GPCR 1

Question 1

GPCR ARE THE ……………………. OF ALL RECEPTOR SUPERFAMILIES

Answer 1

LARGEST

Question 2

THEY HAVE A HIGHLY CONSERVED STRUCTURE OF …. TM DOMAINS

Answer 2

7

Question 3

WHAT DOES THE N TERMINUS USUALLY CONTRIBUTE TO

Answer 3

LIGAND BINDING

Question 4

THE TM DOMAINS ARE CONNECTED BY WHAT

Answer 4

INTRACELLULAR AND EXTRACELLULAR LOOPS

Question 5

THE TM DOMAIN ARE MADE UP OF WHAT

Answer 5

ALPHA HELICES

Question 6

TM3 IS ………………………… LOCATED NEXT TO THE BINDING POCKET AND IS CRUCIAL FOR TRANSDUCTION OF LIGAND BINDING

Answer 6

CENTRALLY

Question 7

MANY LIGAND BINDING SITES ARE BURIED ……………. INTO THE BILAYER BUT THIS CAN VARY IE METABOTROPIC GLUTAMATE RECEPTORS …………………………… ………………

Answer 7

1/3

STICK OUT

Question 8

WHAT HAPPENS DURING BINDING OF AN ACTIVATING LIGAND

Answer 8

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

Question 9

THE C TERMINUS ON GPCR IS AN IMPORTANT SITE OF

Answer 9

REGULATION

Question 10

SUB FAMILIES ARE DIVIDED ACCORDING TO THE STRUCTURE OF THEIR …………………….. ………………. SITES, THE LARGEST BEING ………………………………..

Answer 10

LIGAND BINDING

RHODOPSIN LIKE GPCR

Question 11

WHAT IS AN EXAMPLE OF UNUSUAL ACTIVATION OF GPCR

Answer 11

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

Question 12

KNOWLEDGE OF STRUCTURE CAN LEAD TO WHAT

Answer 12

RATIONAL DESIGN OF NEW SMALL MOLECULE DRUGS TARGETTING GPCR

Question 13

IN WHAT WAY ARE G PROTEINS TIMERS

Answer 13

HOW LONG THERE ARE ACTIVE DETERMINES THE LENGTH OF THE ASSOCIATED SIGNALLING

Question 14

WHERE DO THE G PROTEINS SIT

Answer 14

THEY ARE NATURALLY ANCHORED IN THE PM

Question 15

AT RESTING STATE THE A SUBUNIT OF THE G PROTEIN HAS A ………………… AFFINITY FOR GDP

Answer 15

HIGH

Question 16

WHEN THE LIGAND ACTIVATES THE RECEPTOR AND ITS ……… IS REVEALED, THE ALPHA SUBUNIT …………..
………………. THE CLEFT.

Answer 16

CLEFT

FITS INTO

Question 17

THE ASSOCIATION OF THE ALPHA SUBUNIT IN THE RECEPTOR CLEFT CAUSES THE ALPHA SUBUNIT TO CHANGE SHAPE AND ………………. CAN BIND

Answer 17

GTP

Question 18

BINDING OF …………. WITH …………… SUBUNIT CAUSES REARRANGEMENT OF THE PROTEIN SUCH THAT THE ……………… SUBUNIT …………….. EACH ARE NOW FREE TO ……………….. WITH ……………. MOLECULES

Answer 18

GTP
ALPHA SUBUNIT
BETA-GAMMA
RELEASE
INTERACT
EFFECTOR

Question 19

WHAT IS A G PROTEIN

Answer 19

IT IS A HETEROTRIMERIC PROTEIN MADE UP OF ALPHA BETA AND GAMMA SUBUNITS

Question 20

A G PROTEIN IS ALWAYS NAMED AFTER WHAT

Answer 20

ITS ALPHA SUBUNIT

Question 21

THERE ARE MORE GPRC TO G PROTEINS THEREFORE

Answer 21

THERE IS SHARING OF G PROTEINS

Question 22

THE ALPHA SUBUNIT IS ACTUALLY A WHAT

Answer 22

AN ENZYME THAT CAN HYDROLYSE GTP

Question 23

WHAT DO RGS PROTEINS DO

Answer 23

STIMULATE ALPHA SUBUNIT (GTPASE) ACTIVITY

Question 24

MANY G PROTEINS REGULATE THE ACTIVITY OF ENZYMES THAT

Answer 24

CONTROL LEVELS OF SECOND MESSENGERS

Question 25

LOCAL CONC OF 2ND MESSENGERS ARE DETERMINED BY

Answer 25

RATE OF PRODUCTION
RATE OF DIFFUSION FROM PRODUCTION SITE
RATE OF REMOVAL

Question 26

ADENYLYL CYCLASE CONVERTS ………….. TO ……………

Answer 26

ATP

CAMP

Question 27

WHAT ENZYME BREAKS DOWN CAMP

Answer 27

CAMP PHOSPHODIESTERASE

Question 28

WHAT TYPE OF G PROTEIN SUBUNIT ACTIVATES ADENYLATE CYCLASE

Answer 28

G ALPHA S

Question 29

WHAT TYPE OF G PROTEIN SUBUNIT INHIBITS ADENYLATE CYCLASE

Answer 29

G ALPHA I