Lecture 5 - Protein Strucutre Flashcards
Are structural proteins usually drug targets?
No
Which structural protein has been useful in drug design?
Tubulin
What are the three main drug target proteins?
Receptors, enzymes and transporters
What do transport proteins do (3)?
- Transport chemical building blocks (polar) across the cell membrane
- Transport neurotransmitters back into the neuron
What can go wrong with receptors?
- Over-activation of the cell due to too much messenger
- Under-activation of the cell due to tell little messenger
How do we fix over-activation and under-activation?
- Introduce antagonists
- Introduce agonists
What are the three families of receptors?
Ion channels
G-protein coupled
Kinase-linked
What is signal-transduction
The chain of events that involve secondary messengers, proteins and enzymes
What is the difference between the 3 types of protein drug targets?
1) Enzymes - there is a chemical transformation of the LMW compound
2) Receptors - there is a message and the LMW compound leaves unchanged
3) The LMW is moved into the cell unchanged after binding
What do all amino acids have? (4)
Carboxylic acid groups (Co2H)
Amino group (NH2)
Functional group (R)
Central C-H motif
What is special about the structure of proline
The side chain is bonded to both the amino and carboxylate groups
Where is proline normally found in the protein?
protein ‘bends’
Why is proline also termed an imino acid
It has a 2° amino group instead of a 1° amino group
What are the two S-containing amino acids
Cysteine (SH)
Methionine (S-CH3)
Do charged amino acid residues stabilise protein conformations?
Yes