Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00466

Target Information
NameCAMP-specific 3',5'-cyclic phosphodiesterase 4B    
Type of targetResearch target    
SynonymsDPDE4    
PDE32    
Type 4 cyclic adenosine monophosphate phosphodiesterase (type 4 PDE)    
Type 4B cAMP phosphodiesterase    
DiseaseAsthma
[ICD9: 493   ICD10: J45]
[1]
Chronic lymphocytic leukemia
[ICD9: 204.1   ICD10: C91.1]
[2]
BioChemical ClassHydrolases acting on ester bonds    
EC NumberEC 3.1.4.17
PathwayPurine metabolism
UniProt IDQ07343
PDB Structure1F0J; 1JP1; 1JP2; 1RO6; 1RO9; 1ROR; 1TB5; 1XLX; 1XLZ; 1XM4; 1XM6; 1XMU; 1XMY; 1XN0; 1XOS; 1XOT; 1Y2H; 1Y2J; 2CHM; 2QYL; 3D3P; 3FRG; 3G45; 3GWT; 3HC8; 3HDZ; 3HMV; 3KKT; 3LY2; 3O0J; 3O56; 3O57; 3W5E.    
FunctionMay be involved in mediating central nervous system effects of therapeutic agents ranging from antidepressants to antiasthmatic and anti-inflammatory agents.    
SequenceMKKSRSVMTVMADDNVKDYFECSLSKSYSSSSNTLGIDLWRGRRCCSGNLQLPPLSQRQS ERARTPEGDGISRPTTLPLTTLPSIAITTVSQECFDVENGPSPGRSPLDPQASSSAGLVL HATFPGHSQRRESFLYRSDSDYDLSPKAMSRNSSLPSEQHGDDLIVTPFAQVLASLRSVR NNFTILTNLHGTSNKRSPAASQPPVSRVNPQEESYQKLAMETLEELDWCLDQLETIQTYR SVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEYISNTFLDKQNDVEIPSPTQKDREKKK KQQLMTQISGVKKLMHSSSLNNTSISRFGVNTENEDHLAKELEDLNKWGLNIFNVAGYSH NRPLTCIMYAIFQERDLLKTFRISSDTFITYMMTLEDHYHSDVAYHNSLHAADVAQSTHV LLSTPALDAVFTDLEILAAIFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHL AVGFKLLQEEHCDIFMNLTKKQRQTLRKMVIDMVLATDMSKHMSLLADLKTMVETKKVTS SGVLLLDNYTDRIQVLRNMVHCADLSNPTKSLELYRQWTDRIMEEFFQQGDKERERGMEI SPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVQPDAQDILDTLEDNRNWYQSMIPQSP SPPLDEQNRDCQGLMEKFQFELTLDEEDSEGPEKEGEGHSYFSSTKTLCVIDPENRDSLG ETDIDIATEDKSPVDT
Target ValidationClick to Find Target Validation Information.    
Inhibitor (-)-ROLIPRAM[3]
(R)-Mesopram[4]
(R)-Rolipram[5]
(R)-Rolipram[4]
(S)-Rolipram[5]
(S)-Rolipram[4]
3- (2-Bromophenyl)-2-thioxo-[6]
3-Isobutyl-1-methyl-3,7-dihydro-purine-2,6-dione[7]
8- (3-Nitro-phenyl)-6-phenyl-[1,7]naphthyridine[8]
8-Bromo-Adenosine-5'-Monophosphate[9]
Benzyl- (2-imidazol-1-yl-quinazolin-4-yl)-amine[10]
Benzyl- (2-phenyl-quinazolin-4-yl)-amine[10]
Benzyl- (2-pyridin-3-yl-quinazolin-4-yl)-amine[10]
Benzyl- (2-pyridin-4-yl-quinazolin-4-yl)-amine[10]
Benzyl- (2-thiophen-2-yl-quinazolin-4-yl)-amine[10]
CC-1088[11]
CDP840[12]
CI-1018[13]
CI-1044[14]
DENBUFYLLINE[15]
Filaminast[4]
KURAIDIN[16]
KURARINOL[16]
L-454560[17]
L-869298[18]
NITRAQUAZONE[19]
Piclamilast[20]
RO-201724[21]
ROLIPRAM[22]
RS-14491[22]
S,S- (2-Hydroxyethyl)Thiocysteine[4]
SCH-351591[23]
SCH-365351[24]
SOPHOFLAVESCENOL[16]
UCB-101333-3[25]
[R]-Mesopram[26]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Phosphodiesterase 4 inhibitors and the treatment of asthma: where are we now and where do we go from here? Drugs. 2000 Feb;59(2):193-212. To Reference
Ref 2Type 4 cyclic adenosine monophosphate phosphodiesterase as a therapeutic target in chronic lymphocytic leukemia. Blood. 1998 Oct 1;92(7):2484-94. To Reference
Ref 3J Med Chem. 2007 Jan 25;50(2):344-9.SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase. To Reference
Ref 4Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 5PDE4 inhibitors roflumilast and rolipram augment PGE2 inhibition of TGF-{beta}1-stimulated fibroblasts. Am J Physiol Lung Cell Mol Physiol. 2009 Jun;296(6):L959-69. Epub 2009 Mar 20. To Reference
Ref 6Eur J Med Chem. 2008 Jul;43(7):1349-59. Epub 2007 Dec 21.CODES, a novel procedure for ligand-based virtual screening: PDE7 inhibitors as an application example. To Reference
Ref 7J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. To Reference
Ref 8J Med Chem. 2000 Feb 24;43(4):675-82.Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors. To Reference
Ref 9Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 10J Med Chem. 1995 Sep 1;38(18):3547-57.Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities. To Reference
Ref 11Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74.Thalidomide analogs and PDE4 inhibition. To Reference
Ref 12Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6. Epub 2005 Sep 15.Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. To Reference
Ref 13Bioorg Med Chem Lett. 2004 Jun 21;14(12):3303-6.New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors. To Reference
Ref 14J Med Chem. 2000 Dec 14;43(25):4850-67.Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors. To Reference
Ref 15J Med Chem. 2002 May 23;45(11):2342-5.Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. To Reference
Ref 16Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. To Reference
Ref 17Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5. Epub 2010 Jul 21.The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. To Reference
Ref 18J Med Chem. 2006 Mar 23;49(6):1867-73.Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. To Reference
Ref 19Bioorg Med Chem Lett. 2000 Dec 4;10(23):2661-4.Synthesis and biological evaluation of 2,5-dihydropyrazol. To Reference
Ref 20Beeh KM, Beier J, Lerch C, Schulz AK, Buhl R: Effects of piclamilast, a selective phosphodiesterase-4 inhibitor, on oxidative burst of sputum cells from mild asthmatics and stable COPD patients. Lung. 2004;182(6):369-77. To Reference
Ref 21J Med Chem. 1991 Jan;34(1):291-8.Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones. To Reference
Ref 22J Med Chem. 1997 May 9;40(10):1417-21.Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors. To Reference
Ref 23Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.Synthesis and profile of SCH351591, a novel PDE4 inhibitor. To Reference
Ref 24Bioorg Med Chem Lett. 2002 Jun 17;12(12):1617-9.8-Methoxyquinolines as PDE4 inhibitors. To Reference
Ref 25Bioorg Med Chem Lett. 2006 Apr 1;16(7):1834-9. Epub 2006 Jan 24.First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives. To Reference
Ref 26Bioorg Med Chem. 2010 Mar 15;18(6):2204-18. Epub 2010 Feb 8.In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. To Reference



 

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