Target Information
Target General Infomation | |||||
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Target ID |
T53585
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Former ID |
TTDS00195
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Target Name |
3-hydroxy-3-methylglutaryl-coenzyme A reductase
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Gene Name |
HMGCR
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Synonyms |
HMG coA reductase; HMG-CoA reductase; HMGCR
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Target Type |
Successful
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Disease | Atherosclerosis [ICD9: 414.0, 440; ICD10: I70] | ||||
Arteriosclerosis [ICD9: 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] | |||||
HBV infection [ICD9: 070.2-070.3; ICD10: B16, B18.0, B18.1] | |||||
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78] | |||||
Hypercholesterolemia [ICD10: E78] | |||||
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.
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BioChemical Class |
Short-chain dehydrogenases reductases
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Target Validation |
T53585
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UniProt ID | |||||
EC Number |
EC 1.1.1.34
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Sequence |
MLSRLFRMHGLFVASHPWEVIVGTVTLTICMMSMNMFTGNNKICGWNYECPKFEEDVLSS
DIIILTITRCIAILYIYFQFQNLRQLGSKYILGIAGLFTIFSSFVFSTVVIHFLDKELTG LNEALPFFLLLIDLSRASTLAKFALSSNSQDEVRENIARGMAILGPTFTLDALVECLVIG VGTMSGVRQLEIMCCFGCMSVLANYFVFMTFFPACVSLVLELSRESREGRPIWQLSHFAR VLEEEENKPNPVTQRVKMIMSLGLVLVHAHSRWIADPSPQNSTADTSKVSLGLDENVSKR IEPSVSLWQFYLSKMISMDIEQVITLSLALLLAVKYIFFEQTETESTLSLKNPITSPVVT QKKVPDNCCRREPMLVRNNQKCDSVEEETGINRERKVEVIKPLVAETDTPNRATFVVGNS SLLDTSSVLVTQEPEIELPREPRPNEECLQILGNAEKGAKFLSDAEIIQLVNAKHIPAYK LETLMETHERGVSIRRQLLSKKLSEPSSLQYLPYRDYNYSLVMGACCENVIGYMPIPVGV AGPLCLDEKEFQVPMATTEGCLVASTNRGCRAIGLGGGASSRVLADGMTRGPVVRLPRAC DSAEVKAWLETSEGFAVIKEAFDSTSRFARLQKLHTSIAGRNLYIRFQSRSGDAMGMNMI SKGTEKALSKLHEYFPEMQILAVSGNYCTDKKPAAINWIEGRGKSVVCEAVIPAKVVREV LKTTTEAMIEVNINKNLVGSAMAGSIGGYNAHAANIVTAIYIACGQDAAQNVGSSNCITL MEASGPTNEDLYISCTMPSIEIGTVGGGTNLLPQQACLQMLGVQGACKDNPGENARQLAR IVCGTVMAGELSLMAALAAGHLVKSHMIHNRSKINLQDLQGACTKKTA |
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Drugs and Mode of Action | |||||
Drug(s) | Atorvastatin | Drug Info | Approved | Cardiovascular disease; Hyperlipidemia; Dyslipidemia | [551871] |
Cerivastatin | Drug Info | Approved | Hyperlipidaemia | [539962], [545021] | |
Crestor/TriLipix | Drug Info | Approved | Dyslipidaemias | [551871] | |
Fluvastatin | Drug Info | Approved | Hypercholesterolemia | [537114], [539963] | |
Lovastatin | Drug Info | Approved | Hypercholesterolemia | [537114], [539783] | |
PITAVASTATIN CALCIUM | Drug Info | Approved | Dyslipidaemias | [545795], [551871] | |
Pravastatin | Drug Info | Approved | Hypercholesterolemia | [536361], [539964] | |
Pravigard | Drug Info | Approved | Myocardial infarction; Cerebrovascular ischaemia | [536186] | |
Rosuvastatin | Drug Info | Approved | Hypercholesterolemia | [536372], [539965] | |
Simvastatin | Drug Info | Approved | Hypercholesterolemia | [537114], [539966] | |
Simvistatin | Drug Info | Approved | Hyperlipidaemia | [536186] | |
TOCOTRIENOL | Drug Info | Approved | Hyperlipidaemia | [532347] | |
NK-104 | Drug Info | Phase 4 | Discovery agent | [523598] | |
Premarin/Pravachol | Drug Info | Phase 3 | Hyperlipidaemia | [535747] | |
Rosuvastatin | Drug Info | Phase 3 | Elevated CRP | [536372], [539965] | |
CRILVASTATIN | Drug Info | Phase 2 | Hyperlipidaemia | [545138] | |
XZK-monascus | Drug Info | Phase 2 | Hyperlipidaemia | [549393] | |
Statins | Drug Info | Phase 1/2 | Multiple myeloma | [537114] | |
NCX-6560 | Drug Info | Phase 1 | Cardiovascular disorder | [535747] | |
Simvistatin | Drug Info | Phase 1 | HBV infection | [536186] | |
HMG-CoA reductase inhibitor | Drug Info | Preclinical | Chemotherapy or radiotherapy-induced mucositis | [536838] | |
Dalvastatin | Drug Info | Discontinued in Phase 3 | Hyperlipidaemia | [545019] | |
MK-0524B | Drug Info | Discontinued in Phase 3 | Atherosclerosis | [548247] | |
Bervastatin | Drug Info | Discontinued in Phase 2 | Thrombosis | [545145] | |
BMY-21950 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [539994], [545157] | |
GLENVASTATIN | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [544823] | |
RBx10558 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [548403] | |
PF-3052334 | Drug Info | Discontinued in Phase 1 | Atherosclerosis | [548433] | |
BMY-22089 | Drug Info | Terminated | Hyperlipidaemia | [539985], [545692] | |
CP-83101 | Drug Info | Terminated | Arteriosclerosis | [544592] | |
GT-16-239 | Drug Info | Terminated | Arteriosclerosis | [546960] | |
Mevastatin | Drug Info | Terminated | Discovery agent | [540037], [545220] | |
SQ-33600 | Drug Info | Terminated | Hyperlipidaemia | [545154] | |
SR12813 | Drug Info | Terminated | Arteriosclerosis | [539809], [545153] | |
Inhibitor | (E)-5-octadecen-7,9-diynoic acid | Drug Info | [551349] | ||
(E)-octadecan-9-ynoic acid | Drug Info | [551349] | |||
(R)-Mevalonate | Drug Info | [551393] | |||
(Z)-5-octadecen-7,9-diynoic acid | Drug Info | [551349] | |||
(Z)-7-octedecan-9-ynoic acid | Drug Info | [551349] | |||
1,4-Dithiothreitol | Drug Info | [551393] | |||
2'-Monophosphoadenosine 5'-Diphosphoribose | Drug Info | [551393] | |||
3-(1,3 dodecadiynyl)-6-oxiranebutanoic acid | Drug Info | [551349] | |||
3-Hydroxy-3-Methyl-Glutaric Acid | Drug Info | [551393] | |||
5-ketodihydromevinolin | Drug Info | [533473] | |||
6-hydroxy-7,9-octadecadiynoic acid | Drug Info | [551349] | |||
7,9-octadecadiynoic acid | Drug Info | [551349] | |||
7,9-tetradecadiynoic acid | Drug Info | [551349] | |||
9-octadecynoic acid | Drug Info | [551349] | |||
Adenosine-5'-Diphosphate | Drug Info | [551391] | |||
Atorvastatin | Drug Info | [535246] | |||
Bervastatin | Drug Info | [526518] | |||
BMY-21950 | Drug Info | [532472], [551871] | |||
BMY-22089 | Drug Info | [532472], [551871] | |||
BPL-001 | Drug Info | [543905] | |||
Brutieridin | Drug Info | [543905] | |||
Cerivastatin | Drug Info | [535663] | |||
Coenzyme A | Drug Info | [551393] | |||
compound 1 | Drug Info | [529773] | |||
compound 1 (Patel et al., 1991) | Drug Info | [543905] | |||
compound 11dd | Drug Info | [528092] | |||
compound 11ff | Drug Info | [528092] | |||
compound 11jj | Drug Info | [528092] | |||
compound 11nn | Drug Info | [528092] | |||
compound 13 | Drug Info | [530524] | |||
compound 13b | Drug Info | [529423] | |||
compound 13b | Drug Info | [531456] | |||
compound 13g | Drug Info | [531456] | |||
compound 16f | Drug Info | [529232] | |||
compound 17 | Drug Info | [527410] | |||
compound 17 | Drug Info | [533477] | |||
compound 18 | Drug Info | [529660] | |||
compound 18 | Drug Info | [534034] | |||
compound 18t | Drug Info | [533953] | |||
compound 1a | Drug Info | [531456] | |||
compound 1e | Drug Info | [531456] | |||
compound 1f | Drug Info | [531456] | |||
compound 2 (Dreyer et al., 1991) | Drug Info | [543905] | |||
compound 25 | Drug Info | [532035] | |||
compound 25d | Drug Info | [530191] | |||
compound 28 | Drug Info | [533951] | |||
compound 29 | Drug Info | [532035] | |||
compound 29 | Drug Info | [527151] | |||
compound 29 | Drug Info | [527410] | |||
compound 29f | Drug Info | [528887] | |||
compound 2c | Drug Info | [531456] | |||
compound 2d | Drug Info | [531456] | |||
compound 2f | Drug Info | [531456] | |||
compound 2g | Drug Info | [532037] | |||
compound 2t | Drug Info | [532037] | |||
compound 33 | Drug Info | [528899] | |||
compound 35 | Drug Info | [533951] | |||
compound 3h | Drug Info | [533952] | |||
compound 3j | Drug Info | [531791] | |||
compound 3k | Drug Info | [531791] | |||
compound 3q | Drug Info | [531791] | |||
compound 3u | Drug Info | [531791] | |||
compound 4 (Balasubramanian et al., 1992) | Drug Info | [543905] | |||
compound 41 | Drug Info | [528898] | |||
compound 42 | Drug Info | [528898] | |||
compound 4d | Drug Info | [532037] | |||
compound 4ff | Drug Info | [528092] | |||
compound 4i | Drug Info | [532037] | |||
compound 4p | Drug Info | [529773] | |||
compound 4rr | Drug Info | [528092] | |||
compound 50 | Drug Info | [529210] | |||
compound 5ab | Drug Info | [533951] | |||
compound 6a (Patil et al., 1989) | Drug Info | [543905] | |||
compound 6v | Drug Info | [529773] | |||
compound 7 | Drug Info | [533384] | |||
compound 74 | Drug Info | [528092] | |||
compound 8b | Drug Info | [530523] | |||
compound 9 | Drug Info | [527607] | |||
compound 9 | Drug Info | [533814] | |||
compound 9a (Patil et al., 1989) | Drug Info | [543905] | |||
CP-83101 | Drug Info | [532476] | |||
Crestor/TriLipix | Drug Info | [550288] | |||
CRILVASTATIN | Drug Info | [534229], [551871] | |||
Dalvastatin | Drug Info | [534036] | |||
DFGYVAE | Drug Info | [530939] | |||
F(4-Fluoro)VAE | Drug Info | [529130] | |||
Fluvastatin | Drug Info | [535246] | |||
FPYVAE peptide | Drug Info | [530939] | |||
GFPDGG | Drug Info | [529130] | |||
GFPEGG | Drug Info | [529130] | |||
GFPTGG | Drug Info | [529130] | |||
GLENVASTATIN | Drug Info | [533833], [551871] | |||
GLPDGG peptide | Drug Info | [530939] | |||
GLPTGG | Drug Info | [529130] | |||
HMG-CoA reductase inhibitor | Drug Info | [536838] | |||
Lovastatin | Drug Info | [535491] | |||
Meglutol | Drug Info | [527409] | |||
MK-0524B | Drug Info | [549718], [550977] | |||
NCX-6560 | Drug Info | [535747] | |||
Nicotinamide-Adenine-Dinucleotide | Drug Info | [551393] | |||
NK-104 | Drug Info | [535153] | |||
o-hydroxyatorvastatin | Drug Info | [529527] | |||
PF-3052334 | Drug Info | [529210] | |||
PITAVASTATIN CALCIUM | Drug Info | [529042] | |||
Pravastatin | Drug Info | [535442] | |||
Pravigard | Drug Info | [536186] | |||
RBx10558 | Drug Info | [544419] | |||
Rosuvastatin | Drug Info | [535680] | |||
Simvastatin | Drug Info | [535246] | |||
Simvistatin | Drug Info | [536186] | |||
SQ-33600 | Drug Info | [527403] | |||
Statins | Drug Info | [536740], [537114] | |||
TOCOTRIENOL | Drug Info | [526580], [551871] | |||
Modulator | GT-16-239 | Drug Info | [534777] | ||
MT-001 | Drug Info | [543905] | |||
NCX-1067 | Drug Info | [543905] | |||
Premarin/Pravachol | Drug Info | [535747] | |||
rawsonol | Drug Info | ||||
SR12813 | Drug Info | ||||
Statin | Drug Info | [543905] | |||
XZK-monascus | Drug Info | [531854] | |||
Antagonist | Mevastatin | Drug Info | [551386] | ||
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 | |||||
Ref 523598 | ClinicalTrials.gov (NCT01422382) Drug-Drug Interaction of Cardizem LA (Diltiazem Hydrochloride) on Pitavastatin. U.S. National Institutes of Health. | ||||
Ref 532347 | Vitamin E: tocopherols and tocotrienols as potential radiation countermeasures. J Radiat Res. 2013 Nov 1;54(6):973-88. | ||||
Ref 535747 | Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26. | ||||
Ref 536186 | Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. | ||||
Ref 536361 | Natural 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 536372 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | ||||
Ref 536838 | Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. | ||||
Ref 539783 | (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 539809 | (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 539962 | (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 539963 | (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 539964 | (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 539965 | (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 539966 | (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 539985 | (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 539994 | (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 540037 | (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 544592 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000245) | ||||
Ref 544823 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001230) | ||||
Ref 545019 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001903) | ||||
Ref 545021 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001906) | ||||
Ref 545138 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002276) | ||||
Ref 545145 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002290) | ||||
Ref 545153 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002306) | ||||
Ref 545154 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002307) | ||||
Ref 545157 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002314) | ||||
Ref 545220 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002490) | ||||
Ref 545692 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004222) | ||||
Ref 545795 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004764) | ||||
Ref 546960 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011586) | ||||
Ref 548247 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023729) | ||||
Ref 548403 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025331) | ||||
Ref 548433 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025539) | ||||
Ref 526518 | Effects of simvastatin, an HMG-CoA reductase inhibitor, in patients with hypertriglyceridemia. Clin Cardiol. 2003 Jan;26(1):18-24. | ||||
Ref 526580 | Inhibitory effect of delta-tocotrienol, a HMG CoA reductase inhibitor, on monocyte-endothelial cell adhesion. J Nutr Sci Vitaminol (Tokyo). 2002 Oct;48(5):332-7. | ||||
Ref 527151 | Synthesis 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 527403 | Determination of SQ 33,600, a phosphinic acid containing HMG CoA reductase inhibitor, in human serum by high-performance liquid chromatography combined with ionspray mass spectrometry. Biol Mass Spectrom. 1992 Apr;21(4):189-94. | ||||
Ref 527409 | Bioorg 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 527410 | Three-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 527607 | Inhibitors 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 528092 | Synthesis 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 528887 | Discovery 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 528898 | Design 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 528899 | Design 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 529042 | Bioorg Med Chem. 2007 Dec 15;15(24):7809-29. Epub 2007 Aug 28.Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents. | ||||
Ref 529130 | Bioorg 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 529210 | J 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 529232 | Hepatoselectivity 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 529423 | (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 529527 | Thermodynamic and structure guided design of statin based inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase. J Med Chem. 2008 Jul 10;51(13):3804-13. | ||||
Ref 529660 | 3-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 529773 | Phosphorus-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 530191 | Application 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 530523 | Inhibitors 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. | ||||
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