inosine monophosphate dehydrogenase 2

Target id: 2625

Nomenclature: inosine monophosphate dehydrogenase 2

Family: Nucleoside synthesis and metabolism, 1.-.-.- Oxidoreductases

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 inosine monophosphate dehydrogenase 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 514 3p21.2 IMPDH2 inosine monophosphate dehydrogenase 2
Mouse - 514 9 F2 Impdh2 inosine monophosphate dehydrogenase 2
Rat - 514 8q32 Impdh2 inosine monophosphate dehydrogenase 2
Previous and Unofficial Names
IMP (inosine 5'-monophosphate) dehydrogenase 2 | inosine 5'-phosphate dehydrogenase 2
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.1.1.205

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
mycophenolic acid Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 2x10-8 M) [2]
Description: Reference does not distinguish which enzyme isoform is assayed
ribavirin Hs Inhibition 5.6 – 6.0 pIC50 6
pIC50 5.6 – 6.0 (IC50 2.5x10-6 – 1x10-6 M) [6]
Description: In vitro inhibition of IMPDH (isoform not specified, human and mouse assayed)
mycophenolate mofetil Hs Inhibition - -
See Inhibitor Comment below
thioguanine Hs Inhibition - - 1,5
[1,5]
Inhibitor Comments
In general there is little evidence identifying any isoform specificity in the action of the IMPDH inhibitors.
Further information regarding the use and effectiveness of mycophenolate mofetil is contained in these references:- [3-4].

References

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1. Elgemeie GH. (2003) Thioguanine, mercaptopurine: their analogs and nucleosides as antimetabolites. Curr. Pharm. Des.9 (31): 2627-42. [PMID:14529546]

2. Nelson PH, Eugui E, Wang CC, Allison AC. (1990) Synthesis and immunosuppressive activity of some side-chain variants of mycophenolic acid. J. Med. Chem.33 (2): 833-8. [PMID:1967654]

3. Sanquer S, Maison P, Tomkiewicz C, Macquin-Mavier I, Legendre C, Barouki R, Lang P. (2008) Expression of inosine monophosphate dehydrogenase type I and type II after mycophenolate mofetil treatment: a 2-year follow-up in kidney transplantation. Clin. Pharmacol. Ther.83 (2): 328-35. [PMID:17713475]

4. Sollinger HW. (1996) From mice to man: the preclinical history of mycophenolate mofetil. Clin Transplant10 (1 Pt 2): 85-92. [PMID:8680054]

5. Vethe NT, Bremer S, Bergan S. (2008) IMP dehydrogenase basal activity in MOLT-4 human leukaemia cells is altered by mycophenolic acid and 6-thioguanosine. Scand. J. Clin. Lab. Invest.68 (4): 277-85. [PMID:18609073]

6. Wittine K, Stipković Babić M, Makuc D, Plavec J, Kraljević Pavelić S, Sedić M, Pavelić K, Leyssen P, Neyts J, Balzarini J et al.. (2012) Novel 1,2,4-triazole and imidazole derivatives of L-ascorbic and imino-ascorbic acid: synthesis, anti-HCV and antitumor activity evaluations. Bioorg. Med. Chem.20 (11): 3675-85. [PMID:22555152]

How to cite this page

Nucleoside synthesis and metabolism: inosine monophosphate dehydrogenase 2. Last modified on 13/08/2015. Accessed on 22/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2625.