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CBNS101 Lecture 9: Enzyme-coupled receptors

front 1

T/F Receptor tyrosine kinases (RTKs) are the most common class of enzyme-coupled receptors (60 RTKs in humans)

back 1

True. They are the most common class

front 2

T/F Enzyme coupled receptors usually have 20 transmembrane segments

back 2

False. Typically only 1 segment

front 3

Explain the process of RTK dimerization and autophosphorylation

back 3

When inactive they are far away from each other, but a signal to activate it, will bring the two "rods" closer together (dimerization). The close proximity makes them phosphorylate each other and then phosphorylate the rest of the spaces on the rods. That leads to docking "binding" points for them to start a signal cascade.

front 4

T/F RTKs are always symmetrical

back 4

False. One can solely be the activator and the other can solely be the receiver that phosphorylates both domains.

front 5

What domains do proteins use to dock to RTKs?

back 5

Src homology (SH2) domains or phosphotyrosine binding (PBT) domains

front 6

T/F Some docked proteins to RTK are only stimulatory

back 6

False. They can be inhibitory as well

front 7

*Ran is seen in ______, Rab is seen in ______, and Ras and Rho are seen in ________

back 7

Nuclear transport, vesicular traffic, and cell surface receptors.

front 8

T/F 30% of tumors have hyperactive mutant forms of Ras (Rat sarcoma)

back 8

True. Ras is a key oncogene. A gene that has the potential to cause cancer

front 9

Ras is a membrane bound ________ GTPase

a) heterotrimeric

b) monomeric

back 9

monomeric

front 10

How does Ras play a role in human cancers?

back 10

1/3 cancers are caused by Ras mutations. Meaning it loses the ability to hydrolyze GTP (always ON) so it leads to uncontrolled cell growth.

front 11

The mitogen-activated protein kinase pathway activates MAP _____ which phosphorylates MAP _____ which phosphorylates MAP _____ which phosphorylates _____. It is important for cell proliferation.

back 11

KKK, KK, K, target proteins

front 12

T/ F Humans have 12 MAPKs, 7 MAPKKs, and 7 MAPKKKs

back 12

True. All numbers are correct

front 13

How is unwanted cross activation of kinases avoided?

back 13

Scaffold proteins! So they can activate the assembled set before them and not get confused

front 14

*How does Rho GTPases transmit signals to the cytoskeleton?

back 14

Slide 14: During motor neuron axon growth/migration to the muscle target: Ephrin signals the incorrect cells to activate their Eph RTKs which activates RhoA. The RhoA regulates target proteins by reorganizing actin, collapsing the axon growth cone and repelling the axon growth in that direction

front 15

*How do RTKs signal through membrane bound PI (3,4,5) P3?

back 15

Slide 15

front 16

*PI-3-kinase

back 16

Slide 16

front 17

*mTORC1

back 17

Slide 17