Mode of Action Flashcards
(39 cards)
transduction event
initiated by receptor; activates amplifier
amplifier
(enzyme) makes 2nd messenger; activated by transduction event
second messenger
(CS) made by amplifier; activates internal effector
internal effector
(protein kinase) activated by 2nd messenger
protein kinase
internal effector; puts phosphate on specific substrate
G protein coupled receptor (GCPR)
receptor
G proteins
Gs, Gi, Gq; transducer
adenylyl cyclase (AC)
converts ATP to cAMP
phosphoproteins
de-phosphorylated proteins from PKA
phosphatase
enzyme that removes phosphate from a protein
positive allosteric event
actions of cAMP on PKA; cAMP activates PK; reversible and concentration dependent
transcription factor
CREB produced from cAMP activated PK
EPAC (cAMP regulated guanine nucleotide exchange protein)
cAMP binds to EPAC; Rap-1 causes GTP to GDP
phosphatidylinositol
phospholipid in PM; cleaved into IP3 and DAG by phospholipase C
inositol triphosphate (IP3)
ligand that binds to gated Ca++ channel; phospholipid; 2nd messenger
diacylglycerol (DAG)
allosterically activates PKC; 2nd messenger
calcium as 2nd messenger
IP3/DAG pathway; Ca++ released and activates PKC
protein kinase C
mediates biological response
Ca++/calmodulin (CAM kinase)
calcium binds to calmodulin
guanylate cyclase
converts GTP to cGMP
cGMP
GTP converted to cGMP; pathway w/no G protein
cGMP dependent protein kinase
allosterically activated by cGMP
tyrosine kinase type 1
ligand binds to receptor subunit; another receptor subunit; TK binds to activated complex; TK phosphorylates; bio response; internalized by ubiquitin
tyrosine kinase type 2
TK catalytic site in receptor; binding reversible; PO4 substrate protein mediates bio response; insulin receptor