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pigment epithelium-derived factor   Click here for help

GtoPdb Ligand ID: 13831

Compound class: Endogenous peptide in human, mouse or rat
Comment: The pigment epithelium-derived factor (PEDF) encoded by SERPINF1 is an endogenous ligand of PNPLA2 (a.k.a.adipose triglyceride lipase, ATGL) [7]. PEDF a non-inhibitory member of the serine protease inhibitor (SERPIN) superfamily that is expressed on the surface of retinal epithelial cells [2], and appears to be required for photoreceptor and retinal neuron cell survival [4,8]. Age-related loss of PEDF in the retina is associated with retinal damage and conditions like AMD.

Peptide fragment derivatives of PEDF have demonstrated protective effects in experimental models of degenerative retinal diseases [3,5].
Species: Human
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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.

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View interactive charts of activity data across species
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
patatin like domain 2, triacylglycerol lipase Ligand is endogenous in the given species Hs Activator Binding 8.5 pKd - 7
⤷ pKd 8.5 (Kd 3x10-9 M) [7]
Description: Binding affinity determined using Surface Plasmon Resonance.
Targets where the ligand is described in the comment field
Target Comment
patatin like domain 2, triacylglycerol lipase Endogenous peptide ligand is pigment epithelium-derived factor (SERPINF1) (PEDF), which activates the phospholipase A2 activity of the enzyme [7]. This lipase is commonly called ATGL (adipose triglyceride lipase). It generates diacylglycerol from triacylglycerols, which is subsequently degraded to glycerol and fatty acids by hormone-sensitive lipase (HSL; LIPE) and monoglyceride lipase (MGL; MGLL). In the retina the PNPLA2/PEDF interaction is crucial for the maintenance and survival of retinal epithelial cells, and it prevents retinal degenerative processes.

Lipases including PLA2 and lipases associated with intracellualr lipid droplets (e.g. ATGL, MGLL, FAAH), have been identified as potential molecular targets whose inhibition might provide an antiviral action against infections by RNA viruses (such as SARS-CoV-2 and influenza A virus) in humans [1]. Inhibition of lipase activity is hypothesised to reduce the supply of intracellular free fatty acids upon which the viruses rely for replication, in host cells that are driven to use lipolytic catabolism as a source of free fatty acids and energy in response to virus-induced disruption of normal cellular functions [6].