Exam 2: Chapter 14: Targeted Therapy

Question 1

Why is Gleevec the most successful targeted therapy?

Answer 1

Chronic Myeloid Leukemia patients are homogenous. Meaning they have the same genetic defect that can be treated with this drug.

Question 2

What is the genetic defect associated with CML and Gleevec?

Answer 2

The Philadelphia Chromosome.

Question 3

What is the Philadelphia Chromosome?

Answer 3

A chromosome translocation caused by a fusion of two genes: BRA and ABL

Question 4

What is Gleevec?

Answer 4

The most successful drug in treating Chronic Myeloid leukemia

Question 5

What is the molecular target for gleevec?

Answer 5

Cytoplasmic tyrosine kinase called ABL

Question 6

What are the consequences of The Philadelphia chromosome?

Answer 6

Produces BCR-ABL fusion protein that has a permanently active ABL Kinase

Question 7

How is Gleevec Designed?

Answer 7

It is designed as a small molecule that fits into the ATP binding pocket of ABL kinase

Question 8

How is the blocking of the ATP binding pocket in Gleevec beneficiary?

Answer 8

By blocking the binding pocket it is inhibiting the function of the ABL Kinase and stops growth of the cancer

Question 9

What are the two categories of Antibodies?

Answer 9

Monoclonal and polyclonal

Question 10

What are advantages and differences Monoclonal antibodies have vs small chemical inhibitors?

Answer 10

Monoclonal are:

1. More specific
2. More stable in the bloodstream
3. Stay in the blood stream longer

Question 11

What are disadvantages and differences Monoclonal antibodies have vs small chemical inhibitors?

Answer 11

Monoclonal are:

1. They are too big to pass through the cell membrane
2. They do not penetrate the tumor as easily as small drugs
3. They have to be delivered intravenously
4. More Expensive