phosphodiesterase 4D

Target id: 1303

Nomenclature: phosphodiesterase 4D

Abbreviated Name: PDE4D

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

   GtoImmuPdb view: OFF :     Currently no data for phosphodiesterase 4D in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - PDE4D phosphodiesterase 4D
Mouse - - Pde4d phosphodiesterase 4D, cAMP specific
Rat - - Pde4d phosphodiesterase 4D
Previous and Unofficial Names
phosphodiesterase E3 dunce homolog (Drosophila) | cAMP-specific 3',5'-cyclic phosphodiesterase 4D | phosphodiesterase 4D, cAMP specific | phosphodiesterase 4D, cAMP-specific
Database Links
BRENDA
CATH/Gene3D
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.1.4.17
Activator (Human)
PKA-mediated phosphorylation  [3]
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 Affinity Units Reference
CDP840 Hs Inhibition 8.1 pKi 5
pKi 8.1 (Ki 7.1x10-9 M) [5]
Description: Inhibition of [3H]-R-rolipram binding to recombinant human PDE4D3 isoenzyme
RS-25344 Hs Inhibition 8.4 pIC50 6
pIC50 8.4 [6]
apremilast Hs Inhibition 7.5 pIC50 7
pIC50 7.5 (IC50 3.3x10-8 M) [7]
Description: Potency against recombinant human PDE4D2 isoform in a TR-FRET assay.
OPA-15406 Hs Inhibition >7.3 pIC50 4
pIC50 >7.3 (IC50 <5x10-8 M) [4]
Description: Measuring inhibition of substrate hydrolysis by the PDE4D3 isoform.
rolipram Hs Inhibition 7.2 pIC50 8
pIC50 7.2 (IC50 6.31x10-8 M) [8]
Ro20-1724 Hs Inhibition 6.2 pIC50 8
pIC50 6.2 (IC50 6.31x10-7 M) [8]
CBS-3595 Hs Inhibition 6.1 pIC50 1
pIC50 6.1 (IC50 8x10-7 M) [1]
Description: Determined against the PDE4D3 splice variant.

References

Show »

1. Albrecht W, Unger A, Bauer SM, Laufer SA. (2017) Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. J. Med. Chem.60 (13): 5290-5305. [PMID:28613871]

2. Hanifin JM, Ellis CN, Frieden IJ, Fölster-Holst R, Stein Gold LF, Secci A, Smith AJ, Zhao C, Kornyeyeva E, Eichenfield LF. (2016) OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-controlled study. J. Am. Acad. Dermatol.75 (2): 297-305. [PMID:27189825]

3. Houslay MD, Adams DR. (2003) PDE4 cAMP phosphodiesterases: modular enzymes that orchestrate signalling cross-talk, desensitization and compartmentalization. Biochem. J.370 (Pt 1): 1-18. [PMID:12444918]

4. Okada M, Kato M, Sato N, Uno T, Kitagaki H, Haruta J, Hiyama H, Shibata T. (2007) Oxazole compound and pharmaceutical composition. Patent number: WO2007058338. Assignee: Otsuka Pharmaceutical Co., Ltd.. Priority date: 24/05/2007. Publication date: 15/11/2005.

5. 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]

6. 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]

7. 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]

8. 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]

How to cite this page

Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs): phosphodiesterase 4D. Last modified on 25/01/2018. Accessed on 24/04/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1303.