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

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CCK(2) receptor antagonists containing the conformationally constrained phenylalanine derivatives, including the new amino acid Xic.

The conformationally constrained analogues of phenylalanine, tetrahydroisoquinoline-3-carboxylic acid (Tic), Sic, Hic and Nic, and the new amino acid Xic have been incorporated into a potent and highly selective cholecystokinin-2 (CCK(2)) receptor antagonist (2) in place of the phenylalanine residue, producing compounds 15a-e. High selectivities for CCK(2) over CCK(1) were observed for compounds 15a-e. The in vitro profile of the analogue containing the Nic residue (15d) was identical to that of compound 2, whereas the alternative conformational constraints resulted in a significant loss of affinity. The apparent advantage of Nic in the context of these CCK(2) ligands was subsequently demonstrated to be statistically significant.[1]

References

  1. CCK(2) receptor antagonists containing the conformationally constrained phenylalanine derivatives, including the new amino acid Xic. Gibson, S.E., Guillo, N., Jones, J.O., Buck, I.M., Kalindjian, S.B., Roberts, S., Tozer, M.J. European journal of medicinal chemistry. (2002) [Pubmed]
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