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conformationally constrained histidines in the design of peptidomimetics strategies for the χ-space control构象上限制组氨酸在peptidomimeticsχ-space控制策略的设计
Int. J. Mol. Sci. 2011, 12, 2853-2890; doi:10.3390/ijms OPEN ACCESS International Journal of Molecular Sciences ISSN 1422-0067 /journal/ijms Review Conformationally Constrained Histidines in the Design of Peptidomimetics: Strategies for the χ-Space Control 1 1 1 1 Azzurra Stefanucci , Francesco Pinnen , Federica Feliciani , Ivana Cacciatore , Gino Lucente 2 and Adriano Mollica 1,* 1 Department of Pharmaceutical Sciences, University of Chieti-Pescara “G. d’Annunzio”, Via dei Vestini 31, 66100 Chieti, Italy 2 Institute of Biomolecular Chemistry (CNR), c/o Department of Chemistry and Pharmaceutical Technologies, “Sapienza”, University of Rome, P.le A. Moro, 00185 Rome, Italy * Author to whom correspondence should be addressed; E-Mail: a.mollica@unich.it; Tel.: +39-0871-355-4482; Fax: +39-0871-355-4477. Received: 31 March 2011; in revisedform: 18 April 2011 / Accepted: 20 April 2011 / Published: 3 May 2011 Abstract: A successful design of peptidomimetics must come to terms with χ-space control. The incorporation of χ-space constrained amino acids into bioactive peptides renders the χ1 and χ2 torsional angles of pharmacophore amino acids critical for activity and selectivity as with other relevant structural features of the template. This review describes histidine analogues characte
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