The DOI matches its Crossref record; 27 of the 27 references it cites were found in a registry or an index.
Structural Instability of a Constitutively Active G Protein-coupled Receptor
Open accessAbstract
Mutations in several domains can lead to agonist-independent, constitutive activation of G protein-coupled receptors. However, the nature of the structural and molecular changes that constitutively turn on a G protein-coupled receptor remains unknown. Here we show evidence that a constitutively activated mutant of the beta2 adrenergic receptor (CAM) is characterized by structural instability and an exaggerated conformational response to ligand binding. The structural instability of CAM could be demonstrated by a 4-fold increase in the rate of denaturation of purified receptor at 37 degrees C as compared with the wild type receptor. Spectroscopic analysis of purified CAM labeled with the conformationally sensitive and cysteine-reactive fluorophore, N,N'dimethyl-N-(iodoacetyl)-N'-(7-nitrobenz-2-oxa-1, 3-diazol-4-yl)ethylenediamine, further indicated that both agonist and antagonist elicit more profound structural changes in CAM than in the wild type protein. We propose that the mutation that confers constitutive activity to the beta2 adrenergic receptor removes some stabilizing conformational constraints, allowing CAM to more readily undergo transitions between the inactive and the active states and making the receptor more susceptible to denaturation.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
Ballesteros, J. A., & Weinstein, H. (1995) · Methods in Neurosciences · doi:10.1016/s1043-9471(05)80049-7 · Cited by 2,999
Self-citationSamama, P., Cotecchia, S., Costa, T., & Lefkowitz, R. J. (1993) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)53442-6 · Cited by 1,257
Somatic mutations in the thyrotropin receptor gene cause hyperfunctioning thyroid adenomas
Parma, J., Duprez, L., Sande, J. V., Cochaux, P., Gervy, C., Mockel, J., Dumont, J., & Vassart, G. (1993) · Nature · doi:10.1038/365649a0 · Cited by 918
ROBBINS, L. (1993) · Cell · doi:10.1016/0092-8674(93)90572-8 · Cited by 876
Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
Lefkowitz, R. J., Cotecchia, S., Samama, P., & Costa, T. (1993) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(93)90048-o · Cited by 792
Shenker, A., Laue, L., Kosugi, S., Merendino, J. J., Minegishi, T., & Cutler, G. B. (1993) · Nature · doi:10.1038/365652a0 · Cited by 745
Costa, T., & Herz, A. (1989) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.86.19.7321 · Cited by 536
Constitutively active mutants of rhodopsin
Robinson, P. R., Cohen, G. B., Zhukovsky, E. A., & Oprian, D. D. (1992) · Neuron · doi:10.1016/0896-6273(92)90034-b · Cited by 512
The two-state model of receptor activation
Leff, P. (1995) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(00)88989-0 · Cited by 488
Bond, R. A., Leff, P., Johnson, T. D., Milano, C. A., Rockman, H. A., McMinn, T. R., Apparsundaram, S., Hyek, M. F., Kenakin, T. P., Allen, L. F., et al. (1995) · Nature · doi:10.1038/374272a0 · Cited by 416
Cited by
The Molecular Basis of G Protein–Coupled Receptor Activation
Weis, W. I., & Kobilka, B. K. (2018) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-060614-033910 · Cited by 1,227
Self-citationBiased Signaling Pathways in β 2 -Adrenergic Receptor Characterized by 19 F-NMR
Liu, J. J., Horst, R., Katritch, V., Stevens, R. C., & Wüthrich, K. (2012) · Science · doi:10.1126/science.1215802 · Cited by 697
Gether, U., & Kobilka, B. K. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.29.17979 · Cited by 578
Self-citationMorello, J.-P., Salahpour, A., Laperrière, A., Bernier, V., Arthus, M.-F., Lonergan, M., Petäjä-Repo, U., Angers, S., Morin, D., Bichet, D. G., et al. (2000) · Journal of Clinical Investigation · doi:10.1172/jci8688 · Cited by 565
Action of Molecular Switches in GPCRs - Theoretical and Experimental Studies
Trzaskowski, B., Latek, D., Yuan, S., Ghoshdastider, U., Debinski, A., & Filipek, S. (2012) · Current Medicinal Chemistry · doi:10.2174/092986712799320556 · Cited by 469
Metadata
- Authors
- Gether, U., Seifert, R., Ballesteros, J. A., Sanders-Bush, E., Weinstein, H., & Kobilka, B. K.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 1997-01
- Volume
- 272
- Issue
- 5
- Pages
- 2587-2590
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W2116599708
- Cited by
- 295
- References
- 27
- FWCI
- 9.34
- Type
- journal article
- Language
- en
- Open access
- hybrid
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: Structural Instability of a Constitutively Active G Protein-coupled Receptor. https://app.cochat.ai/papers/10.1074/jbc.272.5.2587
- The paper
- Gether, U., Seifert, R., Ballesteros, J. A., Sanders-Bush, E., Weinstein, H., & Kobilka, B. K. (1997). Structural Instability of a Constitutively Active G Protein-coupled Receptor. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.272.5.2587
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
