Crystallization (Comment) | Organism |
---|---|
molecular docking studies with Hsc70 and apoptozole. The 3,5-bis(trifluoromethyl)phenyl group of apoptozole interacts with the binding site of a triphosphate moiety of ATP through polar interactions, and the two 4-methoxy phenyl moieties of apoptozole are located at the adenosine binding site of Hsc70. The CONH2 group of apoptozole can interact with the Glu376 side chain of Hsc70 via a hydrogen-bonding interaction | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-([2-[3,5-bis(trifluoromethyl)phenyl]-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl]methyl)benzoic acid | inhibits the ATPase activity of Hsc70 by binding to its ATPase domain | Homo sapiens | |
apoptozole | inhibits Hsc70 activity by binding to its ATPase domain | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + H2O | - |
Homo sapiens | ADP + phosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Hsp70 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
metabolism | Hsc70 plays a crucial role in degradation of mutant CFTR by the ubiquitin-proteasome system. The small molecule apoptozole has high cellular potency to promote membrane trafficking of mutant DeltaF508 and its chloride channel activity in cystic fibrosis cells. Apoptozole inhibits the ATPase activity of Hsc70 by binding to its ATPase domain and apoptozole suppresses ubiquitination of DeltaF508 maybe by blocking interaction of the mutant with Hsc70 and E3 ubiquitin ligase CHIP, and, as a consequence, it enhances membrane trafficking of the mutant | Homo sapiens |