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