Related Experiment Video

Updated: Aug 12, 2026

Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
09:39

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

Published on: January 27, 2014

Ciba-Geigy award for outstanding research. Regulation of adrenergic receptor function by phosphorylation

R J Lefkowitz, M G Caron

    Journal of Molecular and Cellular Cardiology
    |September 1, 1986
    PubMed

    More Related Videos

    Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding10:13

    Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

    Published on: June 9, 2017

    BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells09:21

    BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

    Published on: November 7, 2025

    Related Concept Videos

    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...
    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...
    cAMP-dependent Protein Kinase Pathways01:25

    cAMP-dependent Protein Kinase Pathways

    Cyclic Adenosine Monophosphate (cAMP) is an essential second messenger that activates protein kinase A (PKA) and regulates various biological processes. A single epinephrine molecule binds to GPCR and activates several heterotrimeric G proteins, each stimulating multiple adenylyl cyclase, amplifying the signal, and synthesizing large numbers of cAMP molecules. Small changes in cAMP concentration affect PKA activity. The binding of four cAMP molecules induces a conformational change in PKA,...
    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:
    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 C—inositol-1,4,5-trisphosphate...
    Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

    Adrenergic Agonists: Chemistry and Structure-Activity Relationship

    Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
    Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
    Separation of the aromatic...