3.2 Small molecules - TKIs

Question 1

What is the name given to the small molecules involved in targeted therapy of cancer?

Answer 1

tyrosine kinase inhibitors

Question 2

What is the primary intra cellular target of tyrosine kinase inhibitors

Answer 2

protein kinase

Question 3

How can protein kinase lead to tumour progression in cancer?

Answer 3

When protein kinase is dysregualted,

This leads to an increase in proliferative signalling, leading to increased proliferation

Question 4

What is the mode of action of Tyrosine kinase inhibitors?

Answer 4

• Tyrosine kinases are enzymes that transfer phosphate groups from ATP to the amino acid tyrosine on target proteins.
• By inhibiting these enzymes, TKIs disrupt signaling pathways that promote cancer cell growth and survival.

Question 5

Name a commonly used tyrosine kinase inhibitor

Answer 5

imatinib (Gleevec)

Question 6

Pen nib

What is the typical suffix for tyrosine kinase inhibitors?

Answer 6

Nib

Question 7

Small molecule

What is the typical route of administration for tyrosine kinase inhibitors

Answer 7

Oral