Specific recognition of SP or NKB receptors by analogues of SP substituted at positions 8 and 9

Lavielle, Solange; Chassaing, Gérard; Julien, Sylviane; Marquet, Andrée; Bergström, Lena; Beaujouan, Jean‐Claude; Torrens, Y.; Głowiński, J.

doi:10.1016/0014-2999(86)90804-6

Cited by 27 publications

(17 citation statements)

References 3 publications

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“…Therefore, the lack or the lower effect of these two antagonists in the modulation of ACh release provided the first observation suggesting that new NK 1 ‐sensitive receptors might be involved in the responses evoked by SR140333, SSR240600 and GR205171. The inhibitory responses of these three antagonists are specifically mediated by NK 1 receptors because their effect is reversed by a selective agonist of tachykinin NK 1 receptor, [Pro 9 ]SP (Lavielle et al . 1986; Petitet et al .…”

Section: Discussionmentioning

confidence: 99%

The new neurokinin 1‐sensitive receptor mediates the facilitation by endogenous tachykinins of the NMDA‐evoked release of acetylcholine after suppression of dopaminergic transmission in the matrix of the rat striatum

Kemel

Pérez

Beaujouan

et al. 2003

Journal of Neurochemistry

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Using an in vitro microsuperfusion procedure, the NMDAevoked release of [ 3 H]ACh was studied after suppression of dopamine (DA) transmission (a-methyl-p-tyrosine) in striatal compartments of the rat. ]substance P but also by neurokinin A and neuropeptide K (1 nM each). According to the rank order of potency of agonists for counteracting the antagonist responses ([Pro 9 ]substance P, 0.013 nM > neurokinin A, 0.15 nM ? substance P(6-11) 7.7 nM ¼ septide 8.7 nM), the new NK 1 -sensitive receptors mediate the facilitation by endogenous tachykinins of the NMDA-evoked release of ACh in the matrix, after suppression of DA transmission. Solely the NK 1 antagonists having a high affinity for these receptors could be used as indirect anti-cholinergic agents.

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Section: Discussionmentioning

confidence: 99%

The new neurokinin 1‐sensitive receptor mediates the facilitation by endogenous tachykinins of the NMDA‐evoked release of acetylcholine after suppression of dopaminergic transmission in the matrix of the rat striatum

Kemel

Pérez

Beaujouan

et al. 2003

Journal of Neurochemistry

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Section: Discussionmentioning

confidence: 99%

“…The photosensitive probe used in the present investigation is slightly different incorporating (a) a proline residue in place of Gly9 (this constraint led to a selective NK-1 agonist [29] removal of the biotinylated fragments from the complex incuba-NK-1 receptor. However, analysis of the tryptic fragments of the tion mixture with streptavidin-coated beads and subsequent photolabelled human receptor suggested that in our study MALDI-TOF mass spectrometry analysis after direct desorption Met174 and not Met181 had been covalently linked to the from the beads with the MALDI-TOF matrix, facilitated by satu-benzophenone moiety.…”

Section: Discussionmentioning

confidence: 99%

The Use of Photolabelled Peptides to Localize the Substance‐P‐Binding Site in the Human Neurokinin‐1 Tachykinin Receptor

Girault¹,

Sagan²,

Bolbach³

et al. 1996

European Journal of Biochemistry

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104

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The amino acid p-benzoyl-L-phenylalanine, @-Bz)Phe, has been incorporated into substance P (SP), Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2, to localize the agonist-binding domains of the human neurokinin-1 (NK-1) receptor overexpressed in a transfected mammalian cell line. The NK-1 -specific agonist [Pro9]SP was modified at position 8 by @-Bz)Phe and acylated at the N-terminus by a biotinyl sulfone reporter via a 5-aminopentanoyl spacer. After photolysis, the biotinyl sulfone moiety allowed easy and efficient removal of biotinyiated fragments from the complex incubation mixture with streptavidin-coated beads. Direct elution from the beads with the matrix used for matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOFMS), which was facilitated by saturation of streptavidin sites with biotin, and subsequent MALDI-TOF mass spectrometry analysis allowed identification of the NK-1 fragments obtained after photolysis and proteolytic digestion. Trypsin digestion and combined trypsinlstaphylococcus aureus V8 protease enzymatic cleavage established that the site of covalent attachment of the photolabelled SP resides in the second extracellular loop, Thr173 -Arg177. Cyanogen bromide cleavage shows that the probe is covalently attached to the methyl group of a methionine residue from human NK-1. These experiments identified Met174 as the modified residue.Keywords: tachykinin receptor; photolabelling ; substance P; Chinese hamster ovary cells ; mass spectrometry.Chimeric tachykinin NK-UNK-3 or NK-UNK-2 receptors and mutated neurokinin-1 (NK-1) receptors have been constructed to probe the binding domains of NK-1 agonists and antagonists [ 1 -151. Both extracellular domains (N-terminal residues and extracellular loops) and residues from the transmembrane segments [I, 3, 5, 7, 8, 12, 13, 151 have been identified as important determinants for the binding of substance P and specific NK-1 agonists. However, as is evident from the conflicting data, these results do not imply that these critical residues of the NK-1 receptor directly interact with the amino acids of substance P; these residues may only confer the proper folding to the binding site for the agonist in the protein [13, 151. Affinity labelling of the receptor using photoreactive ligands constitutes a complementary strategy to mutagenesis [16]. The use of photolabelled analogues of the ligand-incorporating reactive probes in various positions allows mapping of the agonistbinding site. Theoretically, this strategy seems more precise than mutagenesis for the determination of the amino acids that constitute the binding pocket in the protein. However, numerous photolabelling experiments should be performed to describe the foot-printing of the ligand bound to its receptor. It should be noted that (a) important residues of the ligand cannot usually be modified (loss of the binding potency); the residue that is easily replaced by a photoreactive probe may not contribute to the binding contacts with the protein; and (b) when a compromis...

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“…route in guinea-pigs. The agonists used were septide ([pGlu6,, Wormser et al, 1986), [Sar9,Met(02)"]SP (Regoli et al, 1988) and [ProlSP (Lavielle et al, 1986) for the NKI tachykinin receptor, [Lys5, MeLeu9, Nle'INKA(4-10) (Chassaing et al, 1991) for the NK2 tachykinin receptor and senktide (succinyl-[Asp6,MePhe8]SP(6 -1), Laufer et al, 1986) for the NK3 tachykinin receptor. It has been demonstrated in mice that behavioural responses induced by intrathecal or i.c.v.…”

Section: Introductionmentioning

confidence: 99%

Comparative behavioural profile of centrally administered tachykinin NK₁, NK₂ and NK₃ receptor agonists in the guinea‐pig

Piot

Betschart

Grall

et al. 1995

British J Pharmacology

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Specific recognition of SP or NKB receptors by analogues of SP substituted at positions 8 and 9

Cited by 27 publications

References 3 publications

The new neurokinin 1‐sensitive receptor mediates the facilitation by endogenous tachykinins of the NMDA‐evoked release of acetylcholine after suppression of dopaminergic transmission in the matrix of the rat striatum

The new neurokinin 1‐sensitive receptor mediates the facilitation by endogenous tachykinins of the NMDA‐evoked release of acetylcholine after suppression of dopaminergic transmission in the matrix of the rat striatum

The Use of Photolabelled Peptides to Localize the Substance‐P‐Binding Site in the Human Neurokinin‐1 Tachykinin Receptor

Comparative behavioural profile of centrally administered tachykinin NK₁, NK₂ and NK₃ receptor agonists in the guinea‐pig

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Specific recognition of SP or NKB receptors by analogues of SP substituted at positions 8 and 9

Cited by 27 publications

References 3 publications

The new neurokinin 1‐sensitive receptor mediates the facilitation by endogenous tachykinins of the NMDA‐evoked release of acetylcholine after suppression of dopaminergic transmission in the matrix of the rat striatum

The new neurokinin 1‐sensitive receptor mediates the facilitation by endogenous tachykinins of the NMDA‐evoked release of acetylcholine after suppression of dopaminergic transmission in the matrix of the rat striatum

The Use of Photolabelled Peptides to Localize the Substance‐P‐Binding Site in the Human Neurokinin‐1 Tachykinin Receptor

Comparative behavioural profile of centrally administered tachykinin NK1, NK2 and NK3 receptor agonists in the guinea‐pig

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Comparative behavioural profile of centrally administered tachykinin NK₁, NK₂ and NK₃ receptor agonists in the guinea‐pig