Amino-aromatic interaction between histidine 197 of the neurokinin-1 receptor and CP 96345

Article Abstract:

The neurokinin-1 receptor (NK-1R) is a G-protein-coupled receptor which interacts with substance P and is involved in the mediation paintransmission and neurogenic inflammation. Site-specific mutaganesis was conducted to determine the relevant amino acid residues in NK-1R responsible for binding to CP 96345, a non-peptide antagonist. The results showed that His-197 on the fifth transmembrane helix of NK-1R specifically interacts with CP 96345. Comparisons of the binding affinities of various CP 96345 analogs showed that the histidine residue interacts with the benzhydryl moiety of CP 96345.

Analysis, Tachykinins, Neurotransmitter receptors

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A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists

Article Abstract:

L365260 and L364718 are non-peptide antagonists for cholecystokinin-B/gastrin (CCK-B/gastrin) receptor. These antagonists bind withdifferent affinities to human and canine CCK-B/gastrin receptors, with L365260 and L364718 showing higher affinities for human and canine receptors, respectively. Site-specifice mutagenesis showed that the branched chain aliphatic amino acid at position 319 is responsible for the selective affinities of the antagonists. However, these residues were not important for agonist binding.

Hormone antagonists, Gastrin, cholecystokinin

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Heterodimerization of the Drosophila ecdysone receptor with retinoid X receptor and ultraspiracle

Article Abstract:

An investigation was conducted to determine the cause of Hela cell-specific ecdysone transactivation. Gel shift analysis detected a complex in transfected Hela cells. Further analysis showed that the ecdysone receptor heterodimerizes with either with the retinoid X receptor or its Drosophila homologue, ultraspiracle, to promote DNA binding and transactivation. Therefore, the regulation of EcR activity may involve the replacement of the heterodimer partner as well as partner selection by the hormone.

DNA binding proteins, Ecdysone

Similar abstracts:

• Abstracts: Conversion of antagonist-binding site to metal-ion site in the tachykinin NK-1 receptor. Different binding epitopes on the NK1 receptor for substance P and a non-peptide antagonist

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