GPCR Edition – Week 2
Post on 23-Feb-2016
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GPCR Edition – Week 2
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G proteins IP3/DAG Pathway
GPCR Activation
Second Messenge
rsGPCR
RegulationExperime-
ntalMethods
THE HETEROTRIMERIC G PROTEIN COMPLEX IS COMPOSED OF G-ALPHA, G-BETA, AND
THIS OTHER G PROTEIN
G-GAMMA
G-BETA & G-GAMMA
THESE TWO G PROTEINS SUBUNITS
REMAIN AS HETERODIMERS AFTER G PROTEIN COMPLEX
ACTIVATION
GDP & GTP
ACTIVATION OF G-ALPHA LEADS TO
EXCHANGE OF THESE TWO NUCLEOTIDE
PHOSPHATE MOLECULES
GS
THIS CLASS OF G-ALPHA PROTEINS IS RESPONSIBLE FOR
ACTIVATING ADENYLYL CYCLASE (AC)
EFFECTOR PROTEINS
ACTIVATED G PROTEINS BIND TO AND REGULATE THE FUNCTION OF THIS GENERAL TYPE OF
PROTEINS INVOLVED IN SECOND MESSENGER
SIGNALING
THIS MEMBRANE-BOUND ENZYME IS
THE EFFECTOR PROTEIN THAT
GENERATES IP3 AND DAG
PHOSPHOLIPASE C (PLC)
PIP2 IS ENZYMATICALLY CUT TO FORM IP3 AND
THIS MOLECULE
DIACYLGLYCEROL (DAG)
IP3 WILL STIMULATE THE RELEASE OF THIS
CATION FROM PARTICULAR ION
CHANNELS IN THE ENDOPLASMIC
RETICULUMCALCIUM (CA2+)
THIS PROTEIN KINASE REQUIRES CA2+ AND
DAG TO BE FULLY ACTIVE
PKC
THIS PROTEIN CHANGES ITS
CONFORMATION UPON CA2+ BINDING AND MODULATES THE
ACTIVITY OF MANY PROTEINS, INCLUDING
NOS AND KINASESCALMODULIN (CAM)
LIGANDS THAT ACTIVATE A GPCR ARE
KNOWN AS THIS
AGONISTS
INTRACELLULAR
LIGANDS BINDING TO THE EXTRACELLULAR
DOMAINS OF THE GPCR CAUSE
CONFORMATIONAL CHANGES IN THESE
DOMAINS
GPCRS, UNLIKE LIGHT SWITCHES, CAN BE FINE
TUNED TO HAVE A SPECIFIC SIGNAL
DEPENDING ON THE CELL TYPE AND LIGAND, MUCH
MORE LIKE THIS ANALOGY
RHEOSTAT
THIS 3-AMINO ACID MOTIF IN A GPCR IS
CRITICAL FOR G PROTEIN BINDING AND
ACTIVATIOIN
DRY MOTIF
ACTIVATED GPCRS CAN HAVE THEIR
SIGNALING DOWN OR OFF BY PROTEINS LIKE BETA-ARRESTIN IN A PROCESS KNOWN AS
THISDESENSITIZATION
ADENYLYL CYCLASE USES THIS MOLECULE AS A SUBSTRATE FOR
CAMP SYNTHESIS
ATP
CYCLIC GMP (CGMP)
FORMED BY GUANYLYL CYCLASE AND
ACTIVATES PKG
CAMP BINDS TO THIS SUBUNIT OF PKA TO
ACTIVATE THE CATALYTIC SUBUNIT
REGULATORY
GI
THIS G-ALPHA SUBUNIT LOWERS THE
LEVEL OF CAMP BY INHIBITING ADENYLYL
CYCLASE
THIS ENZYME IS RESPONSIBLE FOR
BREAKING DOWN CYCLIC NUCLEOTIDES
PHOSPHODIESTERASE (PDE)
DAILY DOUBLE
PHOSPHATES ARE ADDED TO THIS INTRACELLULAR DOMAIN OF AN
AGONIST-BOUND GPCR C-TAIL/TERMINUS OR
ICL3
THIS ENZYME PHOSPHORYLATES
ACTIVE GPCRS
GRK
THE PROCESS OF BRINGING A GPCR OFF THE MEMBRANE
AND INTO THE CELL IS KNOWN AS THIS
ENDOCYTOSIS
THIS PROTEIN IS RESPONSIBLE FOR
LINKING A PHOSPHORYLATED GPCR TO PROTEINS LIKE CLATHRIN AND
AP-2(BETA-)ARRESTIN
CLATHRIN HEAVY AND LIGHT CHAINS COME TOGETHER TO FORM
THIS THREE-PRONGED QUATERNARY STRUCTURETRISKELION
ION-EXCHANGE, GEL-FILTRATION AND AFFINITY ARE ALL TYPES OF THIS
METHOD TO PURIFY PROTEINSCOLUMN
CHROMATOGRAPHY
THE PROCESS OF INTRODUCING A
MUTATION INTO A SPECIFIC POSITION WITHIN A GENE IS KNOWN AS THISSITE DIRECTED MUTAGENESIS
IN FLOW CYTOMETRY SIDE SCATTER
MEASURES THE OVERALL INTERNAL COMPLEXITY OF A
CELL, WHILE FORWARD SCATTER MEASURES
THISSIZE/SHAPE
THIS PROCESS USES SHORT SEQUENCES OF
SSRNA TO PREVENT THE TRANSLATION OF A
PARTICULAR MRNA INSIDE A CELL
RNA INTERFERENCE (RNAI)
THE HEISMAN AND NATIONAL
CHAMPIONSHIP FLORIDA QB SHOWN
HERE
TIM TEBOW
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