Med Chem of Tyrosine Kinase Inhibitors (Dr. Parang)

Which type of kinase inhibitors bind to the active conformation of the kinase and compete with ATP?

Type 1 inhibitors

Type 2 inhibitors

Type 3 inhibitors

Type 4 inhibitors

1

Which one of these kinases is a non-receptor kinase?

1. JAK

2. EGFR

3. VEGFR

4. PDGFR

1

What is the mechanism of resistance for Imatinib?

A. The point mutation of a gatekeeper amino acid

B. Slow metabolism

C. Rapid metabolism by CyP450

D. Binding to P-gp

A

What is the gatekeeper residue in Bcr-Abl kinase that affects the binding of certain inhibitors?

A. Aspartate

B. Methionine

C. Threonine

D. Isoleucine

C

matinib and nilotinib are examples of which type of Bcr-Abl inhibitors?

A. Type 1

B. Type 2

C. Type 3

D. Type 4

B

Which of the following drugs have 2-phenylaminopyrimidine as a pharmacophore?

A. Sorafenib

B. Dasatinib

C. Erlotinib

D. Lapatinib

E. Nilotinib

E

Which Bcr_Abl inhibitor exhibits potent T315I inhibitory activity and was developed to overcome steric hindrance in the binding pocket?

A. Nilotinib

B. Imatinib

C. Ponatinib

D. Dasatinib

C

Which of the following receptor tyrosine kinases (RTKs) belongs to the HER family?

A. FGFR

B. IGFR

C. EGFR

D. MET

C

Which HER kinase is also known as ErbB1 and is commonly targeted in cancer therapy?

A. HER2

B. HER3

C. HER4

D. EGFR

D

Which of the following is an example of a Type 1 inhibitor? Select all that apply.

A. Gefitinib

B. Imatinib

C. Nilotinib

D. Erloitinib

A,D

Which one of these inhibitors has 4-anilinoquinazoline pharmacophore? Select all that apply.

A. Erlotinib

B. Sorafenib

C. Gefitinib

D. Ruxolitinib

A,C

What is angiogenesis?

A. Formation of new blood vessels from the endothelium of existing vessels.

B. The death of blood vessels from the endothelium of existing vessels.

C. The fusion of blood vessels from the endothelium of existing vessels.

D. The remodeling of blood vessels from the endothelium of existing vessels.

A

Which of the following is a key enzymatic player in the generation of new blood vessels?

A. VEGF1

B. VEGF2

C. VEGF3

D. VEGF4

B

Which of the following is a type 2 TKI?

A. Sorafenib

B. Sunitinib

C. Gefitinib

D. Erlotinib

A

Which of the following compounds targets both inactive and active conformation of tyrosine kinase? (Select all that apply)

A.Sunitinib

B. Dasatinib

C. Erlotinib

D Gefitinib

E. Sorafenib

A,B