Therapeutic Targets Database
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TTD Target ID: TTDS00063

Target Information
NameInosine-5'-monophosphate dehydrogenase 2    
Type of targetSuccessful target    
SynonymsIMP dehydrogenase 2    
IMPD 2    
IMPDH-II    
DiseaseLeukemia, unspecified    [1]
Drug(s)Mycophenolate mofetilApprovedOrgan transplant rejection[2][3]
Mycophenolic acidApprovedOrgan transplant rejection[2]
Mycophenolate mofetilPhase IIIPemphigus vulgaris[4]
BioChemical ClassOxidoreductases acting on the CH-OH group of donors    
EC NumberEC 1.1.1.205
PathwayDrug metabolism - other enzymes
Metabolic pathways
Purine metabolism
UniProt IDP12268
PDB Structure1B3O; 1NF7; 1NFB.    
FunctionImp is the rate limiting enzyme in the de novo synthesis of guanine nucleotides and therefore is involved in the regulation of cell growth. It may also have a role in the development of malignancy and the growth progression of some tumors.    
SequenceMADYLISGGTSYVPDDGLTAQQLFNCGDGLTYNDFLILPGYIDFTADQVDLTSALTKKIT LKTPLVSSPMDTVTEAGMAIAMALTGGIGFIHHNCTPEFQANEVRKVKKYEQGFITDPVV LSPKDRVRDVFEAKARHGFCGIPITDTGRMGSRLVGIISSRDIDFLKEEEHDCFLEEIMT KREDLVVAPAGITLKEANEILQRSKKGKLPIVNEDDELVAIIARTDLKKNRDYPLASKDA KKQLLCGAAIGTHEDDKYRLDLLAQAGVDVVVLDSSQGNSIFQINMIKYIKDKYPNLQVI GGNVVTAAQAKNLIDAGVDALRVGMGSGSICITQEVLACGRPQATAVYKVSEYARRFGVP VIADGGIQNVGHIAKALALGASTVMMGSLLAATTEAPGEYFFSDGIRLKKYRGMGSLDAM DKHLSSQNRYFSEADKIKVAQGVSGAVQDKGSIHKFVPYLIAGIQHSCQDIGAKSLTQVR AMMYSGELKFEKRTSSAQVEGGVHSLHSYEKRLF
Target ValidationClick to Find Target Validation Information.    
Inhibitor1- (3-cyano-1-methyl-1H-indol-6-yl)-3-phenylurea[5]
1-methoxy-3- (3-[5]
1-methyl-1H-indole-3-carbaldehyde[6]
1-methyl-1H-indole-3-carbonitrile[5]
1-methyl-1H-indole-3-carboxamide[6]
2-Benzyl-6-methoxy-5-oxazol-5-yl-1H-indole[7]
2-methyl-3- (pyridin-4-yl)-1H-indol-6-amine[6]
2-methyl-3- (pyridin-4-yl)-1H-indole[6]
3- (3-cyano-1H-indol-6-yl)-1-methyl-1-phenylurea[5]
3- (furan-3-yl)-1-methyl-1H-indole[6]
3- (furan-3-yl)-1H-indole[6]
3- (pyridin-4-yl)-1H-indol-6-amine[6]
3- (pyridin-4-yl)-1H-indol-7-amine[6]
3- (pyridin-4-yl)-1H-indole[5]
3- (thiophen-3-yl)-1H-indol-6-amine[6]
3-methoxy-4- (oxazol-5-yl)aniline[6]
6-Chloropurine Riboside, 5'-Monophosphate[8]
6-Methoxy-5-oxazol-5-yl-2-phenyl-1H-indole[7]
6-bromo-1-methyl-3- (pyridin-4-yl)-1H-indole[6]
6-bromo-3- (pyridin-4-yl)-1H-indole[6]
6-phenyl-3- (pyridin-4-yl)-1H-indole[5]
C2-MAD[9]
C4-MAD[9]
Inosinic Acid[8]
Mycophenolate mofetil[2][3]
Mycophenolate mofetil[4]
Mycophenolic acid[2]
Mycophenolic bis (sulfonamide)[10]
N-benzyl-9-oxo-9,10-dihydroacridine-3-carboxamide[11]
Nicotinamide-Adenine-Dinucleotide[8]
Selenazole-4-Carboxyamide-Adenine Dinucleotide[8]
ethyl 3- (pyridin-4-yl)-1H-indole-6-carboxylate[5]
mycophenolic hydroxamic acid[12]
tiazofurin adenine dinucleotide[13]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Specific inhibition of type II inosine monophosphate dehydrogenase activity of Tmolt4 T cell human leukaemia cells by 3-methoxy and di-benzohydroxamic acids, maleic hydrazide and malonic acids. J Pharm Pharmacol. 2001 May;53(5):749-55. To Reference
Ref 2Clin Chem. 2009 May;55(5):986-93. Epub 2009 Mar 19.Effect of mycophenolate acyl-glucuronide on human recombinant type 2 inosine monophosphate dehydrogenase. To Reference
Ref 3Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 4Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 5Bioorg Med Chem Lett. 2006 May 1;16(9):2539-42. Epub 2006 Feb 17.Novel indole inhibitors of IMPDH from fragments: synthesis and initial structure-activity relationships. To Reference
Ref 6Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. Epub 2006 Feb 17.Low molecular weight indole fragments as IMPDH inhibitors. To Reference
Ref 7Bioorg Med Chem Lett. 2003 Apr 7;13(7):1273-6.Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3. To Reference
Ref 8Overington 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 9Novel mycophenolic adenine bis(phosphonate) analogues as potential differentiation agents against human leukemia. J Med Chem. 2002 Jan 31;45(3):703-12. To Reference
Ref 10Bioorg Med Chem. 2008 Aug 1;16(15):7462-9. Epub 2008 Jun 10.Bis(sulfonamide) isosters of mycophenolic adenine dinucleotide analogues: inhibition of inosine monophosphate dehydrogenase. To Reference
Ref 11J Med Chem. 2007 Jul 26;50(15):3730-42. Epub 2007 Jun 22.Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419). To Reference
Ref 12Bioorg Med Chem. 2010 Nov 15;18(22):8106-11. Epub 2010 Sep 18.Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase and differentiation induction of K562 cells among the mycophenolic acid derivatives. To Reference
Ref 13J Med Chem. 2007 Dec 27;50(26):6685-91. Epub 2007 Nov 27.Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment. To Reference



 

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