Relation Results

Summary

Name TUBB1
Full Name Tubulin beta-1 chain
Synonyms TBB1_HUMAN
Primary ID Q9H4B7
Links - -
Type protein
Relations 5
Inhibitors docetaxel anhydrous; eribulin mesylate; cabazitaxel; paclitaxel
Function Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeab ...
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Type: Score: Layout: SPV 
0.80.80.80.70.8docetaxel anhydrousTUBB1eribulin mesylatecabazitaxelProliferationpaclitaxel

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Relations
Regulator
Mechanism
target
score ℹ
+ docetaxel anhydrousdown-regulates activity img/direct_inhibition.png chemical inhibition TUBB1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259343 Homo sapiens
pmid sentence
Tubulin exists in the cell as dimers of α and β subunits, which complexes with a variety of regulatory proteins. There is a dynamic equilibrium between free and polymerized tubulin causing a state called "dynamic instability," which is a target of anticancer drugs, which inhibit tubulin through polymerization (taxanes, epothilones) or depolymerization (vinca alkaloids). Docetaxel-based therapy was the first such treatment to demonstrate a survival benefit in men with castration-resistant prostate cancer.
Publications: 1 Organism: Homo Sapiens
+ eribulin mesylatedown-regulates activity img/direct_inhibition.png chemical inhibition TUBB1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259345 Homo sapiens
pmid sentence
The complex marine natural product halichondrin B was compared with NSC 707389 (E7389), a structurally simplified, synthetic macrocyclic ketone analog, which has been selected for clinical trials in human patients. NSC 707389 was invariably more potent than halichondrin B in its interactions with tubulin. Both compounds inhibited tubulin assembly, inhibited nucleotide exchange on beta-tubulin, and were noncompetitive inhibitors of the binding of radiolabeled vinblastine and dolastatin 10 to tubulin.
Publications: 1 Organism: Homo Sapiens
+ cabazitaxeldown-regulates activity img/direct_inhibition.png chemical inhibition TUBB1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259341 Homo sapiens
pmid sentence
Among these, larotaxel (XRP9881, formerly RPR109881A)[3,4] and cabazitaxel (XRP6258, TXD258, RPR116258A)[5] share a mechanism of action unique to taxanes, promoting tubulin assembly and stabilizing microtubules against cold-induced depolymerization
Publications: 1 Organism: Homo Sapiens
+ TUBB1up-regulates img/indirect-activation.png Proliferation 0.7
Identifier Residue Sequence Organism Cell Line
SIGNOR-242138 Rattus norvegicus
pmid sentence
However, evidence suggests that the detyrosination/tyrosination cycle of alpha-tubulin may be linked in some cell types to cell division and proliferationNF-Y
Publications: 1 Organism: Rattus Norvegicus
+ paclitaxeldown-regulates activity img/direct_inhibition.png chemical inhibition TUBB1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259347 Homo sapiens
pmid sentence
Here we integrate a computational model for microtubule assembly with nanometer-scale fluorescence microscopy measurements to identify the kinetic and thermodynamic basis of kinetic stabilization by the MTAs paclitaxel, an assembly promoter, and vinblastine, a disassembly promoter. We identify two distinct modes of kinetic stabilization in live cells, one that truly suppresses on-off kinetics, characteristic of vinblastine, and the other a "pseudo" kinetic stabilization, characteristic of paclitaxel, that nearly eliminates the energy difference between the GTP- and GDP-tubulin thermodynamic states. By either mechanism, the main effect of both MTAs is to effectively stabilize the microtubule against disassembly in the absence of a robust GTP cap.
Publications: 1 Organism: Homo Sapiens
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