Most common Drug Target - Answer: Receptors
Time frame for Channel-linked Receptors - Answer: Milliseconds
Class name for Channel-linked Receptors - Answer: Ionotropic receptors
Example of Channel-linked Receptors - Answer: Nicotinic/ACh Receptors
Time frame for GPCRs - Answer: Seconds
Class name for GPCRs - Answer: Metabotropic Receptors
Example of GPCRs - Answer: Muscarinic/ACh Receptors
Time frame for Kinase-linked Receptors - Answer: Minutes
Insulin receptors fall under which type of receptor category? - Answer: Kinase-linked
Receptors
How long does it take for insulin to take effect? - Answer: Minutes
Time frame of Nuclear receptors - Answer: Hours to Days
How many transmembrane domains are there on GPCRs? - Answer: 7
The alpha subunit of G protein is what type of enzyme? - Answer: GTPase (slow)
1
APPHIA - Crafted with Care and Precision for Academic Excellence.
,The G-proteins are [intracellular or extracellular]? - Answer: intracellular, but membrane
associated
The N-terminus of the GPCR is - Answer: Extracellular
The C-terminus of the GPCR is - Answer: Intracellular
When what is bound to alpha subunit, are the g proteins turned on? - Answer: GTP
alpha S subunit of G protein activates - Answer: adenylyl cyclase
Adenylyl cyclase increases - Answer: cAMP
cAMP activates - Answer: PKA
alpha I subunit of G proteins inhibits - Answer: Adenylyl cyclase
alpha q subunit of G protein activates - Answer: PLC
PLC increases levels of what two things? - Answer: DAG and IP3
IP3 increases levels of intracellular _________ - Answer: Calcium
DAG activates - Answer: PKC
T/F: There are no 2nd messengers in Kinase-linked receptor signaling - Answer: True
2
APPHIA - Crafted with Care and Precision for Academic Excellence.
, In receptors associated w/ cytosolic kinases:
Receptors are initially _____________________
once ligand binds, they _______________________
After that, ________ gets activated which will phosphorylate __________ residues. -
Answer: monomeric; dimerize; JAK; Tyrosine
In receptors associated w/ cytosolic kinases, proteins with _______ domains (such as
STAT, SHC, GRB2, PI3K) bind and gets activated via ______________ of those
residues. Once activated, they act as __________________ and translocate to the
______________. - Answer: SH2; phosphorylation; Trxn factors; nucleus
Receptor tyrosine kinases have ____________________ tyrosine kinase activity. -
Answer: Intrinsic
T/F: Insulin acts on receptor tyrosine kinases. - Answer: True
The _____ subunits of receptor tyrosine kinases phosphorylate _________ residues. -
Answer: beta; tyrosine
In receptor tyrosine kinases that have insulin bound, phosphorylated tyrosine residues
will phosphorylate ________ which will activate ______________ and the ___________
pathways. - Answer: IRS; GRB2/mSOS; PI3K
The GRB2/mSOS pathway activates _____________. - Answer: mek, MAPK, etc.
The PI3K pathway activates _____________ pathway which phosphorylates effector
proteins. - Answer: PKB/AKT
3
APPHIA - Crafted with Care and Precision for Academic Excellence.