Target Information

Target General Infomation
Target ID
T53585
Former ID
TTDS00195
Target Name
3-hydroxy-3-methylglutaryl-coenzyme A reductase
Gene Name
HMGCR
Synonyms
HMG coA reductase; HMG-CoA reductase; HMGCR
Target Type
Successful
Disease Arteriosclerosis [ICD9: 440; ICD10: I70]
Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Cardiovascular disease; Hyperlipidemia; Dyslipidemia [ICD10: I00-I99, E78]
Cardiovascular disorder [ICD10: I00-I99]
Chemotherapy or radiotherapy-induced mucositis [ICD9: 338, 528.0,780; ICD10: K12.3, R52, G89]
Dyslipidaemias [ICD9: 272; ICD10: E78]
Elevated CRP [ICD10: E78.0]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Hypercholesterolemia [ICD10: E78]
HBV infection [ICD9: 070.2-070.3; ICD10: B16, B18.0, B18.1]
Myocardial infarction; Cerebrovascular ischaemia [ICD9: 410, 434.91; ICD10: I21, I22, I61-I63]
Multiple myeloma [ICD9: 203; ICD10: C90]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Unspecified [ICD code not available]
Function
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
BioChemical Class
Short-chain dehydrogenases reductases
Target Validation
T53585
UniProt ID
P04035
EC Number
EC 1.1.1.34
Sequence
MLSRLFRMHGLFVASHPWEVIVGTVTLTICMMSMNMFTGNNKICGWNYECPKFEEDVLSS
DIIILTITRCIAILYIYFQFQNLRQLGSKYILGIAGLFTIFSSFVFSTVVIHFLDKELTG
LNEALPFFLLLIDLSRASTLAKFALSSNSQDEVRENIARGMAILGPTFTLDALVECLVIG
VGTMSGVRQLEIMCCFGCMSVLANYFVFMTFFPACVSLVLELSRESREGRPIWQLSHFAR
VLEEEENKPNPVTQRVKMIMSLGLVLVHAHSRWIADPSPQNSTADTSKVSLGLDENVSKR
IEPSVSLWQFYLSKMISMDIEQVITLSLALLLAVKYIFFEQTETESTLSLKNPITSPVVT
QKKVPDNCCRREPMLVRNNQKCDSVEEETGINRERKVEVIKPLVAETDTPNRATFVVGNS
SLLDTSSVLVTQEPEIELPREPRPNEECLQILGNAEKGAKFLSDAEIIQLVNAKHIPAYK
LETLMETHERGVSIRRQLLSKKLSEPSSLQYLPYRDYNYSLVMGACCENVIGYMPIPVGV
AGPLCLDEKEFQVPMATTEGCLVASTNRGCRAIGLGGGASSRVLADGMTRGPVVRLPRAC
DSAEVKAWLETSEGFAVIKEAFDSTSRFARLQKLHTSIAGRNLYIRFQSRSGDAMGMNMI
SKGTEKALSKLHEYFPEMQILAVSGNYCTDKKPAAINWIEGRGKSVVCEAVIPAKVVREV
LKTTTEAMIEVNINKNLVGSAMAGSIGGYNAHAANIVTAIYIACGQDAAQNVGSSNCITL
MEASGPTNEDLYISCTMPSIEIGTVGGGTNLLPQQACLQMLGVQGACKDNPGENARQLAR
IVCGTVMAGELSLMAALAAGHLVKSHMIHNRSKINLQDLQGACTKKTA
Drugs and Mode of Action
Drug(s) Atorvastatin Drug Info Approved Cardiovascular disease; Hyperlipidemia; Dyslipidemia [1]
Cerivastatin Drug Info Approved Hyperlipidaemia [2], [3]
Crestor/TriLipix Drug Info Approved Dyslipidaemias [1]
Fluvastatin Drug Info Approved Hypercholesterolemia [4], [5]
Lovastatin Drug Info Approved Hypercholesterolemia [4], [6]
PITAVASTATIN CALCIUM Drug Info Approved Dyslipidaemias [7], [1]
Pravastatin Drug Info Approved Hypercholesterolemia [8], [9]
Pravigard Drug Info Approved Myocardial infarction; Cerebrovascular ischaemia [10]
Rosuvastatin Drug Info Approved Hypercholesterolemia [11], [12]
Simvastatin Drug Info Approved Hypercholesterolemia [4], [13]
Simvistatin Drug Info Approved Hyperlipidaemia [10]
TOCOTRIENOL Drug Info Approved Hyperlipidaemia [14]
NK-104 Drug Info Phase 4 Discovery agent [15]
Premarin/Pravachol Drug Info Phase 3 Hyperlipidaemia [16]
Rosuvastatin Drug Info Phase 3 Elevated CRP [11], [12]
CRILVASTATIN Drug Info Phase 2 Hyperlipidaemia [17]
XZK-monascus Drug Info Phase 2 Hyperlipidaemia [18]
Statins Drug Info Phase 1/2 Multiple myeloma [4]
NCX-6560 Drug Info Phase 1 Cardiovascular disorder [16]
Simvistatin Drug Info Phase 1 HBV infection [10]
HMG-CoA reductase inhibitor Drug Info Preclinical Chemotherapy or radiotherapy-induced mucositis [19]
Dalvastatin Drug Info Discontinued in Phase 3 Hyperlipidaemia [20]
MK-0524B Drug Info Discontinued in Phase 3 Atherosclerosis [21]
Bervastatin Drug Info Discontinued in Phase 2 Thrombosis [22]
BMY-21950 Drug Info Discontinued in Phase 2 Hyperlipidaemia [23], [24]
GLENVASTATIN Drug Info Discontinued in Phase 2 Hyperlipidaemia [25]
RBx10558 Drug Info Discontinued in Phase 2 Hyperlipidaemia [26]
PF-3052334 Drug Info Discontinued in Phase 1 Atherosclerosis [27]
BMY-22089 Drug Info Terminated Hyperlipidaemia [28], [29]
CP-83101 Drug Info Terminated Arteriosclerosis [30]
GT-16-239 Drug Info Terminated Arteriosclerosis [31]
Mevastatin Drug Info Terminated Discovery agent [32], [33]
SQ-33600 Drug Info Terminated Hyperlipidaemia [34]
SR12813 Drug Info Terminated Arteriosclerosis [35], [36]
Inhibitor (E)-5-octadecen-7,9-diynoic acid Drug Info [37]
(E)-octadecan-9-ynoic acid Drug Info [37]
(R)-Mevalonate Drug Info [38]
(Z)-5-octadecen-7,9-diynoic acid Drug Info [37]
(Z)-7-octedecan-9-ynoic acid Drug Info [37]
1,4-Dithiothreitol Drug Info [38]
2'-Monophosphoadenosine 5'-Diphosphoribose Drug Info [38]
3-(1,3 dodecadiynyl)-6-oxiranebutanoic acid Drug Info [37]
3-Hydroxy-3-Methyl-Glutaric Acid Drug Info [38]
5-ketodihydromevinolin Drug Info [39]
6-hydroxy-7,9-octadecadiynoic acid Drug Info [37]
7,9-octadecadiynoic acid Drug Info [37]
7,9-tetradecadiynoic acid Drug Info [37]
9-octadecynoic acid Drug Info [37]
Adenosine-5'-Diphosphate Drug Info [40]
Atorvastatin Drug Info [41]
Bervastatin Drug Info [42]
BMY-21950 Drug Info [43], [1]
BMY-22089 Drug Info [43], [1]
BPL-001 Drug Info [44]
Brutieridin Drug Info [44]
Cerivastatin Drug Info [45]
Coenzyme A Drug Info [38]
compound 1 Drug Info [46]
compound 1 (Patel et al., 1991) Drug Info [44]
compound 11dd Drug Info [47]
compound 11ff Drug Info [47]
compound 11jj Drug Info [47]
compound 11nn Drug Info [47]
compound 13 Drug Info [48]
compound 13b Drug Info [49]
compound 13b Drug Info [50]
compound 13g Drug Info [50]
compound 16f Drug Info [51]
compound 17 Drug Info [52]
compound 17 Drug Info [53]
compound 18 Drug Info [54]
compound 18 Drug Info [55]
compound 18t Drug Info [56]
compound 1a Drug Info [50]
compound 1e Drug Info [50]
compound 1f Drug Info [50]
compound 2 (Dreyer et al., 1991) Drug Info [44]
compound 25 Drug Info [57]
compound 25d Drug Info [58]
compound 28 Drug Info [59]
compound 29 Drug Info [60]
compound 29 Drug Info [52]
compound 29 Drug Info [57]
compound 29f Drug Info [61]
compound 2c Drug Info [50]
compound 2d Drug Info [50]
compound 2f Drug Info [50]
compound 2g Drug Info [62]
compound 2t Drug Info [62]
compound 33 Drug Info [63]
compound 35 Drug Info [59]
compound 3h Drug Info [64]
compound 3j Drug Info [65]
compound 3k Drug Info [65]
compound 3q Drug Info [65]
compound 3u Drug Info [65]
compound 4 (Balasubramanian et al., 1992) Drug Info [44]
compound 41 Drug Info [66]
compound 42 Drug Info [66]
compound 4d Drug Info [62]
compound 4ff Drug Info [47]
compound 4i Drug Info [62]
compound 4p Drug Info [46]
compound 4rr Drug Info [47]
compound 50 Drug Info [67]
compound 5ab Drug Info [59]
compound 6a (Patil et al., 1989) Drug Info [44]
compound 6v Drug Info [46]
compound 7 Drug Info [68]
compound 74 Drug Info [47]
compound 8b Drug Info [69]
compound 9 Drug Info [70]
compound 9 Drug Info [71]
compound 9a (Patil et al., 1989) Drug Info [44]
CP-83101 Drug Info [72]
Crestor/TriLipix Drug Info [73]
CRILVASTATIN Drug Info [74], [1]
Dalvastatin Drug Info [75]
DFGYVAE Drug Info [76]
F(4-Fluoro)VAE Drug Info [77]
Fluvastatin Drug Info [41]
FPYVAE peptide Drug Info [76]
GFPDGG Drug Info [77]
GFPEGG Drug Info [77]
GFPTGG Drug Info [77]
GLENVASTATIN Drug Info [78], [1]
GLPDGG peptide Drug Info [76]
GLPTGG Drug Info [77]
HMG-CoA reductase inhibitor Drug Info [19]
Lovastatin Drug Info [79]
Meglutol Drug Info [80]
MK-0524B Drug Info [81], [82]
NCX-6560 Drug Info [16]
Nicotinamide-Adenine-Dinucleotide Drug Info [38]
NK-104 Drug Info [83]
o-hydroxyatorvastatin Drug Info [84]
PF-3052334 Drug Info [67]
PITAVASTATIN CALCIUM Drug Info [85]
Pravastatin Drug Info [86]
Pravigard Drug Info [10]
RBx10558 Drug Info [87]
Rosuvastatin Drug Info [88]
Simvastatin Drug Info [41]
Simvistatin Drug Info [10]
SQ-33600 Drug Info [89]
Statins Drug Info [90], [4]
TOCOTRIENOL Drug Info [91], [1]
Modulator GT-16-239 Drug Info [92]
MT-001 Drug Info [44]
NCX-1067 Drug Info [44]
Premarin/Pravachol Drug Info [16]
rawsonol Drug Info
SR12813 Drug Info
Statin Drug Info [44]
XZK-monascus Drug Info [93]
Antagonist Mevastatin Drug Info [94]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Superpathway of geranylgeranyldiphosphate biosynthesis I (via mevalonate)
Superpathway of cholesterol biosynthesis
Mevalonate pathway
KEGG Pathway Terpenoid backbone biosynthesis
Metabolic pathways
Biosynthesis of antibiotics
AMPK signaling pathway
Bile secretion
NetPath Pathway IL5 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
TSH Signaling Pathway
PANTHER Pathway Cholesterol biosynthesis
PathWhiz Pathway Steroid Biosynthesis
WikiPathways Statin Pathway
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Activation of Gene Expression by SREBP (SREBF)
SREBF and miR33 in cholesterol and lipid homeostasis
Integrated Breast Cancer Pathway
SREBP signalling
Cholesterol Biosynthesis
References
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REF 2(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2950).
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001906)
REF 4Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
REF 5(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2951).
REF 6(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2739).
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004764)
REF 8Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
REF 9(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2953).
REF 10Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
REF 11Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.
REF 12(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2954).
REF 13(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2955).
REF 14Vitamin E: tocopherols and tocotrienols as potential radiation countermeasures. J Radiat Res. 2013 Nov 1;54(6):973-88.
REF 15ClinicalTrials.gov (NCT01422382) Drug-Drug Interaction of Cardizem LA (Diltiazem Hydrochloride) on Pitavastatin. U.S. National Institutes of Health.
REF 16Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26.
REF 17Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002276)
REF 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036391)
REF 19Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.
REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001903)
REF 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023729)
REF 22Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002290)
REF 23(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2981).
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002314)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001230)
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025331)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025539)
REF 28(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2973).
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004222)
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000245)
REF 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011586)
REF 32(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3031).
REF 33Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002490)
REF 34Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002307)
REF 35(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2763).
REF 36Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002306)
REF 37Novel Acetylenic Acids from the Root Bark of Paramacrolobium caeruleum: Inhibitors of 3-Hydroxy-3-methyl-glutaryl Coenzyme A Reductase J. Nat. Prod. 52(1):153-161 (1989).
REF 38How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 39Total synthesis and biological evaluation of structural analogues of compactin and dihydromevinolin. J Med Chem. 1987 Oct;30(10):1858-73.
REF 40DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
REF 41Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64.
REF 42Effects of simvastatin, an HMG-CoA reductase inhibitor, in patients with hypertriglyceridemia. Clin Cardiol. 2003 Jan;26(1):18-24.
REF 43Selective inhibition of cholesterol synthesis in liver versus extrahepatic tissues by HMG-CoA reductase inhibitors. J Lipid Res. 1990 Jul;31(7):1271-82.
REF 44(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 639).
REF 45HMG-CoA reductase inhibitor has protective effects against stroke events in stroke-prone spontaneously hypertensive rats. Stroke. 2003 Jan;34(1):157-63.
REF 46Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety. J Med Chem. 1991 Sep;34(9):2804-15.
REF 47Synthesis and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids. J Med Chem. 1991 Oct;34(10):2962-83.
REF 48Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase. J Med Chem. 1991 Jan;34(1):463-6.
REF 49(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential. J Med Chem. 2008 May 8;51(9):2722-33.
REF 50Synthesis and biological activity of new HMG-CoA reductase inhibitors. 2. Derivatives of 7-(1H-pyrrol-3-yl)-substituted-3,5-dihydroxyhept-6(E)-enoic (-heptanoic) acids. J Med Chem. 1990 Jan;33(1):61-70.
REF 51Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1151-6. Epub 2007 Dec 5.
REF 52Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparativemolecular similarity indices analysis (CoMSIA). Bioorg Med Chem Lett. 2005 Feb 15;15(4):1027-32.
REF 533-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 5. 6-(Fluoren-9-yl)- and 6-(fluoren-9-ylidenyl)-3,5-dihydroxyhexanoic acids and their lactone derivatives. J Med Chem. 1986 May;29(5):852-5.
REF 543-Hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors. 7. Modification of the hexahydronaphthalene moiety of simvastatin: 5-oxygenated and 5-oxa derivatives. J Med Chem. 1991 Aug;34(8):2489-95.
REF 5532-Methyl-32-oxylanosterols: dual-action inhibitors of cholesterol biosynthesis. J Med Chem. 1993 Feb 5;36(3):410-6.
REF 56HMG-CoA reductase inhibitors: design, synthesis, and biological activity of tetrahydroindazole-substituted 3,5-dihydroxy-6-heptenoic acid sodium salts. J Med Chem. 1993 Nov 12;36(23):3674-85.
REF 57Inhibitors of cholesterol biosynthesis. 2. 1,3,5-trisubstituted [2-(tetrahydro-4-hydroxy-2-oxopyran-6-yl)ethyl]pyrazoles. J Med Chem. 1990 Jan;33(1):31-8.
REF 58Application of a 3,3-diphenylpentane skeleton as a multi-template for creation of HMG-CoA reductase inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4228-31.
REF 59Inhibitors of cholesterol biosynthesis. 1. 3,5-Dihydroxy-7-(N-imidazolyl)-6-heptenoates and -heptanoates, a novel series of HMG-CoA reductase inhibitors. J Med Chem. 1993 Nov 12;36(23):3646-57.
REF 60Synthesis and biological evaluation of dihydroeptastatin, a novel inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. J Med Chem. 1992 Sep 4;35(18):3388-93.
REF 61Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase. Bioorg Med Chem. 2007 Aug 15;15(16):5576-89. Epub 2007 May 17.
REF 62Synthesis and biological activity of new HMG-CoA reductase inhibitors. 1. Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids. J Med Chem. 1990 Jan;33(1):52-60.
REF 63Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4538-44. Epub 2007 Jun 6.
REF 64Inhibitors of cholesterol biosynthesis. 2. 3,5-Dihydroxy-7-(N-pyrrolyl)-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. J Med Chem. 1993 Nov 12;36(23):3658-62.
REF 65Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis. J Med Chem. 1990 Nov;33(11):2952-6.
REF 66Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4531-7. Epub 2007 Jun 6.
REF 67J Med Chem. 2008 Jan 10;51(1):31-45. Epub 2007 Dec 12.Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
REF 68Synthesis and biological evaluation of a monocyclic, fully functional analogue of compactin. J Med Chem. 1989 Jan;32(1):197-202.
REF 69Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2 H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors. J Med Chem. 1991 Jan;34(1):367-73.
REF 70Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted- pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones. J Med Chem. 1992 May 29;35(11):2095-103.
REF 71Synthesis and biological activity of bile acid-derived HMG-CoA reductase inhibitors. The role of 21-methyl in recognition of HMG-CoA reductase and the ileal bile acid transport system. J Med Chem. 1994 Sep 30;37(20):3240-6.
REF 72Efficacy, tissue distribution and biliary excretion of methyl (3R*,5S*)-(E)-3,5-dihydroxy-9,9-diphenyl-6,8-nonadienoate (CP-83101), a hepatoselective inhibitor of HMG-CoA reductase activity in the rat. Biochem Pharmacol. 1990 Sep 15;40(6):1281-93.
REF 73Clinical pipeline report, company report or official report of AstraZeneca (2009).
REF 74Differences in hypolipidaemic effects of two statins on Hep G2 cells or human hepatocytes in primary culture. Br J Pharmacol. 1996 Aug;118(7):1862-8.
REF 75RG 12561 (dalvastatin): a novel synthetic inhibitor of HMG-CoA reductase and cholesterol-lowering agent. Pharmacology. 1993;46(1):13-22.
REF 76Peptide fragmentation as an approach in modeling of an active peptide and designing a competitive inhibitory peptide for HMG-CoA reductase. Bioorg Med Chem. 2010 Jun 15;18(12):4300-9.
REF 77Bioorg Med Chem. 2008 Feb 1;16(3):1309-18. Epub 2007 Oct 23.Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone.
REF 78Bile acid derived HMG-CoA reductase inhibitors. Biochim Biophys Acta. 1994 Nov 29;1227(3):137-54.
REF 79Microarray and biochemical analysis of lovastatin-induced apoptosis of squamous cell carcinomas. Neoplasia. 2002 Jul-Aug;4(4):337-46.
REF 80Bioorg Med Chem Lett. 2005 Feb 15;15(4):989-94.Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase.
REF 81A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
REF 82Selective Targeting of CTNBB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs. PLoS One. 2015 May 27;10(5):e0125021. doi: 10.1371/journal.pone.0125021. eCollection 2015.
REF 83Cholesterol-lowering effect of NK-104, a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, in guinea pig model of hyperlipidemia. Arzneimittelforschung. 2001;51(3):197-203.
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