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PLD2

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Target id: 1434

Nomenclature: PLD2

Family: Phosphatidylcholine-specific phospholipase D, Hydrolases & Lipases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 933 17p13.2 PLD2 phospholipase D2
Mouse - 933 11 42.99 cM Pld2 phospholipase D2
Rat - 933 10q24 Pld2 phospholipase D2
Previous and Unofficial Names Click here for help
Choline phosphatase 2 | phosphatidylcholine-hydrolyzing phospholipase D2 | phospholipase D2 | PLD1C
Database Links Click here for help
Alphafold O14939 (Hs), P97813 (Mm), P70498 (Rn)
BRENDA 3.1.4.4
CATH/Gene3D 2.30.29.30, 3.30.1520.10
ChEMBL Target CHEMBL2734 (Hs), CHEMBL3309055 (Mm)
Ensembl Gene ENSG00000129219 (Hs), ENSMUSG00000020828 (Mm), ENSRNOG00000019604 (Rn)
Entrez Gene 5338 (Hs), 18806 (Mm), 25097 (Rn)
Human Protein Atlas ENSG00000129219 (Hs)
KEGG Enzyme 3.1.4.4
KEGG Gene hsa:5338 (Hs), mmu:18806 (Mm), rno:25097 (Rn)
OMIM 602384 (Hs)
Pharos O14939 (Hs)
RefSeq Nucleotide NM_002663 (Hs), NM_008876 (Mm), NM_033299 (Rn)
RefSeq Protein NP_002654 (Hs), NP_032902 (Mm), NP_150641 (Rn)
UniProtKB O14939 (Hs), P97813 (Mm), P70498 (Rn)
Wikipedia PLD2 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.1.4.4
Description Reaction Reference
A phosphatidylcholine + H2O <=> choline + a phosphatidate
Endogenous inhibitor (Human)
Gβγ  [3]

Download all structure-activity data for this target as a CSV file go icon to follow link

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
oleic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Activation - - 4
⤷ [4]
PIP2 Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Hs Activation - - 2
⤷ [2]
ADP-ribosylation factor 1 {Sp: Human} Peptide Ligand is endogenous in the given species Hs Activation - -
⤷
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
FIPI Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.8 pIC50 5
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [5]
VU0364739 Small molecule or natural product Hs Inhibition 7.7 pIC50 1
⤷ pIC50 7.7 (IC50 1.99x10-8 M) [1]
compound 69 [PMID: 19136975] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 5
⤷ pIC50 6.0 (IC50 9.33x10-7 M) [5]
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cellular signalling
Immuno Process:  Antigen presentation

References

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1. Lavieri RR, Scott SA, Selvy PE, Kim K, Jadhav S, Morrison RD, Daniels JS, Brown HA, Lindsley CW. (2010) Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor. J Med Chem, 53 (18): 6706-19. [PMID:20735042]

2. Lopez I, Arnold RS, Lambeth JD. (1998) Cloning and initial characterization of a human phospholipase D2 (hPLD2). ADP-ribosylation factor regulates hPLD2. J Biol Chem, 273 (21): 12846-52. [PMID:9582313]

3. Preininger AM, Henage LG, Oldham WM, Yoon EJ, Hamm HE, Brown HA. (2006) Direct modulation of phospholipase D activity by Gbetagamma. Mol Pharmacol, 70 (1): 311-8. [PMID:16638972]

4. Sarri E, Pardo R, Fensome-Green A, Cockcroft S. (2003) Endogenous phospholipase D2 localizes to the plasma membrane of RBL-2H3 mast cells and can be distinguished from ADP ribosylation factor-stimulated phospholipase D1 activity by its specific sensitivity to oleic acid. Biochem J, 369 (Pt 2): 319-29. [PMID:12374567]

5. Scott SA, Selvy PE, Buck JR, Cho HP, Criswell TL, Thomas AL, Armstrong MD, Arteaga CL, Lindsley CW, Brown HA. (2009) Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol, 5 (2): 108-17. [PMID:19136975]

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