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  • 1
    Electronic Resource
    Electronic Resource
    Structural comparison of NK2 receptor agonists and antagonists (1994)
    Springer
    Journal of computer aided molecular design 8 (1994), S. 341-344 
    Details
    ISSN: 1573-4951
    Keywords: Tachykinins ; NK2 ; MEN-10627 ; Binding ; Agonist ; Antagonist
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary The conformational space of two NK2 receptor agonists and a new potent antagonist has been sampled by the simulated annealing technique. Low-energy conformers were obtained, which were compared with respect to their key residues, namely phenylalanine, leucine and methionine. The hypothesis is that they share part of the binding site on the receptor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00126750
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  • 2
    Electronic Resource
    Electronic Resource
    Conformational rigidity versus flexibility in a novel peptidic neurokinin A receptor antagonist (1995)
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Peptide Science 1 (1995), S. 236-240 
    Details
    ISSN: 1075-2617
    Keywords: Tachykinins ; NK-2 antagonist ; cyclic peptide ; conformation ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Neurokinin A receptor antagonists have been proposed as a new class of drugs for several applications in humans (asthama, 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. MEN 10627 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.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/psc.310010404
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