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Updated: Jun 24, 2026
09:39
Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
Published on: January 27, 2014
Capturing adenylyl cyclases as potential drug targets.
Sandra Pierre1, Thomas Eschenhagen, Gerd Geisslinger
1Pharmazentrum Frankfurt, ZAFES, Institut für Klinische Pharmakologie, Klinikum der Goethe-Universität Frankfurt, Theodor-Stern-Kai 7, 60590 Frankfurt, Germany.
Nature Reviews. Drug Discovery
|April 2, 2009
Summary
Adenylyl cyclases (ACs) generate cyclic AMP (cAMP), a key signaling molecule. Targeting specific AC isoforms with novel drugs shows promise for treating conditions like neuropathic pain and heart failure.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Cyclic AMP (cAMP) is a crucial intracellular messenger.
- Nine membrane-bound and one soluble adenylyl cyclase (AC) isoforms generate cAMP in mammals.
- ACs are not typically targeted directly by drugs, despite their importance.
Purpose of the Study:
- To explore the therapeutic potential of targeting specific adenylyl cyclase (AC) isoforms.
- To review advances in developing isoform-selective AC inhibitors and activators.
- To discuss the clinical applications of AC-targeting compounds.
Main Methods:
- Review of physiological functions of mammalian AC isoforms.
- Analysis of recent developments in isoform-selective AC modulator research.
- Discussion of therapeutic strategies involving AC targeting.
Main Results:
- ACs play diverse physiological roles.
- Development of isoform-selective AC inhibitors and activators has advanced significantly.
- Targeting ACs offers potential therapeutic benefits across various diseases.
Conclusions:
- Adenylyl cyclases represent promising drug targets.
- Isoform-selective AC modulators could be valuable therapeutics.
- Potential applications include neuropathic pain, neurodegenerative diseases, heart failure, asthma, and male contraception.
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Major types that are helpful drug targets include:
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01:26Targets for Drug Action: Overview
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