Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor.

Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor. Research Abstract Details 

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Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor. Abstract Text:

L J Miller,M Dong,K G Harikumar,F Gao,

The secretin receptor is prototypic of Class II GPCRs (G-protein-coupled receptors), based on its structural and functional characteristics and those of its natural agonist ligand. Secretin represents a linear 27-residue peptide with diffuse pharmacophoric domain. The secretin receptor includes the typical signature sequences for this receptor family within its predicted transmembrane segments and the highly conserved six cysteine residues contributing to three intradomain disulfide bonds within its long N-terminus. This domain is critical for secretin binding based on receptor mutagenesis and photoaffinity labelling studies. Full agonist analogues of secretin incorporating a photolabile moiety at various positions throughout the pharmacophore covalently label residues within this region, while only N-terminal probes have labelled the core helical bundle domain. Combining insights coming from receptor structural studies, peptide structure-activity relationship considerations, photoaffinity labelling, and application of fluorescence techniques has resulted in the development of a working model of the secretin-receptor complex. This supports the initial docking of the peptide agonist within a cleft in the receptor N-terminus, providing the opportunity for an endogenous sequence within that domain to interact with the core of the receptor. This interaction is believed to be key in the molecular basis of conformational change associated with activation of this receptor. The site of action of this endogenous agonist could also provide a possible target for small molecule agonists to act.

Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor. Publishing Authors By Initials

LJ Miller,M Dong,KG Harikumar,F Gao,

For similar hormones, hormone substitutes, and hormone antagonists: hormones: gastrointestinal hormones: secretin research abstracts see: hormones, hormone substitutes, and hormone antagonists: hormones: gastrointestinal hormones: secretin research

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Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor. Journal Published:

PUBLICATION TYPE: Review

Journal: Biochemical Society transactions

VOLUME: 35

Page Numbers: 709-12

Journal Abbreviation: Biochem. Soc. Trans.

ISSN: 0300-5127

DAY: 3

MONTH: Aug

YEAR: 2007

Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor. Information

Number of References: 23

LANGUAGE: eng

NlmUniqueID: 7506897

Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor. Keywords Mesh Terms:

KEYWORDS: Secretin

MESH TERMS: physiology

Chemical & Substance for Abstract: Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor. Information

Substance Name: Secretin

Registry Number: 1393-25-5

Grant and Affiliation Information for Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor.

AFFILIATION: Mayo Clinic, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA. miller@mayo.edu

Country: England

AGENCY: United States NIDDK

GRANT: DK46577

ACRONYM: DK

MEDLINETA: Biochem Soc Trans

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