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inosine monophosphate dehydrogenase 1

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Target not currently curated in GtoImmuPdb

Target id: 2624

Nomenclature: inosine monophosphate dehydrogenase 1

Abbreviated Name: IMPDH1

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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 514 7q32.1 IMPDH1 inosine monophosphate dehydrogenase 1
Mouse - 514 6 A3.3 Impdh1 inosine monophosphate dehydrogenase 1
Rat - 514 4q22 Impdh1 inosine monophosphate dehydrogenase 1
Previous and Unofficial Names Click here for help
LCA11 | IMP (inosine 5'-monophosphate) dehydrogenase 1 | inosine 5'-phosphate dehydrogenase 1
Database Links Click here for help
Alphafold P20839 (Hs), P50096 (Mm), D3ZLZ7 (Rn)
BRENDA 1.1.1.205
CATH/Gene3D 3.20.20.70
ChEMBL Target CHEMBL1822 (Hs)
DrugBank Target P20839 (Hs)
Ensembl Gene ENSG00000106348 (Hs), ENSMUSG00000003500 (Mm), ENSRNOG00000020032 (Rn)
Entrez Gene 3614 (Hs), 23917 (Mm), 362329 (Rn)
Human Protein Atlas ENSG00000106348 (Hs)
KEGG Enzyme 1.1.1.205
KEGG Gene hsa:3614 (Hs), mmu:23917 (Mm), rno:362329 (Rn)
OMIM 146690 (Hs)
Orphanet ORPHA122649 (Hs)
Pharos P20839 (Hs)
RefSeq Nucleotide NM_000883 (Hs), NM_011829 (Mm), NM_001108619 (Rn)
RefSeq Protein NP_000874 (Hs), NP_035959 (Mm), NP_001102089 (Rn)
UniProtKB P20839 (Hs), P50096 (Mm), D3ZLZ7 (Rn)
Wikipedia IMPDH1 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.1.1.205

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
mycophenolic acid Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure 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 Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure 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 Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition - -
⤷
thioguanine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure 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.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cellular signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
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 Transplant, 10 (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

Nucleoside synthesis and metabolism: inosine monophosphate dehydrogenase 1. Last modified on 28/11/2018. Accessed on 09/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2624.