Cancer Chemotherapy - Anti-mitotics Flashcards
What is an Agonist
A molecule that activates a protein to produce a biological response
What is an Antagonist
A molecule that prevents a protein from producing a biological response
What is a Orthosteric inhibitor?
A molecule that binds into the active site of a protein, preventing its activity
What is a Allosteric inhibitor?
A molecule that binds to a different site on a protein, preventing its activity
What is a Covalent inhibitor?
A molecule that forms a covalent, irreversible bond to its target, preventing its activity
Which part of the cells do Anti-mitotics target?
The microtubules
What are microtubules and why are they important in chemotherapy?
- Microtubules are spindle-like structures in cells which provide structural support
- In chemotherapy they pull apart the chromosomes during mitosis and meiosis
What are microtubules composed of?
αβ-tubulin dimers
What are the 2 mechanism of actions of Anti-mitotics?
- Disruption of microtubule assembly
- Inhibition of microtubule disassembly
How do compounds disrupt the assembly of microtubules?
- By binding to free αβ-tubulin dimers
- That disrupts the balance between polymerisation and depolymerisation
- That then results in the dissolution of microtubules and the destruction of mitotic spindle.
In healthy cells, what does disruption of microtubules lead to?
Cell cycle arrest
In cancer cells, what does disruption of microtubules lead to?
Cell death by catastrophic mitosis
Vinca alkaloids are natural products isolated from what plant?
Periwinkle plant
How can cell replication be prevented?
Stabilisation of microtubules and prevention of microtubule disassemble
Microtubule inhibitors leads to the formation of…
Abnormal bundles of microtubuli
