- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: AZD3965 is an inhibitor of the monocarboxylate (lactate) transporter MCT1 (SLC16A1) . Eklevated MCT1 expression has been reported in a range of solid tumours  and it is functionally essential in certain lymphomas which are highly dependent on the glycolytic metabolic pathway . It appears that cancer cells exploit MCT1 to efflux lactate so as to prevent intracellular acidification so as to prevent metabolic catastrophe. MCT1 inhibitors are being investigated for their potential to inhibit glycolysis and tumour growth.
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.✖
|AZD3965-induced inhibition of MCT1 and the subsequent build-up of intracellular lactate, is reported to inhibit lipid biosynthesis and to increase immune cell infiltration of tumours in an in vivo model . The tumours are infiltrated by dendritic and natural killer cells. The combined effects of MCT1 inhibition manifest as tumour growth inhibition.|