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Biochem Receptor & Second Messengers
ross University
49
Chemistry
Graduate
11/27/2009

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Term
KD
Definition
Dissociation Constant. It's equal to ([receptor][hormone])/[receptor-hormone] where 1/2 of the receptors are bound by hormone. (or where the concentration of [H] = [H-R]
Term

Steroid Hormone

How reach receptor? Where?

R-H binds what?

Function?

 

Definition

Diffuse across Plasma Membrane.

Binds receptor in cytoplasm.

H-R binds response elements in promoter & enhancers of genes.

Get transcription.

Term
4 steroid hormones
Definition

thyroid hormones

retinoic acid (Vit A)

Calcitriol (Vit B)

steroid hormones

Term

Nicotinic Acetylcholine receptor.

where found.

function?

Definition

Neuromuscular Junction

Ion channel

Term

Ligand Gated Ion Channel

fast / slow effect?

open / closed at rest?

2 types?

Definition

Fast effects of NT's

Closed @ rest

open when NT binds

2 types - Na channel - depolarize membrane

Cl & K channel hyperpolarize membrane

Term

Gaba A receptor.

where?

function?

Definition

in brain

chloride channel (inhibitor)

Term

synthesis of cyclic AMP

degradation?

Definition

ATP - acdenylate cyclase -> cyclic AMP (cleave 2 phosphate groups & attach oxygen of last one to the #3 carbon on ribose sugar.

Degraded by cyclic AMP phosphodiesterase to AMP.

Term

G-Protein

binding site?

subunits?

function?

Definition

Guanine binding site

3 subunits α, β & γ (last two are membrane bound)

α subunit function to activate adenylyl cyclase.

Term
cyclic AMP signal cascade
Definition

cyclic AMP activate PKA by attaching to regulatory subunits to dissociate from PKA. 

activated PKA catalytic subunit activates CREB by phosphorylation

(CREB - cyclic AMP response binding element)

CREB = transcription factor

Term
mechanism of inhibiting adenylate cyclase
Definition
G-Protein has a different αi-subunit that inhibits adenylate cyclase
Term

cAMP action on liver

hormone?

Definition

hormone = glucagon

glycogen breakdown

Term

cAMP action in adipose tissue.

hormone?

what receptor?

Definition

hormone = epinephrine

on β-receptor

cause Fat breakdown

Term

cAMP action on bronchial & vascular smooth muscle

hormone?

receptor?

action?

Definition

relaxation

β-receptor

epinephrine

Term

cAMP action on thyroid gland

hormone?

 

Definition

proliferation / hormone synthesis

TSH = hormone

Term

cAMP action on adrenal cortex

hormone?

Definition

proliferation / hormone synthesis

ACTH

Term

cAMP action on melanocytes

hormone?

Definition

melanin synthesis

MSH

Term

cAMP action on intestine

hormone

Definition

Diarrhea

pancreatic polypeptide

Term

cAMP on kidney

hormone?

Definition

water retention

vasopressin

Term

inhibition of cAMP in intestine cause?

hormone?

Definition

constipation

opioid peptides

Term

inhibition of cAMP in brain response?

3 diff hormones?

Definition

opioid peptides - analgesia

epinephrine (α-2 receptor) hypotension

dopamine - euphoria

Term

inhibition of cAMP on pituitary gland response?

hormone?

 

Definition

inhibition of growth hormone GH excretion

somatostatin

Term

inhibition of cAMP on melanocytes response?

hormone?

Definition

inhibition of melanin synthesis

melatonin

Term

Pseudohypoparathyroidism

normal PTH function

cause of disease?

symptoms?

Definition

PTH normally raises blood Ca level by raising cAMP

disease caused by mutation in PTH receptor

pt has hypocalcemia, tetany

Term

Toxic thyroid nodules

3 causes?

Definition

hyperthyroidism

tumors in thyroid gland - overproduction of hormones.

caused by either mutation in TSH receptor. (TSH is the thyroid stimulating hormone from pituitary gland)

or a mutated Gs protein that keeps G-protein active by blocking the GTPase activity

Term

Cholera Toxin 

effect in intestines?

also pertussis toxin in respiratory tract.

Definition

bacterial infection in intestine 

it enters cells, modify α-subunit of Gs protein thus no more GTPase activity leaving it in permanently active state.

Term
mechanism of DAG (diacylglycerol) & IP3 as second msngrs
Definition

signal -> G-protein linked receptor

activated G-protein α-subunit activate phospholipaseC

this cleaves IP3 from diacylglycerol

IP3 trigger Ca release from ER

Term
smooth muscle contraction mech
Definition

Ca add to Calmodulin

which active MLC-Kinase (myosin light chain) by phosphorilation

get contraction.

Term
3 ways to elevate cytoplasmic Ca
Definition

hormones acting on G-protein & IP3

ligand-gated Ca channel (NMDA receptor in brain)

voltage-gated channel

Term
3 intracellular Ca receptors
Definition

protein kinase C

calmodulin

troponin C

Term
calcium action & hormone in pancreas
Definition
acetylcholine - enzyme secretion
Term
calcium action & hormone in mast cells
Definition
antigens - histamine secretion
Term
calcium action & hormone in bronchial smooth muscle
Definition
histamine - contraction
Term
calcium action & 3 hormones in vascular smooth muscle
Definition
epinephrine (a1 receptors) - contraction
vasopressin & angiotensin (IP3 system) - contraction
Term
calcium action & hormone in liver
Definition
vasopressin - glycogen breakdown
Term
calcium action & hormone in platelets
Definition
thrombin - activation
Term
calcium action & hormone in endothelial cells
Definition
bradykinnin/histamine/Ach - NO synthesis
Term
cGMP affect in smooth muscle, 2 hormones
Definition
ANF (atrial natriuretic factor) & Nitric Oxide (NO) relaxes muscle.
Term
PDE5 inhibitor mech in smooth muscle
Definition
inhibit cGMP-specific phosphodiesterase - used in Viagra
Term
ANF (atrial natrouretic factor), it's receptor type? what's it's function?
Definition
receptor = ligand-activated guanylate cyclase. It makes cGMP which stimulates Protein kinase C which phosphorylates proteins
Term
when is ANF released by the heart? what two organ systems does it work on?
Definition
released when BP is to high cuz too much Na around.
Kidney - incr Na excretion
Relax bloodvessels & vascular smooth muscles
Term
2 methods of regulating guanylate cyclase
Definition
1. membrane bound guanylate cyclase is activated by hormones
2. cytoplasmic guanylate cyclase is activated by nictric oxide (NO)
Term
Affect of Ca in endothelial cells
Definition
initiate Argenine to donate a nitrogen to make NO
NO diffuse through to smooth muscle & cause conversion of GTP to cGMP and get relaxation
Term
affect of Ca in vascular smooth muscle
Definition
causes contraction
Term

growth factor receptors

mechanism?

Definition

receptor oligomerizes

receptor autophophorylates

signal protein w/ SH2 domain bind

signal protein -> activated allosterically

or tyrosine -> phosphorylated

Term

insulin receptor

similar to what receptor?

what 2 differences to that receptor?

Definition

similar to growth factor receptors

diff: unstimulated receptor is a disulfide-bonded tetramer

most effects are mediated by IRS1 & 2

 

Term

growth factor receptor activation of IP3 system

 

Definition

Phospholipase C-γ catalize PIP3 to IP3

IP3 -> Ca release from ER

Term
growth factor receptor activation of protein kinase B
Definition

autophosporylated receptor activates

Phosphoionositide-3-kinase (lipid kinase) convert PIP2 to PIP3 

which activates PKB (protein kinase B or AKT)

Term
growth factor receptor activating MAP kinases
Definition

autophosphorylated receptor 

activate RAS (a small G-protein) 

which initiate phosphorylation cascade

which activates MAP kinase (mitogen-activated protein kinase)

Term
desensitization of beta-adrenergic receptors
Definition

receptor phosphorylated by BARK/PKA thus becomes inactive

arrestin binds it

gets pulled in from cell membrane to go to lysosome

BARK = (β-adrenergic receptor kinase)

PKA = Protein kinase A

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