2022-10-13T02:09:02+03:00[Europe/Moscow] en true <p>regulatory, enzymes, transport, and structural</p>, <p>nuclear, rtk, cytokine, ion channel, gpcrs</p>, <p>Nuclear receptor</p>, <p>activating gene expression</p>, <p>several</p>, <p>Nuclear</p>, <p>RTKs</p>, <p>ligand binds ec domain; conformational change; units dimerize, kinase domains come together</p>, <p>Dimerization</p>, <p>ligand or cell type</p>, <p>Cytokine receptors</p>, <p>cytokine</p>, <p>Ligand-gated ion channels</p>, <p>multiple subunits</p>, <p>endogenous ligands</p>, <p>ions, speed of activation/inactivation, direction of ion flow</p>, <p>endogenous ligand receptors</p>, <p>resting, open, desensitized </p>, <p>resting</p>, <p>open</p>, <p>desensitized </p>, <p>modify the orthosteric site to alter transition from rest to active, block open channels, allosterically modulate desensitization</p>, <p>force resting channels open/closed, block open channels, modulate inactivation, modulating subunits</p>, <p>GPCR</p>, <p>GPCR</p>, <p>ec ligand binds to specific R, G-protein gets activated on cytoplasmic/intracellular surface, G-protein changes activity of some effector</p>, <p>G-proteins</p>, <p>heterotrimeric &amp; small g proteins</p>, <p>by the secondary activity on their effectors</p>, <p>cAMP</p>, <p>adenyly</p>, <p>cGMP</p>, <p>guanylate cyclase</p>, <p>effects begin high, diminish over time</p>, <p>ATP, substrate, and co-factor</p>, <p>inhibitors</p>, <p>structural proteins</p> flashcards
Drug-Receptor Interactions

Drug-Receptor Interactions

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  • regulatory, enzymes, transport, and structural

    What are our 4 types of drug receptors?

  • nuclear, rtk, cytokine, ion channel, gpcrs

    What are our 5 types of regulatory receptors?

  • Nuclear receptor

    -primarily responds to lipid-soluble drugs

    -drugs can cross cell membrane and act via intracellular receptors

  • activating gene expression

    What is the most common downstream mechanism for Nuclear receptors?

  • several

    A typical nuclear receptor is composed of ______ domains

  • Nuclear

    What receptor class do these receptors fall under: glucocorticoid, estrogen, androgen, thyroid hormone?

  • RTKs

    -receptors are transmembrane proteins with extracellular ligand binding domains and intracellular enzyme domains

  • ligand binds ec domain; conformational change; units dimerize, kinase domains come together

    How does signaling event work in RTKs?

  • Dimerization

    The chemical reaction that joins two molecular subunits, resulting in the formation of a single dimer

  • ligand or cell type

    Dimerization partners are dependent on ______ or _______

  • Cytokine receptors

    -large class of molecules

    -pass signaling event from extra- to intra-cellular

  • cytokine

    Which form of regulatory receptor possess signaling mechanisms extracellular & intracellularly?

  • Ligand-gated ion channels

    ligand binds receptor---> opens channel, ions flux down electrochemical gradients

  • multiple subunits

    Ligand-gated & Voltage-gated are both composed of what ?

  • endogenous ligands

    How are ligand-gated ion channels categorized?

  • ions, speed of activation/inactivation, direction of ion flow

    How are voltage-gated ion channels categorized?

  • endogenous ligand receptors

    GABA-A, ACh- nAChR, and NMDA-R are what kind of receptors?

  • resting, open, desensitized

    what are the three stages of signaling in ligand-gated ion channels?

  • resting

    - channel is closed and ready to activate when ligand binds

  • open

    -ions are allowed to pass through the cell membrane

  • desensitized

    -no longer passing ions but not ready to activate again-not "sensitive" to ligand

  • modify the orthosteric site to alter transition from rest to active, block open channels, allosterically modulate desensitization

    How can we modulate the three states of ligand-gated ion channels?

  • force resting channels open/closed, block open channels, modulate inactivation, modulating subunits

    How can we modify voltage-gated ion channels?

  • GPCR

    -most complicated of the coupling systems

    -leads to great signal amplification

  • GPCR

    Which regulatory receptor consists of signal transduction or pathways/cascades?

  • ec ligand binds to specific R, G-protein gets activated on cytoplasmic/intracellular surface, G-protein changes activity of some effector

    How do GPCRs work?

  • G-proteins

    -family of proteins that function as molecular switch, an intermediate in R-E coupling

  • heterotrimeric & small g proteins

    _______ & ________ are two types of G-proteins

  • by the secondary activity on their effectors

    How can we further divide G-proteins?

  • cAMP

    -most famous/common intracellular 2nd messenger

    -mediates hormal responses, renal water conservation, calcium homeostasis, etc

  • adenyly

    How is cAMP activated?

  • cGMP

    -only active in a few cell types, i.e. intestinal mucosa and vascular smooth muscle

    -similar activity to cAMP

  • guanylate cyclase

    How are cGMPs activated?

  • effects begin high, diminish over time

    Explain GPCR signaling dynamics.

  • ATP, substrate, and co-factor

    What do enzymes require to signal?

  • inhibitors

    what are most enzyme - targeting drugs characterized as ?

  • structural proteins

    -critical for mechanical support and cellular movement

    -drug targets include tubulin