当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Analysis of C-terminally substituted tachykinin-like peptide agonists by means of aequorin-based luminescent assays for human and insect neurokinin receptors.

Analysis of C-terminally substituted tachykinin-like peptide agonists by means of aequorin-based luminescent assays for human and insect neurokinin receptors.

Abstract：

:Aequorin-based assays for stable fly, Stomoxys calcitrans, (STKR) and human (neurokinin receptor 1 (NK1), neurokinin receptor 2 (NK2)) neurokinin-like receptors were employed to investigate the impact of a C-terminal amino acid exchange in synthetic vertebrate ('FXGLMa') and invertebrate ('FX1GX2Ra') tachykinin-like peptides. C-terminally (Arg to Met) substituted analogs of the insect tachykinin-related peptide, Lom-TK I, displayed increased agonistic potencies in luminescent assays for human NK1 and NK2 receptors, whereas they showed reduced potencies in the STKR-assay. The opposite effects were observed when C-terminally (Met to Arg) substituted analogs of substance P were analysed. These substance P analogs proved to be very potent STKR-agonists, being more potent than Lom-TK I. On the other hand, Lom-TK-LMa, was shown to be a very potent NK1-agonist and was suggested to have more substance-P-mimetic than neurokinin-A-mimetic properties. NK1 and NK2 receptor agonists appeared to be more sensitive to changes at the penultimate amino acid position than STKR-agonists. This is also reflected in the sequence conservation that is observed in the naturally occurring tachykinin subgroups ('FXGLMa' vs. 'FX1GX2Ra'). The differential Arg-Met preference appears to be a major coevolutionary change between insect and human peptide-receptor couples. With regard to the peptide agonists, this change can theoretically be based on a single point mutation.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Torfs H,Detheux M,Oonk HB,Akerman KE,Poels J,Van Loy T,De Loof A,Vassart G,Parmentier M,Vanden Broeck J

doi

10.1016/s0006-2952(02)00914-0

subject

Has Abstract

pub_date

2002-05-01 00:00:00

pages

1675-82

issue

9

eissn

0006-2952

issn

1873-2968

pii

S0006295202009140

journal_volume

63

pub_type

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