Skip to main content
. 2019 Nov 11;176(Suppl 1):S297–S396. doi: 10.1111/bph.14752
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=639
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:5006, http://www.uniprot.org/uniprot/P04035
EC number http://www.genome.jp/dbget‐bin/www_bget?ec:1.1.1.34: http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3040 + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3041 ‐>http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3042 + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3044 + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3045 Reaction mechanism:: First step: (S)‐3‐hydroxy‐3‐methylglutaryl‐CoA + NADPH ‐> mevaldyl‐CoA + NADP+ Second step: mevaldyl‐CoA + H2O ‐>(R)‐mevalonate + NADP+
Inhibitors http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2739 (Competitive) (pK i 9.2) [http://www.ncbi.nlm.nih.gov/pubmed/6933445?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2954 (Competitive) (pIC50 8.3) [http://www.ncbi.nlm.nih.gov/pubmed/11349148?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2950 (Competitive) (pK i 8.2) [http://www.ncbi.nlm.nih.gov/pubmed/16128575?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2949 (Competitive) (pIC50 8.1) [http://www.ncbi.nlm.nih.gov/pubmed/11349148?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2950 (Competitive) (pIC50 8) [http://www.ncbi.nlm.nih.gov/pubmed/15686906?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2955 (Competitive) (pIC50 8) [http://www.ncbi.nlm.nih.gov/pubmed/11349148?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2951 (Competitive) (pIC50 7.6) [http://www.ncbi.nlm.nih.gov/pubmed/11349148?dopt=AbstractPlus]
Comments HMGCoA reductase is associated with intracellular membranes; enzymatic activity is inhibited by phosphorylation by AMP‐activated kinase. The enzymatic reaction is a three‐step reaction involving the intermediate generation of mevaldehyde‐CoA and mevaldehyde.