Inhibitors of Serine/Threonine Kinases

Question 1

Serine/Threonine Kinase protein example

Answer 1

mTOR

Question 2

Ser/Threo inh agents

Answer 2

Temsirolimus/Everolimus
Vemrafenib
Dabrafenib + Trametinib

Question 3

Temsirolimus/Everolimus

Answer 3

for advanced renal cell carcinoma. Or pancreatic.

–inhibits mTOR and G1 growth arrest. Rash, Naus, Edema

Question 4

Vemurafenib

Answer 4

for mutant BRAF+ metastatic melanoma. Inhibits B-raf. Causes neoplasms, skin and GI.

Question 5

Dabrafenib + Trametinib

Answer 5

give together for BRAF+ met.mel. Inhibits BRAF and MEK, respectively.
–Causes neoplasms and cardiomyopathy.

Question 6

Genetic mutation example

Answer 6

Melanoma-p16/INK4

also CDK4

Question 7

Somatic mutation example

Answer 7

Burkitt’s lymphoma-MYC oncogene

Question 8

Epigenetic modification example

Answer 8

loss of Histone de-acetylation by HDAC

NOT a mutation, these are modifications (on or off) and are reversible!

Question 9

Bcr-abl is…

Answer 9

an oncogene, result of a chromosomal translocation

Gleevec targets is

Question 10

Cyclin for G1

Answer 10

D

Question 11

Cyclin for S phase

Answer 11

E

Question 12

Cyclin for G2

Answer 12

A

Question 13

Cyclin for M phase

Answer 13

A and B1

Question 14

Tumor suppressor genes, recessive

Answer 14

Rb

p53

Question 15

Oncogenes, dominant

Answer 15

Ras

gets stuck in active GTP bound formation

Question 16

H-ras

Answer 16

Squamous cell carcinoma

Question 17

K-ras

Answer 17

lung carcinoma

colon cancer

Question 18

N-Ras

Answer 18

melanoma

Question 19

Adenocarcinoma mutations

Answer 19

Hras and p53