Cancer

Question 1

How does alkylation work (nucleic acids)?

Answer 1

• Alkylating agents form strong bonds with DNA
• Alone they are unselective for cancer cells
• Will attack anything which is a good nucleophile
• By mimicking nutrients, cells can be tricked into active uptake

Question 2

Metallation (nucleic acids)

Answer 2

• Can displace the chlorines on cisplatin
• Cisplatin can be injected intravenously and passes through cell membrane, lower chlorine conc inside cells so they are displaced by water ligands
• Cancer cells can develop a resistance to cisplatin because they divide rapidly but oxaliplatin can be used to over come this

Question 3

Topoisomerase inhibition

Answer 3

• Cancer cells divide more rapidly so targeting DNA replication machinery can be selective

Question 4

Hormone receptors

Answer 4

• Some cancers are hormone dependent, so you treat them with hormones with the opposing effect or with antagonsits

Question 5

Structural proteins

Answer 5

• Microtubules are needed for cell division - when a cell divides there are spindles which separates the chromosomes from each other to allow the nuclei to go in the right place and these spindles are made from microtubules
• If we stop microtubules being made then the cell will stop dividing and will stop polymerisation or if we stop them being destroyed it stops depolymerisation

Question 6

Kinase inhibitors

Answer 6

• Kinases are enzymes which perform phosphorylation reactions on certain amino acids
• This changes the structure and function of the phosphorylated protein
• Phosphorylation is often used to activate another kinase
• Blocks chemical messengers which signal the cell to grow and divide

Question 7

Rigidification

Answer 7

• Reduces the available shapes that it can adopt so it will bind to the protein you want it to and will also lose less entropy when binding because it already lost some when becoming more rigid
• Increases selectivity and binding strength (doesnt lose the degree of rotation when it binds)