| + |
paclitaxel | down-regulates activity 
chemical inhibition
|
TUBB1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259347 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 28298489 |
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 |
| + |
TUBB1 | up-regulates 
|
Proliferation |
0.7 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-242138 |
|
|
Rattus norvegicus |
|
| pmid |
sentence |
| 17118269 |
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 |
| + |
docetaxel anhydrous | down-regulates activity
chemical inhibition
|
TUBB1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259343 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23337758 |
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 mesylate | down-regulates activity
chemical inhibition
|
TUBB1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259345 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 16940412 |
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 |
| + |
cabazitaxel | down-regulates activity
chemical inhibition
|
TUBB1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259341 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 21770474 |
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 |
3.0
TUBB1
- 
- 