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The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptors

✍ Scribed by David C. Horwell; Andrew I. Morrell; Edward Roberts


Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
112 KB
Volume
6
Category
Article
ISSN
0960-894X

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✦ Synopsis


2,4-disubstituted morpholin-3-one based ligands which show affinity for tachykinin receptors have been designed and synthesised. Variation of the side chains attached to the central template gives rise to selectivity between receptor subtypes. This selectivity is directly analogous to that exhibited by dipcptide ligands for the same receptor subtypes.


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## Abstract Bifunctional affinity ligands based on a triazine scaffold were rationally designed to target prion protein and shown to bind recombinant prion protein with high affinity and selectivity. The ligands were capable of discriminating between prion protein glycoforms and monomeric and dimer