Tubulin (microtubules)
The protein that builds the microtubule scaffolding a cell needs to pull its chromosomes apart. Taxanes freeze the scaffold and vinca alkaloids and eribulin stop it forming; either way the dividing cell stalls and dies.
Overview
Alpha and beta tubulin dimers assemble into microtubules, the dynamic fibres that form the mitotic spindle, move cargo and shape the cell. Taxanes such as paclitaxel and docetaxel bind beta tubulin and lock microtubules in place; vinca alkaloids such as vincristine and the halichondrin analogue eribulin bind the growing ends and stop assembly. Both leave the spindle unable to segregate chromosomes, triggering mitotic arrest. The same mechanism carries the MMAE payload of brentuximab vedotin and enfortumab vedotin and the maytansinoid payload of trastuzumab emtansine. Peripheral neuropathy, from microtubule damage in long axons, is the shared dose-limiting toxicity.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · The protein that builds the microtubule scaffolding a cell needs to pull its chromosomes apart. Taxanes freeze the scaffold and vinca alkaloids and eribulin stop it forming; either way the dividing cell stalls and dies.
- 1 · What it is
The protein that builds the microtubule scaffolding a cell needs to pull its chromosomes apart. Taxanes freeze the scaffold and vinca alkaloids and eribulin stop it forming; either way the dividing cell stalls and dies.
- 2 · What goes wrong in cancer
Heterodimeric building block of microtubules; drug binding at the taxane, vinca or maytansine site disrupts spindle dynamics.
- 3 · How drugs use it
No product in this corpus aims at Tubulin (microtubules) yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
External identifiers
Biology
Heterodimeric building block of microtubules; drug binding at the taxane, vinca or maytansine site disrupts spindle dynamics.
- Every dividing cell; the basis of taxane, vinca alkaloid, eribulin and tubulin-payload antibody-drug conjugate therapy
Latest papers
topQuery for this target: (TITLE:"Tubulin" OR ABSTRACT:"Tubulin" OR TITLE:"microtubules" OR ABSTRACT:"microtubules" OR TITLE:"TUBB" OR ABSTRACT:"TUBB") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Tubulin (microtubules), not a curated reading list.
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