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Related Concept Videos

Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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 affinity and are together...
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
IP3/DAG Signaling Pathway01:11

IP3/DAG Signaling Pathway

Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the  phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and produces two-second...
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 cells.
Two...
Amplifying Signals via Enzymatic Cascade01:22

Amplifying Signals via Enzymatic Cascade

When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze the...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.

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Related Experiment Video

Updated: May 16, 2026

Visualization of Replisome Encounters with an Antigen Tagged Blocking Lesion
08:24

Visualization of Replisome Encounters with an Antigen Tagged Blocking Lesion

Published on: July 27, 2021

Activated PLCγ breaking loose.

Peter Gierschik1, Anja Buehler, Claudia Walliser

  • 1Institute of Pharmacology and Toxicology, University of Ulm Medical Center, 89081 Ulm, Germany. peter.gierschik@uni-ulm.de

Structure (London, England : 1993)
|December 11, 2012
PubMed
Summary

Protein tyrosine phosphorylation activates phospholipase C-gamma(1) through a receptor-mediated process. This study details the molecular events involved in this crucial cell signaling pathway.

Area of Science:

  • Biochemistry
  • Structural Biology
  • Cell Signaling

Background:

  • Receptor-mediated activation of phospholipase C-gamma(1) is critical for cellular signaling.
  • Protein tyrosine phosphorylation plays a key role in regulating this activation process.

Discussion:

  • This study investigates the molecular mechanisms underlying PLCγ1 activation by protein tyrosine phosphorylation.
  • Bunney and colleagues employed a multidisciplinary approach including NMR, SAXS, crystallography, ITC, and biochemical assays.
  • The research elucidates the precise sequence of events leading to PLCγ1 activation.

Key Insights:

  • Detailed molecular understanding of PLCγ1 activation sequence.
  • Identification of key structural and functional changes upon phosphorylation.

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Generation and On-Demand Initiation of Acute Ictal Activity in Rodent and Human Tissue

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  • Integration of data from diverse biophysical and biochemical methods.
  • Outlook:

    • Further insights into PLCγ1 regulation could reveal new therapeutic targets.
    • Understanding these signaling cascades is vital for deciphering complex cellular processes.
    • Potential for novel drug development targeting aberrant cell signaling.