Signal Transduction Flashcards
Signal transduction
Mechanisms by which signals detected at a cells surface are
transmitted into the cell’s interior, resulting in changes in the cell’s
behavior / gene expression
Information flow during cell signaling
Receptor-ligand interaction
Result in:
* Conformational changes
* Clustering
* Combination
* Binding affinities measured in Kd
Agonist
synthetic
compound, similar
response
usually causes enhanced response
Antagonist
inhibitor, block
response
Switching receptors off
Signal amplification
Basic types of signaling pathways
- Ligand-gated ion channel
-G protein-coupled receptor - Enzyme-coupled receptor (receptor tyrosine kinase)
- Nuclear receptor
GPCRs structure
- Ligand binding activates a particular G
protein. - G protein: guanine-nucleotide binding
protein. - Activated G protein binds to a target
enzyme or channel, altering their
activity - E.g. olfactory receptors, β-adrenergic
receptors, some hormone receptors,
and opioid receptors
Activation and inactivation of GPCRs
insert
α and βγ Subunits and Signaling
- βγ subunit activates GPR kinases
- α subunits interact with adenylyl cyclase & phospholipase C
insert
G proteins and cAMP
- GSα subunit activates adenylyl cyclase
- adenylyl cyclase converts ATP → cAMP
- cAMP activates protein kinase A
- Phosphodiesterase breaks down cAMP
insert
Protein kinase A activation
by cAMP
Insert
* PKA transfers phosphate from ATP to
Ser/Thr residues
* cAMP regulates PKA activity
* Detach reg unit from cat unit
cell specific cAMP functions
IP3 and DAG in Signaling
Insert
* Ligand-GPCR interaction → activation of Gq
* Gq activates phospholipase C (Cβ), generating
IP3 + DAG.
* IP3 activates the ligand-gated calcium channel,
the IP3 receptor channel → Ca2+ release.
* DAG activates PKC