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Identification and sequence of a binding site peptide of the beta 2-adrenergic receptor.

Publication ,  Journal Article
Dohlman, HG; Caron, MG; Strader, CD; Amlaiky, N; Lefkowitz, RJ
Published in: Biochemistry
March 22, 1988

p-(Bromoacetamido)benzyl-1-[125I]iodocarazolol (125I-pBABC) is a potent derivative of the beta-adrenergic receptor antagonist p-aminobenzylcarazolol. Treatment of the receptor with 125I-pBABC results in efficient covalent incorporation of the ligand into the receptor binding site. Extensive degradation of 125I-pBABC-labeled beta 2-adrenergic receptor with either cyanogen bromide or Staphylococcus aureus V8 protease results in specifically labeled fragments having Mr's of about 1600 and 3500, respectively. Because the primary structure of the beta 2-adrenergic receptor is known, and these proteolytic reagents are highly sequence specific, the site of 125I-pBABC incorporation may be deduced from the sizes of the specifically labeled fragments. Thus the fragment generated by cyanogen bromide cleavage corresponds to residues 83-96, a region of 14 amino acids included in the second membrane spanning domain (helix II) of the beta 2-adrenergic receptor. This assignment was confirmed by direct amino acid sequencing of this labeled fragment, though the actual amino acid modified could not be determined. These data permit the assignment of a part of the hormone binding region of the beta 2-adrenergic receptor.

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Published In

Biochemistry

DOI

ISSN

0006-2960

Publication Date

March 22, 1988

Volume

27

Issue

6

Start / End Page

1813 / 1817

Location

United States

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Protein Conformation
  • Propanolamines
  • Peptide Fragments
  • Molecular Weight
  • Molecular Sequence Data
  • Lung
  • Cricetinae
  • Cell Membrane
  • Biochemistry & Molecular Biology
 

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Dohlman, H. G., Caron, M. G., Strader, C. D., Amlaiky, N., & Lefkowitz, R. J. (1988). Identification and sequence of a binding site peptide of the beta 2-adrenergic receptor. Biochemistry, 27(6), 1813–1817. https://doi.org/10.1021/bi00406a002
Dohlman, H. G., M. G. Caron, C. D. Strader, N. Amlaiky, and R. J. Lefkowitz. “Identification and sequence of a binding site peptide of the beta 2-adrenergic receptor.Biochemistry 27, no. 6 (March 22, 1988): 1813–17. https://doi.org/10.1021/bi00406a002.
Dohlman HG, Caron MG, Strader CD, Amlaiky N, Lefkowitz RJ. Identification and sequence of a binding site peptide of the beta 2-adrenergic receptor. Biochemistry. 1988 Mar 22;27(6):1813–7.
Dohlman, H. G., et al. “Identification and sequence of a binding site peptide of the beta 2-adrenergic receptor.Biochemistry, vol. 27, no. 6, Mar. 1988, pp. 1813–17. Pubmed, doi:10.1021/bi00406a002.
Dohlman HG, Caron MG, Strader CD, Amlaiky N, Lefkowitz RJ. Identification and sequence of a binding site peptide of the beta 2-adrenergic receptor. Biochemistry. 1988 Mar 22;27(6):1813–1817.
Journal cover image

Published In

Biochemistry

DOI

ISSN

0006-2960

Publication Date

March 22, 1988

Volume

27

Issue

6

Start / End Page

1813 / 1817

Location

United States

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Protein Conformation
  • Propanolamines
  • Peptide Fragments
  • Molecular Weight
  • Molecular Sequence Data
  • Lung
  • Cricetinae
  • Cell Membrane
  • Biochemistry & Molecular Biology