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Related Concept Videos

GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
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GTPases and their Regulation02:14

GTPases and their Regulation

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Guanine nucleotide-binding proteins (G-proteins), also known as GTPases, are a superfamily of proteins that regulate many cellular processes, such as cell signaling, vesicular transport, and the regulation of cell shape and motility. Mutation or dysfunction of these proteins can lead to disease. There are around 40,000 known G-proteins that can broadly be classified into two groups ‒  small G-proteins consisting of a single domain and large multi-domain G-proteins.
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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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Small GTPases - Ras and Rho01:24

Small GTPases - Ras and Rho

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Ras and Rho are small monomeric GTPases that act downstream of receptor tyrosine kinase (RTK) and regulate various cellular processes. These GTPases switch between active and inactive states by binding to guanine nucleotides.
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Related Experiment Video

Updated: Oct 18, 2025

Mapping the Cellular Distribution of an Optogenetic Protein Using a Light-Stimulation Grid
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Mapping the Cellular Distribution of an Optogenetic Protein Using a Light-Stimulation Grid

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Soluble GC stimulators and activators: Past, present and future.

Peter Sandner1,2, Markus Follmann1, Eva Becker-Pelster1

  • 1Pharmaceuticals Research & Development, Bayer AG, Wuppertal, Germany.

British Journal of Pharmacology
|October 2, 2021
PubMed
Summary

Soluble guanylate cyclase (sGC) stimulators and activators offer new ways to treat cardiovascular diseases. These drugs, like riociguat and vericiguat, target NO-sGC signaling for improved patient outcomes.

Keywords:
NOcGMPriociguatruncaciguatsGC activatorssGC stimulatorssoluble GC (sGC)vericiguat

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Measurement of Cyclic Guanosine Monophosphate (cGMP) in Solid Tissues using Competitive Enzyme-Linked Immunosorbent Assay (ELISA)
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Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
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Last Updated: Oct 18, 2025

Mapping the Cellular Distribution of an Optogenetic Protein Using a Light-Stimulation Grid
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Measurement of Cyclic Guanosine Monophosphate (cGMP) in Solid Tissues using Competitive Enzyme-Linked Immunosorbent Assay (ELISA)
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Measurement of Cyclic Guanosine Monophosphate (cGMP) in Solid Tissues using Competitive Enzyme-Linked Immunosorbent Assay (ELISA)

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Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
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Area of Science:

  • Pharmacology
  • Cardiovascular Medicine
  • Biochemistry

Background:

  • Soluble guanylate cyclase (sGC) is a key enzyme in nitric oxide (NO) signaling.
  • sGC modulators offer therapeutic potential for cardiovascular and other diseases.
  • First-generation sGC modulators have paved the way for advanced drug development.

Purpose of the Study:

  • To review the discovery and development of sGC stimulators and activators.
  • To elucidate the unique mechanisms of action for sGC modulators.
  • To summarize preclinical and clinical findings of sGC-targeted therapies.

Main Methods:

  • Literature review of sGC stimulator and activator research.
  • Analysis of pharmacological properties and clinical trial data.
  • Comparison of different generations of sGC modulators.

Main Results:

  • sGC stimulators (e.g., riociguat, vericiguat) enhance sGC activity with or without NO.
  • sGC activators target the oxidized, heme-free form of sGC.
  • Newer activators like runcaciguat show promise in clinical trials for conditions like CKD and DR.

Conclusions:

  • sGC modulators represent a significant advancement in cardiovascular pharmacotherapy.
  • The distinct mechanisms of stimulators and activators offer versatile therapeutic strategies.
  • Further exploration of sGC agonists is expected to yield novel treatments for diverse indications.