Part 2

Question 1

What do kinases do?

Answer 1

They catalyse phosphorylation

Question 2

What are the different types of kinases?

Answer 2

1. Protein kinases - Phosphorylation of amino acids (serine, threonine and tyrosine)
2. Lipid Kinases - Synthesis PIP2 and PIP3 and other substrates such as Nucleotide kinases
3. Membrane bound Kinases - are integral membrane proteins associated with membrane proteins
4. Cytosolic kinases
5. Nuclear Kinases

Question 3

Why use kinases as drug targets?

Answer 3

They are key regulators of signal transduction

Question 4

Give three examples of kinase inhibitors?

Answer 4

Sunitinib, erlotininb and lapatinib

Question 5

What does the kinase phylogenetic tree determine?

Answer 5

It can be used to determine the efficacy of drug due to closely related kinases.

Question 6

Describe the structure of a Kinase

Answer 6

It has an N terminal lobe (made up of B sheet)

and a C terminal lobe (made up of a Helix)/ a hinge back.

Question 7

How do kinases increase specificity?

Answer 7

They increase specificity by using hydrophobic pockets

Question 8

What does the gatekeeper residue do?

Answer 8

It determines access to hydrophobic pockets

Question 9

What is imatinib used for and how does it work?

Answer 9

Imatinib is a kinase inhibitor drug used to treat myelogenous leukaemia. It binds kinase domain in BcrAbI.

Question 10

What are methods for inhibiting kinases?

Answer 10

1. Cetuximab - inhibits ligand binding
2. Pertuzumab - inhibits dimerization
3. Trastuzumab - receptor internalisation