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#vinblastine

2 public questions tagged with this topic.

Plant tissue culture 3

Vincristine and Vinblastine belong to:

Catharanthus roseus produces complex dimeric alkaloids via coupling of vindoline derived from tabersonine and catharanthine moieties through peroxidase α-3′,4′-anhydrovinblastine synthase. Resulting vinblastine and vincristine contain indole and dihydroindole units fused through intricate polycyclic framework bearing basic nitrogen essential for biological activity. They disrupt mitosis by specifically binding at vinca site on β-tubulin, preventing microtubule polymerization, arresting cells at metaphase, and inducing apoptosis through JNK pathway. Clinical importance in chemotherapy of childh

Ref: van Der Heijden Curr Med Chem 2004 Catharanthus alkaloids; NCBI NBK21154 indole alkaloid; Cragg Nat Prod Vinca; PubMed 15075446.

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Cytoskeleton

Which drug binds tubulin subunits and prevents polymerization?

Microtubule targeting agents divided into destabilizers preventing polymerization and stabilizers blocking depolymerization used as chemotherapeutics and cell biology tools. Nocodazole colchicine and colcemid belong to destabilizer class binding soluble tubulin dimer interface. Nocodazole binds beta tubulin at colchicine adjacent site near intradimer interface distorting dimer curvature preventing straight conformation compatible with lattice addition and reducing lateral contacts. Result reduces effective free tubulin pool shifts equilibrium below critical concentration triggering disassembly

Ref: Jordan & Wilson, Nat Rev Cancer 2004 – Microtubule destabilizers nocodazole binds tubulin prevents polymerization.

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