lanosterol synthase | Lanosterol biosynthesis pathway | IUPHAR/BPS Guide to PHARMACOLOGY

lanosterol synthase

Target id: 2434

Nomenclature: lanosterol synthase

Family: Lanosterol biosynthesis pathway

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 lanosterol synthase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 732 21q22.3 LSS lanosterol synthase 6
Mouse - 733 10 39.10cM Lss lanosterol synthase
Rat - 733 20p12 Lss lanosterol synthase
Previous and Unofficial Names
OSC | oxidosqualene-lanosterol cyclase | 2,3-epoxysqualene-lanosterol cyclase | lanosterol synthase (2,3-oxidosqualene-lanosterol cyclase) | lanosterol synthase (2
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
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
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
Enzyme Reaction
EC Number: 5.4.99.7 (S)-2,3-epoxysqualene = lanosterol

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
compound 4 [PMID: 9003518] Rn Inhibition 9.6 pIC50 3
pIC50 9.6 (IC50 2.6x10-10 M) [3]
29-methylidene-2,3-oxidosqualene Rn Inhibition 9.5 pIC50 3
pIC50 9.5 (IC50 3x10-10 M) [3]
compound 4 [PMID: 22533316] Hs Inhibition 8.5 pIC50 4
pIC50 8.5 (IC50 2.9x10-9 M) [4]
compound 8 [PMID: 22533316] Hs Inhibition 8.3 pIC50 4
pIC50 8.3 (IC50 5x10-9 M) [4]
Ro 48-8071 Hs Inhibition 8.2 pIC50 4
pIC50 8.2 (IC50 5.7x10-9 M) [4]
compound 6 [PMID: 22533316] Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 7.8x10-9 M) [4]
compound 1 [PMID: 22533316] Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 8x10-9 M) [4]
compound 5 [PMID: 22533316] Hs Inhibition 8.0 pIC50 4
pIC50 8.0 (IC50 1x10-8 M) [4]
compound 9 [PMID: 22533316] Hs Inhibition 7.9 pIC50 4
pIC50 7.9 (IC50 1.12x10-8 M) [4]
compound 7 [PMID: 22533316] Hs Inhibition 7.9 pIC50 4
pIC50 7.9 (IC50 1.27x10-8 M) [4]
compound 3 [PMID: 22533316] Hs Inhibition 7.8 pIC50 4
pIC50 7.8 (IC50 1.78x10-8 M) [4]
compound 10 [PMID: 22533316] Hs Inhibition 7.5 pIC50 4
pIC50 7.5 (IC50 2.87x10-8 M) [4]
compound 3 [PMID: 9003518] Rn Inhibition 7.3 pIC50 3
pIC50 7.3 (IC50 5x10-8 M) [3]
compound 1 [Gotteland et al., 1997] Hs Inhibition 7.2 pIC50 1
pIC50 7.2 (IC50 7x10-8 M) [1]
compound 4b [Marquart et al., 1994] Rn Inhibition 6.8 pIC50 2
pIC50 6.8 (IC50 1.7x10-7 M) [2]
compound 4a [Marquart et al., 1994] 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.

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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How to cite this page

Helen E. Benson.
Lanosterol biosynthesis pathway: lanosterol synthase. Last modified on 08/01/2015. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2434.