phosphodiesterase 4C | Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) | IUPHAR/BPS Guide to PHARMACOLOGY

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phosphodiesterase 4C

target has curated data in GtoImmuPdb

Target id: 1302

Nomenclature: phosphodiesterase 4C

Abbreviated Name: PDE4C

Family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - PDE4C phosphodiesterase 4C
Mouse - - Pde4c phosphodiesterase 4C, cAMP specific
Rat - - Pde4c phosphodiesterase 4C
Previous and Unofficial Names
phosphodiesterase E1 dunce homolog (Drosophila) | cAMP-specific 3,5-cyclic phosphodiesterase 4C | phosphodiesterase 4C, cAMP-specific
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.1.4.17
Rank order of affinity (Human)
cyclic AMP >> cyclic GMP

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CDP840 Hs Inhibition 7.7 pKi 3
pKi 7.7 (Ki 1.89x10-8 M) [3]
Description: Inhibition of [3H]-R-rolipram binding to recombinant human PDE4C2 isoenzyme
RS-25344 Hs Inhibition 8.1 pIC50 4
pIC50 8.1 [4]
MK-0359 Hs Inhibition 8.0 pIC50 1
pIC50 8.0 (IC50 9.1x10-9 M) [1]
apremilast Hs Inhibition 6.9 pIC50 5
pIC50 6.9 (IC50 1.18x10-7 M) [5]
Description: Potency against recombinant human PDE4C1 isoform in a TR-FRET assay.
ibudilast Hs Inhibition 6.6 pIC50 2
pIC50 6.6 (IC50 2.39x10-7 M) [2]
rolipram Hs Inhibition 6.5 pIC50 7
pIC50 6.5 (IC50 3.16x10-7 M) [7]
UFM24 Hs Inhibition 5.8 pIC50 6
pIC50 5.8 (IC50 1.75x10-6 M) [6]
Description: Inhibition of PDE4C1 activity in vitro.
Ro20-1724 Hs Inhibition 5.4 pIC50 7
pIC50 5.4 (IC50 3.98x10-6 M) [7]
Immunopharmacology Comments
PDE4 is a drug target, whose inhibition has anti-inflammatory action. PDE4 inhibitors have already entered clinical use, being employed in the treatment of inflammatory skin conditions such as psoriatic arthritis (apremilast) and atopic dermatitis (crisaborole).

References

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1. Huang Z, Dias R, Jones T, Liu S, Styhler A, Claveau D, Otu F, Ng K, Laliberte F, Zhang L et al.. (2007) L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition. Biochem. Pharmacol., 73 (12): 1971-81. [PMID:17428447]

2. Kodimuthali A, Jabaris SS, Pal M. (2008) Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. J. Med. Chem., 51 (18): 5471-89. [PMID:18686943]

3. Perry MJ, O'Connell J, Walker C, Crabbe T, Baldock D, Russell A, Lumb S, Huang Z, Howat D, Allen R et al.. (1998) CDP840: a novel inhibitor of PDE-4. Cell Biochem Biophys., 29: 113-32. [PMID:9631241]

4. Saldou N, Obernolte R, Huber A, Baecker PA, Wilhelm R, Alvarez R, Li B, Xia L, Callan O, Su C et al.. (1998) Comparison of recombinant human PDE4 isoforms: interaction with substrate and inhibitors. Cell. Signal., 10 (6): 427-40. [PMID:9720765]

5. Schafer PH, Parton A, Capone L, Cedzik D, Brady H, Evans JF, Man HW, Muller GW, Stirling DI, Chopra R. (2014) Apremilast is a selective PDE4 inhibitor with regulatory effects on innate immunity. Cell. Signal., 26 (9): 2016-29. [PMID:24882690]

6. Tsai YF, Chu TC, Chang WY, Wu YC, Chang FR, Yang SC, Wu TY, Hsu YM, Chen CY, Chang SH et al.. (2017) 6-Hydroxy-5,7-dimethoxy-flavone suppresses the neutrophil respiratory burst via selective PDE4 inhibition to ameliorate acute lung injury. Free Radic. Biol. Med., 106: 379-392. [PMID:28263828]

7. Wang P, Myers JG, Wu P, Cheewatrakoolpong B, Egan RW, Billah MM. (1997) Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D. Biochem. Biophys. Res. Commun., 234 (2): 320-4. [PMID:9177268]

Contributors

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