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Synonyms: 17-AAG | 17-allylamino-17-demethoxygeldanamycin | 17-N-allylamino-17-demethoxygeldanamycin | 17AAG | compound 4 [PMID:15978816]
Compound class: Synthetic organic
Comment: 17-AAG inhibits the activity of hsp90. The compound is a derivative of the antibacterial geldanamycin.
As with other natural products, there is some ambiguity in the absolute stereochemistry annotated by different online resources. PubChem records an alternative isomer with a Z bond at position 12 which has CID 6505803. 17-AAG acts as a femtomolar inhibitor of Met tyrosine kinase receptor-dependent urokinase-plasminogen activation .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.
|Summary of Clinical Use
|The EMA has granted orphan drug designation for this compound as a treatment for malignant gastrointestinal stromal tumours (GIST), chronic myeloid leukemia (CML, and the FDA for the same indication) and multiple myeloma (MM). 17-AAG was investigated as a potential antineoplastic therapy . Click here to link to ClinicalTrials.gov's list of registered tanespimycin trials. There are no currently active trials (Sept 2014).
|Mechanism Of Action and Pharmacodynamic Effects
|17-AAG binds to the common N-terminal domain ATP/ATP binding site on both α and β Hsp90 isoforms. This destabilises Hsp90 client proteins, a number of which are oncogenic, and cells undergo apoptosis .