Application of photoaffinity crosslinking in determining the interaction between calcitonin and its receptor

Vi Pham, John D. Wade, Patrick M. Sexton

Research output: Contribution to journalArticleResearchpeer-review

Abstract

Understanding the molecular mechanism underlying how the peptide ligands bind to their receptors with subsequent receptor activation and cellular response is of great long-term value in designing receptor-targeted drugs. This is more difficult for class-II G protein-coupled receptors as only minimal structural data is available and their natural peptide ligands contain a large and diffuse pharmacophore. To address this problem, photoaffinity labeling studies have been developed to identify the spatial proximity between the photophore-modified ligand and its receptor. This minireview looks at the application of this approach in determining the proximal sites between class-II G protein-coupled receptor peptide ligands and their corresponding receptors, including parathyroid hormone, secretin and vasoactive intestinal polypeptide. More specifically, we will highlight interaction sites between positions 19, 16 and 26 of calcitonin with C 134 -K 141 , and F 137 and T 30 of the receptor, respectively.

Original languageEnglish
Pages (from-to)447-453
Number of pages7
JournalLetters in Peptide Science
Volume10
Issue number5-6
DOIs
Publication statusPublished - 1 Nov 2003
Externally publishedYes

Keywords

  • Calcitonin
  • Calcitonin receptor
  • Class II G protein-coupled receptor
  • Ligand-receptor interaction
  • Photoaffinity cross-linking

Cite this

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abstract = "Understanding the molecular mechanism underlying how the peptide ligands bind to their receptors with subsequent receptor activation and cellular response is of great long-term value in designing receptor-targeted drugs. This is more difficult for class-II G protein-coupled receptors as only minimal structural data is available and their natural peptide ligands contain a large and diffuse pharmacophore. To address this problem, photoaffinity labeling studies have been developed to identify the spatial proximity between the photophore-modified ligand and its receptor. This minireview looks at the application of this approach in determining the proximal sites between class-II G protein-coupled receptor peptide ligands and their corresponding receptors, including parathyroid hormone, secretin and vasoactive intestinal polypeptide. More specifically, we will highlight interaction sites between positions 19, 16 and 26 of calcitonin with C 134 -K 141 , and F 137 and T 30 of the receptor, respectively.",
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Application of photoaffinity crosslinking in determining the interaction between calcitonin and its receptor. / Pham, Vi; Wade, John D.; Sexton, Patrick M.

In: Letters in Peptide Science, Vol. 10, No. 5-6, 01.11.2003, p. 447-453.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Pham, Vi

AU - Wade, John D.

AU - Sexton, Patrick M.

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