tyrosine, phenylalanine and histidine, form a charge-relay system. The studied ANG II AT~ receptor antagonists were found to accommodate this relay system. The proposed model offers a motivation to synthetic chemists to develop ANG II antagonists that differ from the losartan prototype structure but possess an enhanced biological profile.

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