Conversion of antagonist-binding site to metal-ion site in the tachykinin NK-1 receptor

Article Abstract:

Analysis of the antagonist-binding site in human tachykinin NK-1 receptor indicates that the presence of histidine residues results in transforming this binding site to a metal-ion-binding site of good affinity. This change in the nature of the binding site enables a detailed study of helical interactions in receptors coupled with G-proteins. The conformational variations arising due to this transformation in the mutants are stabilized by Zn2+, which functions as an 'allosteric competitive' antagonist.

Research, Binding sites (Biochemistry), Active sites (Biochemistry), Histidine, Tachykinins

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Different binding epitopes on the NK1 receptor for substance P and a non-peptide antagonist

Article Abstract:

CP 96345 is a non-peptide antagonist for substance P which binds to the NK1 receptor. An investigation was conducted to determine the binding epitopes on NK1 which is responsible for CP 96345 binding. The results showed that two epitopes at the top of transmembrane segment V and one epitope at the top of transmembrane segment VI are required for CP 96345 binding. Unexpectedly, these epitopes are not important for substance P binding.

Identification and classification, Cell receptors, Antigenic determinants, Substance P

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A new cytokine-receptor binding mode revealed by the crystal structure of the IL-1 receptor with an antagonist

Article Abstract:

The crystal structure at 2.7 A resolution of the soluble extracellular part of type-I IL1R complexed with IL1RA was described. The receptor consists of three domains that are immunoglobulin-like. An area called the receptor trigger site which is essential for biological function in IL-1beta is not directly in contact with the receptor in the IL1RA complex. Studies have shown that this trigger site could induce domain 3 movement.

Cytokines

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