Related Experiment Video

Updated: Jan 13, 2026

Real-time Live-cell Flow Cytometry to Investigate Calcium Influx, Pore Formation, and Phagocytosis by P2X7 Receptors in Adult Neural Progenitor Cells
11:47

Real-time Live-cell Flow Cytometry to Investigate Calcium Influx, Pore Formation, and Phagocytosis by P2X7 Receptors in Adult Neural Progenitor Cells

Published on: April 3, 2019

9.7K

Activity of Peptides Modulating the Action of p2x Receptors: Focus on the p2x7 Receptor

Jonathas Albertino De Souza Oliveira Carneiro1,2, Guilherme Pegas Teixeira1,3, Leandro Rocha3,4

  • 1Laboratory for Evaluation and Promotion of Evaluation and Promotion of Environmental Health (LAPSA), Oswaldo Cruz Institute, Oswaldo Cruz Foundation, Rio de Janeiro 21040-900, Brazil.

Pharmaceuticals (Basel, Switzerland)
|October 29, 2025
PubMed

Insights

Peptides can modulate P2X receptors, particularly the P2X7 subtype, influencing ion channel function. This review explores how various peptides interact with and affect these crucial cellular gatekeepers.

Area of Science:

  • Ion channel physiology
  • Molecular pharmacology
  • Immunology

Background:

  • P2X receptors are ATP-gated ion channels critical in neuronal and immune cells.
  • The P2X7 receptor subtype, activated by high ATP levels, mediates inflammation and cell death.
  • Antimicrobial peptides (AMPs) are key defense molecules with diverse mechanisms, including membrane interaction and ion channel modulation.

Purpose of the Study:

  • To review the direct and indirect modulatory effects of various peptides on P2X receptor subtypes, with a focus on P2X7.
  • To elucidate the relationship between distinct peptide characteristics and their functional impact on P2X receptors.

Main Methods:

  • Literature review of studies investigating peptide interactions with P2X receptors.
  • Analysis of peptides known to modulate P2X7 receptors, including beta-amyloid, LL-37/hCap18, Pep19-2.5, rCRAMP, ADESG, and polymyxin B.

Main Results:

  • Several peptides directly interact with and modulate P2X7 receptor activity.
  • Peptides exhibit diverse mechanisms, affecting ion channel gating, pore formation, and downstream cellular responses.
  • The specific characteristics of peptides influence their efficacy and selectivity towards P2X receptor subtypes.

Conclusions:

  • Peptides represent a significant class of modulators for P2X receptors, offering potential therapeutic avenues.
  • Understanding peptide-P2X receptor interactions is crucial for developing new treatments for inflammatory and neurological conditions.
  • Further research into peptide structure-activity relationships can optimize their use in targeting P2X channel function.
Keywords:
P2X receptorsP2X7 receptorspeptidespurinergic receptors

More Related Videos

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels16:36

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels

Published on: May 18, 2009

15.2K
Screening Peptides that Activate MRGPRX2 using Engineered HEK Cells12:38

Screening Peptides that Activate MRGPRX2 using Engineered HEK Cells

Published on: November 6, 2021

3.0K

Related Concept Videos

Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
3.8K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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...
7.3K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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:
3.8K
Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....
4.7K
Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
2.7K
G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
5.6K