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Cited by 279Receptor Mechanisms and SignalingPhosphodiesterase function and regulationProtein Kinase Regulation and GTPase Signaling

The DOI matches its Crossref record; 54 of the 55 references it cites were found in a registry or an index.

Forskolin as a Tool for Examining Adenylyl Cyclase Expression, Regulation, and G Protein Signaling

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Insel, Paul A., Ostrom, Rennolds S.·2003·Cellular and Molecular Neurobiology
DOI 10.1023/a:1023684503883PMC PMC11530207
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Abstract

1. As initially shown by Seamon and Daly, the diterpene forskolin directly activates adenylyl cyclase (AC) and raises cyclic AMP levels in a wide variety of cell types. In this review, we discuss several aspects of forskolin action that are often unappreciated. These include the utility of labeled forskolin as a means to quantitate the number of AC molecules; results of those types of studies, coupled with efforts to increase AC expression, document that such expression stoichiometrically limits cyclic AMP formation by hormones and neurotransmitters. 2. Response to forskolin is also strongly influenced by the activation of AC by the heterotrimeric G-protein, Gs. Gs-promoted enhancement of AC activity in response to forskolin occurs not only when cells are incubated with exogenously administered agonists that activate G-protein-coupled receptors but also by agonists that can be endogenously released by cells. 3. Such agonists, which include ATP and prostaglandins, serve as autocrine/paracrine regulators of cellular levels of cyclic AMP under "basal" conditions and also in response to forskolin and to agonists that promote release of such regulators. 4. The ability of forskolin to prominently activate cyclic AMP generation has proved valuable for understanding stoichiometry of the multiple components involved in "basal" cyclic AMP formation, in enzymologic studies of AC as well as in defining responses to cyclic AMP in cells within and outside the nervous system.

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  1. Green, D. A., and Clark, R. B. (1982bs). Direct evidence for the role of the coupling proteins in forskolin activation of adenylate cyclase. J. Cyclic Nucleotide Res. 8:337–346.

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Metadata

Authors
Insel, P. A., & Ostrom, R. S.
Affiliations
University of California San Diego (US)
Corresponding author
Insel, Paul A.
ORCID
Venue
Cellular and Molecular Neurobiology
Publisher
Springer Science and Business Media LLC
Published
2003-06
Volume
23
Issue
3
Pages
305-314
ISSN
  • 0272-4340 (ISSN-L)
  • 1573-6830
DOI
10.1023/a:1023684503883
PMC
PMC11530207
OpenAlex
W1517339234
Cited by
277
References
55
Citations by year
2026: 11 · 2025: 12 · 2024: 12 · 2023: 8 · 2022: 8 · 2021: 20 · 2020: 13 · 2019: 9 · 2018: 14 · 2017: 6 · 2016: 17 · 2015: 8 · 2014: 16 · 2013: 14 · 2012: 15
FWCI
0.73
Type
journal article
Language
en
Open access
Licence
Locations
  • Cellular and Molecular Neurobiology (publishedVersion)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Phosphodiesterase function and regulation
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Keywords
forskolin, adenylate cyclase, cyclic AMP, Gs protein, G protein signaling, autocrine and paracrine regulation, ATP, prostaglandins, G protein-coupled receptors, enzyme activity assay
MeSH terms
Cyclic AMP, Adenosine Triphosphate, Adenylyl Cyclases, Animals, Cell Membrane, Eukaryotic Cells, Colforsin, Humans, Signal Transduction, Gene Expression Regulation, Enzymologic, GTP-Binding Proteins

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