Cytoskeleton as a therapeutic target Flashcards
What is the mechanism of vinca alkaloids?
- Inhibits microtubule formation
- Binds to beta-tubulin and blocks alpha-tubule polymerization into microtubules
- Disrupts mitotic spindle formation (M-phase arrest)
- Inhibits proliferating cancer cells
What is the mechanism of taxanes?
- Inhibits microtubule disassembly
- Taxanes stabilize GDP-bound tubulin and disrupts microtubule depolymerization
- Inhibits mitotic cell division; anaphase does not occur
- Inhibits proliferating cancer cells
What are cytoskeleton agents such as paclitaxel used in?
Prevention of restenosis coronary stunts
What are some examples of vinca alkaloids?
Vincristine, Vinblastine, Vindesine, Vinorelbine, Vinflunine
What are some examples of taxanes?
Paclitaxel, Docetaxel, Abraxane, Cabazitaxel
What is the mechanism of Colchicine?
- Binds to tubulin and disrupts microtubule polymerization
low concentration stabilizes microtubule dynamics
high concentration stabilizes microtubule dynamics
What conditions is colchicine used for?
- Gout
- Sweet’s syndrome
- Behcet’s syndrome
- scleroderma and liver cirrhosis
- Familial Mediterrean fever
What is the mechanism of Rotenone
Pesticide (prevents microtubule assembly)
What is the mechanism of Mebendazole?
Antihelmintic (microtubule dysfunction)
What is the mechanism of Griseofulin?
-Antifungal
Tinea capitis treatment (disrupts microtubule function and cell division)