isopentenyl-diphosphate Δ-isomerase 1 | Lanosterol biosynthesis pathway | IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

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isopentenyl-diphosphate Δ-isomerase 1

Target id: 646

Nomenclature: isopentenyl-diphosphate Δ-isomerase 1

Family: Lanosterol biosynthesis pathway

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 227 10p15.3 IDI1 isopentenyl-diphosphate delta isomerase 1 3
Mouse - 227 13 A1; 13 Idi1 isopentenyl-diphosphate delta isomerase
Rat - 227 17q12.1 Idi1 isopentenyl-diphosphate delta isomerase 1
Previous and Unofficial Names
IPPI1 | methylbutenylpyrophosphate isomerase | IPP isomerase 1 | isopentenyl pyrophosphate isomerase 1
Database Links
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  The crystal structure of human isopentenyl diphophate isomerase
Resolution:  1.7Å
Species:  Human
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  Human isopentenyl diphophate isomerase complexed with substrate analog
Ligand:  dimethylallyl diphosphate   This ligand is endogenous
Resolution:  1.93Å
Species:  Human
References:  6
Enzyme Reaction
EC Number: Isopentenyl diphosphate = dimethylallyl diphosphate
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
isopentenyl diphosphate Hs Km 3.3x10-5 M pKm 4.5 Recombinant human protein expressed in E coli and purified pH 7, 37°C Km value obtained using the Grafit curve-fitting programme. 10-500 µM IPP; 20mM MgCl2 2
isopentenyl diphosphate Hs Vmax 4.1 µmol/min/mg Recombinant human protein expressed in E coli and purified. 0.02µg of enzyme used in assay. pH 7, 37°C Vmax value obtained using the Grafit curve-fitting programme. 10-500 µM IPP; 20mM MgCl2 2
Cofactor Species Comments Reference
Mg2+ Human Enzyme activity increases with increasing Mg2+ up to 20mM. 2
Mn2+ Human Activity increases up to a concentration of 100 micromolar Mn2+ then sharply decreases. 2,5

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Ligand Sp. Action Value Parameter Reference
NE21650 Hs Inhibition ~4.2 pIC50 4
pIC50 ~4.2 (IC50 ~7x10-5 M) [4]
Description: in vitro inhibition assay
Conditions: Recombinant enzyme expressed and partially purified. pH 7.0, 37°C; 10mM MgCl2
Tissue Distribution Comments
Ubiquitously expressed [1].


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1. Breitling R, Laubner D, Clizbe D, Adamski J, Krisans SK. (2003) Isopentenyl-diphosphate isomerases in human and mouse: evolutionary analysis of a mammalian gene duplication. J. Mol. Evol., 57 (3): 282-91. [PMID:14629038]

2. Hahn FM, Xuan JW, Chambers AF, Poulter CD. (1996) Human isopentenyl diphosphate: dimethylallyl diphosphate isomerase: overproduction, purification, and characterization. Arch. Biochem. Biophys., 332 (1): 30-4. [PMID:8806705]

3. Kato T, Emi M, Sato H, Arawaka S, Wada M, Kawanami T, Katagiri T, Tsuburaya K, Toyoshima I, Tanaka F et al.. (2010) Segmental copy-number gain within the region of isopentenyl diphosphate isomerase genes in sporadic amyotrophic lateral sclerosis. Biochem. Biophys. Res. Commun., 402 (2): 438-42. [PMID:20955688]

4. Thompson K, Dunford JE, Ebetino FH, Rogers MJ. (2002) Identification of a bisphosphonate that inhibits isopentenyl diphosphate isomerase and farnesyl diphosphate synthase. Biochem. Biophys. Res. Commun., 290 (2): 869-73. [PMID:11785983]

5. Zhang C, Liu L, Xu H, Wei Z, Wang Y, Lin Y, Gong W. (2007) Crystal structures of human IPP isomerase: new insights into the catalytic mechanism. J. Mol. Biol., 366 (5): 1437-46. [PMID:17137593]

6. Zheng W, Sun F, Bartlam M, Li X, Li R, Rao Z. (2007) The crystal structure of human isopentenyl diphosphate isomerase at 1.7 A resolution reveals its catalytic mechanism in isoprenoid biosynthesis. J. Mol. Biol., 366 (5): 1447-58. [PMID:17250851]


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