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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Conformational rigidity versus flexibility in a novel peptidic neurokinin A receptor antagonist.

Neurokinin A receptor antagonists have been proposed as a new class of drugs for several applications in humans (asthma, intestinal motility, etc.). The rational design, synthesis, structural characterization and biological activity evaluation of a new potent, highly selective, long-lasting, peptide-based receptor antagonist are reported. The structure-activity relationship indicates that the conformational rigidity determines potency, specificity and especially the long life of the molecule in the living body. MEN10627 is the prototype of a new class of cyclic, peptide-based, neurokinin A receptor antagonists and it is a suitable candidate for clinical testing in humans.[1]

References

  1. Conformational rigidity versus flexibility in a novel peptidic neurokinin A receptor antagonist. Pavone, V., Lombardi, A., Maggi, C.A., Quartara, L., Pedone, C. J. Pept. Sci. (1995) [Pubmed]
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