Tubulin binders

Tubuline binders are also known as tubulin inhibitors.

  • Tubuline depolymerization inhibitors: paclitaxel, epothilone, docetaxel, discodermolide
  • Tubuline polymerization inhibitors:
    • colchicine-binding site: colchicine, combrestatin, 2-methoxyestradiol, methoxy benzenesulfonamides
    • vinca alkaloid binding site: vinblastine, vincristine, vinorelbine, vinflunine, dolastatins, halichondrins, hemiasterlins, cryptophysin
Name Structure
Colchicine colchicine
Taxol taxol
Vinblastine vinblastine
Epothilone epothilone
Discodermolide discodermolide

Interactions with the target


  1. What is the name of the heterocycle in epothilone? And in vinblastine? Taxol?
  2. How many aromatic rings does colchicine have?
  3. What is the name for macrocyclic lactone natural products?
  4. What are the key steps in K.C. Nicolau’s total synthesis of epothilone A?
  5. Describe briefly the key biosynthetic enzymes involved in the synthesis of epothilone?

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