Anti-Miotics And Anti-Metabolites W6 Flashcards
Agonist
activates a protein to produce a biological response
Antagonist
Prevents a protein from producing a biological response
Orthosteric inhibitor
Binds to the active site of a protein preventing its activity
Allosteric inhibitor
Vines to a different site on a protein prevent preventing its activity
Covalent inhibitor
Forms a covalent irreversible bond to its target, preventing it activity
What do anti-mitotics target?
Microtubules in cells
What are microtubules?
Spindle structures in a cell which provides structural support
Microtubules in chemotherapy
They pull apart the chromosomes during mitosis and meiosis
What are microtubules made of?
Alpha and beta tubulin
Two mechanisms of action of antimitotic on microtubules
Disruption of microbial assembly
Inhibition of microtubule disassembly
Disruption of micro tubular assembly
Compounds disrupt the assembly of microtubules by binding to free alpha/beta tubulin dimmers
This results in the dissolution of microtubules and the destruction of my topic spindle
In healthy cells, this leads to cell cycle arrest
In cancer cells, this leads to death by catastrophic mitosis
Inhibition of micro tubular disassembly
Stabilisation of microtubules and prevention of their disassembly prevents cell replication
Resistance of microtubule inhibitors
Over expression of P – glycoprotein
Mutations in tubulin gene
Summary
Antimitotic agents interact with tubulin
They can inhibit the formation of microtubules
They can inhibit the disassembly of microtubules
Both inhibition mechanisms lead to cell death
What are anti-metabolites?
Toxic analog is of essential pre-curses for macromolecules
What are anti-metabolites designed to do?
Inhibit essential enzymes and disrupt the formation of macro molecules
Folic acid
An important drug in the formation of pyrimidine bases
Summary of anti-metabolites
They inhibit metabolic processes that generate nucleic acids required in proliferating cells
