Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Calmodulin-dependent Signaling01:16

Calmodulin-dependent Signaling

5.2K
Calmodulin (CaM) is a calcium-binding protein in eukaryotes that controls various calcium-regulated cellular processes. It has four calcium-binding sites that bind calcium to form the calcium-calmodulin ( Ca2+-CaM) complex. GPCR stimulation increases the calcium levels in the cells that bind to CaM and induces a conformational change.
The Ca2+-CaM complex does not have enzymatic activity by itself. Instead, the complex binds downstream target proteins, including membrane proteins or enzymes,...
5.2K
Global Regulatory Systems01:28

Global Regulatory Systems

62
Global regulatory systems in bacteria enable rapid and coordinated responses to environmental changes by integrating sensory inputs with gene expression, ensuring efficient adaptation to fluctuating conditions. Key global regulatory mechanisms include regulons, two-component systems, sigma factors, and secondary messengers.Regulons and Global RegulatorsA regulon is a collection of genes and operons controlled by a common global regulator. These regulators enable bacteria to prioritize resource...
62
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

5.8K
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...
5.8K
Regulation of Nuclear Protein Sorting01:45

Regulation of Nuclear Protein Sorting

2.4K
Nuclear protein sorting regulates nucleus composition and gene expression, crucial for determining the fate of a eukaryotic cell. Hence, the entry and exit of molecules across the nuclear envelope is a tightly controlled process. Nuclear protein sorting can be inhibited by one of the following ways: 1) masking cargo signal sequences, 2) modifying the nuclear receptor's affinity for cargo, 3) controlling the nuclear pore size, 4) retaining the cargo during its transit to the cytosol or the...
2.4K
Intracellular Signaling Cascades01:24

Intracellular Signaling Cascades

47.4K
Once a ligand binds to a receptor, the signal is transmitted through the membrane and into the cytoplasm. The continuation of a signal in this manner is called signal transduction. Signal transduction only occurs with cell-surface receptors, which cannot interact with most components of the cell, such as DNA. Only internal receptors can interact directly with DNA in the nucleus to initiate protein synthesis. When a ligand binds to its receptor, conformational changes occur that affect the...
47.4K
Secondary Messengers in Hormone Action01:26

Secondary Messengers in Hormone Action

2.6K
Water-soluble hormones cannot cross the plasma membrane, so they rely on protein receptors that span the membrane to trigger intracellular signaling pathways. These pathways then activate second messengers inside the cell, including cAMP or calcium ions.
Many hormones bind to transmembrane G protein-coupled receptors that connect to regulatory G proteins. These G proteins can then activate enzymes such as adenylyl cyclase or phospholipase C. Adenylyl cyclase converts ATP to cAMP, activating...
2.6K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Designer binders.

Science signaling·2026
Same author

Cholinergic signals and antibodies.

Science signaling·2026
Same author

SIRT2 versus Lck.

Science signaling·2026
Same author

Ca<sup>2+</sup>-driven E3 ligase activity.

Science signaling·2025
Same author

STING's cysteine modifications.

Science signaling·2025
Same author

Tailored receptor modulators.

Science signaling·2025
Same journal

ZNRF3 and RNF43 are active monomeric E3 ubiquitin ligases that self-associate.

Science signaling·2026
Same journal

Allosteric ligands with distinct properties uncover tissue-specific physiological regulation mediated by free fatty acid receptor 2.

Science signaling·2026
Same journal

Diacylglycerol kinase ζ in B lymphocytes supports CD40-mediated immune synapse formation, mTORC1 signaling, and plasma cell fate.

Science signaling·2026
Same journal

The APC/C adaptor Cdh1 stabilizes STING to potentiate innate immune activation in renal cell carcinoma.

Science signaling·2026
Same journal

Fattening mother's milk with oxytocin.

Science signaling·2026
Same journal

Virion display reveals MD-1 as an endogenous agonist for the orphan receptor GPRC5B.

Science signaling·2026
See all related articles

Related Experiment Video

Updated: Aug 24, 2025

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
08:48

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

Published on: January 26, 2016

11.9K

Modulation by macrocyclic peptides.

John F Foley1

  • 1Science Signaling, AAAS, Washington, DC 20005, USA.

Science Signaling
|October 25, 2022
PubMed
Summary
This summary is machine-generated.

Macrocyclic peptides can enter cells to block the active or inactive forms of Gαs, offering a way to precisely control cellular signals.

More Related Videos

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
07:11

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Published on: September 28, 2022

2.8K
Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
10:12

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers

Published on: September 19, 2022

2.2K

Related Experiment Videos

Last Updated: Aug 24, 2025

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
08:48

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

Published on: January 26, 2016

11.9K
Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
07:11

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Published on: September 28, 2022

2.8K
Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
10:12

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers

Published on: September 19, 2022

2.2K

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) mediate cellular responses.
  • Gαs is a key signaling protein downstream of certain GPCRs.
  • Dysregulation of Gαs signaling is implicated in various diseases.

Purpose of the Study:

  • To develop cell-permeable macrocyclic peptides.
  • To investigate the ability of these peptides to antagonize Gαs.
  • To explore the potential for fine-tuning Gαs signaling pathways.

Main Methods:

  • Synthesis of cell-permeable macrocyclic peptides.
  • Biochemical assays to assess Gαs binding and activity.
  • Cell-based assays to measure downstream signaling effects.

Main Results:

  • Developed peptides that efficiently enter cells.
  • Demonstrated peptide antagonism of both active and inactive Gαs states.
  • Showcased the ability to modulate Gαs-mediated signaling.

Conclusions:

  • Cell-permeable macrocyclic peptides are effective modulators of Gαs.
  • These peptides offer a novel approach for precise control of Gαs signaling.
  • Potential therapeutic applications in diseases involving Gαs dysregulation.