GPCR 1 Flashcards
GPCR ARE THE ……………………. OF ALL RECEPTOR SUPERFAMILIES
LARGEST
THEY HAVE A HIGHLY CONSERVED STRUCTURE OF …. TM DOMAINS
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WHAT DOES THE N TERMINUS USUALLY CONTRIBUTE TO
LIGAND BINDING
THE TM DOMAINS ARE CONNECTED BY WHAT
INTRACELLULAR AND EXTRACELLULAR LOOPS
THE TM DOMAIN ARE MADE UP OF WHAT
ALPHA HELICES
TM3 IS ………………………… LOCATED NEXT TO THE BINDING POCKET AND IS CRUCIAL FOR TRANSDUCTION OF LIGAND BINDING
CENTRALLY
MANY LIGAND BINDING SITES ARE BURIED ……………. INTO THE BILAYER BUT THIS CAN VARY IE METABOTROPIC GLUTAMATE RECEPTORS …………………………… ………………
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WHAT HAPPENS DURING BINDING OF AN ACTIVATING LIGAND
AN AGONIST REACHES THE POCKET DETECTED BY TM3
THIS UNDERGOES A CONFORMATIONAL CHANGE THAT MOVES TM5 AND TM6 TO REVEAL A G PROTEIN BINDING POCKET
THE C TERMINUS ON GPCR IS AN IMPORTANT SITE OF
REGULATION
SUB FAMILIES ARE DIVIDED ACCORDING TO THE STRUCTURE OF THEIR …………………….. ………………. SITES, THE LARGEST BEING ………………………………..
LIGAND BINDING
RHODOPSIN LIKE GPCR
WHAT IS AN EXAMPLE OF UNUSUAL ACTIVATION OF GPCR
PAR RECEPTORS ARE GPCR ACTIVATED BY PROTEINASES
PART OF THE N TERMINUS IS CLEAVED BY A PROTEINASE, THE REMAINING TERMINUS FOLDS INTO ITS OWN BINDING SITE TO ACTIVATE THE RECEPTOR
KNOWLEDGE OF STRUCTURE CAN LEAD TO WHAT
RATIONAL DESIGN OF NEW SMALL MOLECULE DRUGS TARGETTING GPCR
IN WHAT WAY ARE G PROTEINS TIMERS
HOW LONG THERE ARE ACTIVE DETERMINES THE LENGTH OF THE ASSOCIATED SIGNALLING
WHERE DO THE G PROTEINS SIT
THEY ARE NATURALLY ANCHORED IN THE PM
AT RESTING STATE THE A SUBUNIT OF THE G PROTEIN HAS A ………………… AFFINITY FOR GDP
HIGH
WHEN THE LIGAND ACTIVATES THE RECEPTOR AND ITS ……… IS REVEALED, THE ALPHA SUBUNIT …………..
………………. THE CLEFT.
CLEFT
FITS INTO
THE ASSOCIATION OF THE ALPHA SUBUNIT IN THE RECEPTOR CLEFT CAUSES THE ALPHA SUBUNIT TO CHANGE SHAPE AND ………………. CAN BIND
GTP
BINDING OF …………. WITH …………… SUBUNIT CAUSES REARRANGEMENT OF THE PROTEIN SUCH THAT THE ……………… SUBUNIT …………….. EACH ARE NOW FREE TO ……………….. WITH ……………. MOLECULES
GTP ALPHA SUBUNIT BETA-GAMMA RELEASE INTERACT EFFECTOR
WHAT IS A G PROTEIN
IT IS A HETEROTRIMERIC PROTEIN MADE UP OF ALPHA BETA AND GAMMA SUBUNITS
A G PROTEIN IS ALWAYS NAMED AFTER WHAT
ITS ALPHA SUBUNIT
THERE ARE MORE GPRC TO G PROTEINS THEREFORE
THERE IS SHARING OF G PROTEINS
THE ALPHA SUBUNIT IS ACTUALLY A WHAT
AN ENZYME THAT CAN HYDROLYSE GTP
WHAT DO RGS PROTEINS DO
STIMULATE ALPHA SUBUNIT (GTPASE) ACTIVITY
MANY G PROTEINS REGULATE THE ACTIVITY OF ENZYMES THAT
CONTROL LEVELS OF SECOND MESSENGERS
LOCAL CONC OF 2ND MESSENGERS ARE DETERMINED BY
RATE OF PRODUCTION
RATE OF DIFFUSION FROM PRODUCTION SITE
RATE OF REMOVAL
ADENYLYL CYCLASE CONVERTS ………….. TO ……………
ATP
CAMP
WHAT ENZYME BREAKS DOWN CAMP
CAMP PHOSPHODIESTERASE
WHAT TYPE OF G PROTEIN SUBUNIT ACTIVATES ADENYLATE CYCLASE
G ALPHA S
WHAT TYPE OF G PROTEIN SUBUNIT INHIBITS ADENYLATE CYCLASE
G ALPHA I
