Last minute learn

Question 1

Metformin 1

Answer 1

X Resp comp 1
Decrease ATP synth
Increase AMP:ATP
AMPK activayion
DEcreased gluconeo, uncreased uptake

Question 2

Metformin 2

Answer 2

X AMP demainase
Incrase AMP
AMPK activation
DEcreased gluconeo, uncreased uptake

Question 3

Metformin 3

Answer 3

X mGDP
Decrease DHAP:G3P shuttle
Increase in ratios - G3P:DHAP, NADH:NAD, Lactiate: Pyruv
DEcreased gluconeo, uncreased uptake
(Madiraju 2014)

Question 4

Receptor (EX) drugs

Answer 4

Trastuzumab (herceptin) - ErbB2, Jusxtamembrane region, block ectodomain cleavage

Pertuzumab - ErbB2, Blocks dimerisation arm

Cetuximab - ErbB1 (EGFR) - ligand bindinhg competitor

Question 5

Receptor (Cy) drugs

Answer 5

Iressa (class 1) - sites 1+2 (active)
Lapatinib (Class 2) - Allosteric (inactive)
AMP-PNT - ATP analogue

Question 6

BCR-ABL ( chromic myelogenous leukemia) drugs

Answer 6

Imatnib (Class 2) - Sites 1 + 2 (inactrive) - where ATP would bind

Escape mutant T1315 - forms H boond

2nd Gen: Ponatninib - Lower IC50 (inactive) interferes by stopping re-orientation

Question 7

Transpoeters of the intestine cells

Answer 7

SGLT1 - GandG
GLUT5 - F

into blood: GLUT2
don’t forget ATPase shuttleb

Question 8

Epigenetic histone modifiers

Answer 8

HDACs - remove acetylation
HATs - Add acetylation
HMTs - Cionsending histon meth
HDMs - Decondensing histone meth

Question 9

Epigenetic histone activation/deactivation examples

Answer 9

Histone acetylation: H3K27ac
Histone meth (unfold chromatin): H3K4me2
Histone meth (condense C): H3K27me3

Question 10

Ref for EGFR actuvation

Answer 10

Buregess 2003