inosine monophosphate dehydrogenase 1

Target id: 2624

Nomenclature: inosine monophosphate dehydrogenase 1

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 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 599 7q31.3-q32 IMPDH1 inosine monophosphate dehydrogenase 1
Mouse - 514 6 A3 Impdh1 inosine monophosphate dehydrogenase 1
Rat - 514 4q22 Impdh1 inosine monophosphate dehydrogenase 1
Previous and Unofficial Names
LCA11 | IMP (inosine 5'-monophosphate) dehydrogenase 1 | inosine 5'-phosphate dehydrogenase 1
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
Orphanet
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 3
pIC50 7.7 (IC50 2x10-8 M) [3]
Description: Reference does not distinguish which enzyme isoform is assayed
ribavirin Hs Inhibition 5.6 – 6.0 pIC50 7
pIC50 5.6 – 6.0 (IC50 2.5x10-6 – 1x10-6 M) [7]
Description: In vitro inhibition of IMPDH (isoform not specified, human and mouse assayed)
mycophenolate mofetil Hs Inhibition - -
thioguanine Hs Inhibition - - 2,6
[2,6]
Inhibitor Comments
Further information regarding the use and effectiveness of mycophenolate mofetil is contained in these references:- [4-5]. In general there is little evidence identifying any isoform specificity in the action of the IMPDH inhibitors.
Clinically-Relevant Mutations and Pathophysiology
Disease:  Leber congenital amaurosis 11; LCA11
Synonyms: Amaurosis congenita of Leber
Leber congenital amaurosis [Orphanet: ORPHA65] [Disease Ontology: DOID:14791]
Disease Ontology: DOID:14791
OMIM: 613837
Orphanet: ORPHA65
References:  1
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human R105W 313C>T 1
Missense Human N198K 594T>G 1
Disease:  Retinitis pigmentosa 10; RP10
Synonyms: Retinitis pigmentosa [Orphanet: ORPHA791] [Disease Ontology: DOID:10584]
Disease Ontology: DOID:10584
OMIM: 180105
Orphanet: ORPHA791
References:  1
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human D226N 1

References

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1. Bowne SJ, Sullivan LS, Mortimer SE, Hedstrom L, Zhu J, Spellicy CJ, Gire AI, Hughbanks-Wheaton D, Birch DG, Lewis RA et al.. (2006) Spectrum and frequency of mutations in IMPDH1 associated with autosomal dominant retinitis pigmentosa and leber congenital amaurosis. Invest. Ophthalmol. Vis. Sci.47 (1): 34-42. [PMID:16384941]

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

3. 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]

4. 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]

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

6. 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]

7. 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

1.-.-.- Oxidoreductases: inosine monophosphate dehydrogenase 1. Last modified on 13/08/2015. Accessed on 17/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2624.