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Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity.

Publication ,  Journal Article
Kobilka, BK; Kobilka, TS; Daniel, K; Regan, JW; Caron, MG; Lefkowitz, RJ
Published in: Science
June 3, 1988

The alpha 2 and beta 2 adrenergic receptors, both of which are activated by epinephrine, but which can be differentiated by selective drugs, have opposite effects (inhibitory and stimulatory) on the adenylyl cyclase system. The two receptors are homologous with each other, rhodopsin, and other receptors coupled to guanine nucleotide regulatory proteins and they contain seven hydrophobic domains, which may represent transmembrane spanning segments. The function of specific structural domains of these receptors was determined after construction and expression of a series of chimeric alpha 2-,beta 2-adrenergic receptor genes. The specificity for coupling to the stimulatory guanine nucleotide regulatory protein lies within a region extending from the amino terminus of the fifth hydrophobic domain to the carboxyl terminus of the sixth. Major determinants of alpha 2- and beta 2-adrenergic receptor agonist and antagonist ligand binding specificity are contained within the seventh membrane spanning domain. Chimeric receptors should prove useful for elucidating the structural basis of receptor function.

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Published In

Science

DOI

ISSN

0036-8075

Publication Date

June 3, 1988

Volume

240

Issue

4857

Start / End Page

1310 / 1316

Location

United States

Related Subject Headings

  • Yohimbine
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic, alpha
  • Protein Conformation
  • Pindolol
  • Molecular Sequence Data
  • Humans
  • General Science & Technology
  • GTP-Binding Proteins
  • Cloning, Molecular
 

Citation

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Kobilka, B. K., Kobilka, T. S., Daniel, K., Regan, J. W., Caron, M. G., & Lefkowitz, R. J. (1988). Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity. Science, 240(4857), 1310–1316. https://doi.org/10.1126/science.2836950
Kobilka, B. K., T. S. Kobilka, K. Daniel, J. W. Regan, M. G. Caron, and R. J. Lefkowitz. “Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity.Science 240, no. 4857 (June 3, 1988): 1310–16. https://doi.org/10.1126/science.2836950.
Kobilka BK, Kobilka TS, Daniel K, Regan JW, Caron MG, Lefkowitz RJ. Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity. Science. 1988 Jun 3;240(4857):1310–6.
Kobilka, B. K., et al. “Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity.Science, vol. 240, no. 4857, June 1988, pp. 1310–16. Pubmed, doi:10.1126/science.2836950.
Kobilka BK, Kobilka TS, Daniel K, Regan JW, Caron MG, Lefkowitz RJ. Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity. Science. 1988 Jun 3;240(4857):1310–1316.
Journal cover image

Published In

Science

DOI

ISSN

0036-8075

Publication Date

June 3, 1988

Volume

240

Issue

4857

Start / End Page

1310 / 1316

Location

United States

Related Subject Headings

  • Yohimbine
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic, alpha
  • Protein Conformation
  • Pindolol
  • Molecular Sequence Data
  • Humans
  • General Science & Technology
  • GTP-Binding Proteins
  • Cloning, Molecular