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lanosterol synthase

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Target not currently curated in GtoImmuPdb

Target id: 2434

Nomenclature: lanosterol synthase

Family: Lanosterol biosynthesis pathway

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 732 21q22.3 LSS lanosterol synthase 6
Mouse - 733 10 39.1 cM Lss lanosterol synthase
Rat - 733 20p12 Lss lanosterol synthase
Previous and Unofficial Names Click here for help
OSC | oxidosqualene-lanosterol cyclase | 2,3-epoxysqualene-lanosterol cyclase | lanosterol synthase (2,3-oxidosqualene-lanosterol cyclase) | lanosterol synthase (2
Database Links Click here for help
Alphafold P48449 (Hs), Q8BLN5 (Mm), P48450 (Rn)
BRENDA 5.4.99.7
ChEMBL Target CHEMBL3593 (Hs), CHEMBL3262 (Rn)
Ensembl Gene ENSG00000160285 (Hs), ENSMUSG00000033105 (Mm), ENSRNOG00000054549 (Rn)
Entrez Gene 4047 (Hs), 16987 (Mm), 81681 (Rn)
Human Protein Atlas ENSG00000160285 (Hs)
KEGG Enzyme 5.4.99.7
KEGG Gene hsa:4047 (Hs), mmu:16987 (Mm), rno:81681 (Rn)
OMIM 600909 (Hs)
Pharos P48449 (Hs)
RefSeq Nucleotide NM_001145437 (Hs), NM_001145436 (Hs), NM_001001438 (Hs), NM_002340 (Hs)
RefSeq Protein NP_001001438 (Hs), NP_001138909 (Hs), NP_001138908 (Hs), NP_002331 (Hs)
SynPHARM 78769 (in complex with Ro 48-8071)
UniProtKB P48449 (Hs), Q8BLN5 (Mm), P48450 (Rn)
Wikipedia LSS (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human OSC in complex with Ro 48-8071
PDB Id:  1W6J
Ligand:  Ro 48-8071
Resolution:  2.2Å
Species:  Human
References:  5
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human OSC in complex with lanosterol
PDB Id:  1W6K
Ligand:  lanosterol   This ligand is endogenous
Resolution:  2.1Å
Species:  Human
References:  5
Enzyme Reaction Click here for help
EC Number: 5.4.99.7 (S)-2,3-epoxysqualene = lanosterol

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
compound 4 [PMID: 9003518] Small molecule or natural product Rn Inhibition 9.6 pIC50 3
⤷ pIC50 9.6 (IC50 2.6x10-10 M) [3]
29-methylidene-2,3-oxidosqualene Small molecule or natural product Rn Inhibition 9.5 pIC50 3
⤷ pIC50 9.5 (IC50 3x10-10 M) [3]
compound 4 [PMID: 22533316] Small molecule or natural product Hs Inhibition 8.5 pIC50 4
⤷ pIC50 8.5 (IC50 2.9x10-9 M) [4]
compound 8 [PMID: 22533316] Small molecule or natural product Hs Inhibition 8.3 pIC50 4
⤷ pIC50 8.3 (IC50 5x10-9 M) [4]
Ro 48-8071 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.2 pIC50 4
⤷ pIC50 8.2 (IC50 5.7x10-9 M) [4]
compound 6 [PMID: 22533316] Small molecule or natural product Hs Inhibition 8.1 pIC50 4
⤷ pIC50 8.1 (IC50 7.8x10-9 M) [4]
compound 1 [PMID: 22533316] Small molecule or natural product Hs Inhibition 8.1 pIC50 4
⤷ pIC50 8.1 (IC50 8x10-9 M) [4]
compound 5 [PMID: 22533316] Small molecule or natural product Hs Inhibition 8.0 pIC50 4
⤷ pIC50 8.0 (IC50 1x10-8 M) [4]
compound 9 [PMID: 22533316] Small molecule or natural product Hs Inhibition 7.9 pIC50 4
⤷ pIC50 7.9 (IC50 1.12x10-8 M) [4]
compound 7 [PMID: 22533316] Small molecule or natural product Hs Inhibition 7.9 pIC50 4
⤷ pIC50 7.9 (IC50 1.27x10-8 M) [4]
compound 3 [PMID: 22533316] Small molecule or natural product Hs Inhibition 7.8 pIC50 4
⤷ pIC50 7.8 (IC50 1.78x10-8 M) [4]
compound 10 [PMID: 22533316] Small molecule or natural product Hs Inhibition 7.5 pIC50 4
⤷ pIC50 7.5 (IC50 2.87x10-8 M) [4]
compound 3 [PMID: 9003518] Small molecule or natural product Rn Inhibition 7.3 pIC50 3
⤷ pIC50 7.3 (IC50 5x10-8 M) [3]
compound 1 [Gotteland et al., 1997] Small molecule or natural product Hs Inhibition 7.2 pIC50 1
⤷ pIC50 7.2 (IC50 7x10-8 M) [1]
compound 4b [Marquart et al., 1994] Small molecule or natural product Rn Inhibition 6.8 pIC50 2
⤷ pIC50 6.8 (IC50 1.7x10-7 M) [2]
compound 4a [Marquart et al., 1994] Small molecule or natural product Rn Inhibition 6.4 pIC50 2
⤷ pIC50 6.4 (IC50 4.3x10-7 M) [2]
View species-specific inhibitor tables

References

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1. Gotteland JP, Dax C, Halazy S. (1997) Design and synthesis of new potential photoaffinity labels for mammalian squalene epoxidase. Bioorg Med Chem Lett, 7 (9): 1153-1156. DOI: 10.1016/S0960-894X(97)00175-3

2. Marquart AL, Schatzman GL, Peet NP, Moore WR, Huber EW, Gallion SL, Angelastro MR. (1994) Inhibition of oxidosqualene cyclase by substituted quinolizidines. Bioorg Med Chem Lett, 4 (11): 1317-1318.

3. Stach D, Zheng YF, Perez AL, Oehlschlager AC, Abe I, Prestwich GD, Hartman PG. (1997) Synthesis and inhibition studies of sulfur-substituted squalene oxide analogues as mechanism-based inhibitors of 2,3-oxidosqualene-lanosterol cyclase. J Med Chem, 40 (2): 201-9. [PMID:9003518]

4. Staedler D, Chapuis-Bernasconi C, Dehmlow H, Fischer H, Juillerat-Jeanneret L, Aebi JD. (2012) Cytotoxic effects of combination of oxidosqualene cyclase inhibitors with atorvastatin in human cancer cells. J Med Chem, 55 (11): 4990-5002. [PMID:22533316]

5. Thoma R, Schulz-Gasch T, D'Arcy B, Benz J, Aebi J, Dehmlow H, Hennig M, Stihle M, Ruf A. (2004) Insight into steroid scaffold formation from the structure of human oxidosqualene cyclase. Nature, 432 (7013): 118-22. [PMID:15525992]

6. Young M, Chen H, Lalioti MD, Antonarakis SE. (1996) The human lanosterol synthase gene maps to chromosome 21q22.3. Hum Genet, 97 (5): 620-4. [PMID:8655142]

Contributors

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