Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T53585
(Former ID: TTDS00195)
|
|||||
Target Name |
HMG-CoA reductase (HMGCR)
|
|||||
Synonyms |
3-hydroxy-3-methylglutaryl-coenzyme A reductase
|
|||||
Gene Name |
HMGCR
|
|||||
Target Type |
Successful target
|
[1] | ||||
Disease | [+] 7 Target-related Diseases | + | ||||
1 | Cardiovascular disease [ICD-11: BA00-BE2Z] | |||||
2 | Dyslipidemia [ICD-11: 5C80-5C81] | |||||
3 | Hyper-lipoproteinaemia [ICD-11: 5C80] | |||||
4 | Multiple sclerosis [ICD-11: 8A40] | |||||
5 | Myocardial infarction [ICD-11: BA41-BA43] | |||||
6 | Pain [ICD-11: MG30-MG3Z] | |||||
7 | Coronary atherosclerosis [ICD-11: BA80] | |||||
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.
Click to Show/Hide
|
|||||
BioChemical Class |
CH-OH donor oxidoreductase
|
|||||
UniProt ID | ||||||
EC Number |
EC 1.1.1.34
|
|||||
Sequence |
MLSRLFRMHGLFVASHPWEVIVGTVTLTICMMSMNMFTGNNKICGWNYECPKFEEDVLSS
DIIILTITRCIAILYIYFQFQNLRQLGSKYILGIAGLFTIFSSFVFSTVVIHFLDKELTG LNEALPFFLLLIDLSRASTLAKFALSSNSQDEVRENIARGMAILGPTFTLDALVECLVIG VGTMSGVRQLEIMCCFGCMSVLANYFVFMTFFPACVSLVLELSRESREGRPIWQLSHFAR VLEEEENKPNPVTQRVKMIMSLGLVLVHAHSRWIADPSPQNSTADTSKVSLGLDENVSKR IEPSVSLWQFYLSKMISMDIEQVITLSLALLLAVKYIFFEQTETESTLSLKNPITSPVVT QKKVPDNCCRREPMLVRNNQKCDSVEEETGINRERKVEVIKPLVAETDTPNRATFVVGNS SLLDTSSVLVTQEPEIELPREPRPNEECLQILGNAEKGAKFLSDAEIIQLVNAKHIPAYK LETLMETHERGVSIRRQLLSKKLSEPSSLQYLPYRDYNYSLVMGACCENVIGYMPIPVGV AGPLCLDEKEFQVPMATTEGCLVASTNRGCRAIGLGGGASSRVLADGMTRGPVVRLPRAC DSAEVKAWLETSEGFAVIKEAFDSTSRFARLQKLHTSIAGRNLYIRFQSRSGDAMGMNMI SKGTEKALSKLHEYFPEMQILAVSGNYCTDKKPAAINWIEGRGKSVVCEAVIPAKVVREV LKTTTEAMIEVNINKNLVGSAMAGSIGGYNAHAANIVTAIYIACGQDAAQNVGSSNCITL MEASGPTNEDLYISCTMPSIEIGTVGGGTNLLPQQACLQMLGVQGACKDNPGENARQLAR IVCGTVMAGELSLMAALAAGHLVKSHMIHNRSKINLQDLQGACTKKTA Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A00809 ; BADD_A02409 ; BADD_A05311 ; BADD_A05828 | |||||
HIT2.0 ID | T21Q0D |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Approved Drug(s) | [+] 13 Approved Drugs | + | ||||
1 | Aspirin | Drug Info | Approved | Pain | [1], [2] | |
2 | Atorvastatin | Drug Info | Approved | Cardiovascular disease | [3] | |
3 | Cerivastatin | Drug Info | Approved | Hyperlipidaemia | [4], [5] | |
4 | Crestor/TriLipix | Drug Info | Approved | Dyslipidemia | [3] | |
5 | Fluvastatin | Drug Info | Approved | Hypercholesterolaemia | [6], [7] | |
6 | Lovastatin | Drug Info | Approved | Hypercholesterolaemia | [7], [8] | |
7 | PITAVASTATIN CALCIUM | Drug Info | Approved | Dyslipidemia | [3], [9] | |
8 | Pravastatin | Drug Info | Approved | Hypercholesterolaemia | [10], [11] | |
9 | Rosuvastatin | Drug Info | Approved | Hypercholesterolaemia | [12], [13] | |
10 | Simvastatin | Drug Info | Approved | Hypercholesterolaemia | [7], [14] | |
11 | Teriflunomide | Drug Info | Approved | Hyperlipidaemia | [1] | |
12 | TOCOTRIENOL | Drug Info | Approved | Hyperlipidaemia | [15] | |
13 | LAROPIPRANT | Drug Info | Phase 4 | Coronary heart disease | [16] | |
Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
1 | Premarin/Pravachol | Drug Info | Phase 3 | Hyperlipidaemia | [17] | |
2 | CRILVASTATIN | Drug Info | Phase 2 | Hyperlipidaemia | [18] | |
3 | XZK-monascus | Drug Info | Phase 2 | Hyperlipidaemia | [19] | |
4 | NCX-6560 | Drug Info | Phase 1 | Cardiovascular disease | [17] | |
Discontinued Drug(s) | [+] 11 Discontinued Drugs | + | ||||
1 | Dalvastatin | Drug Info | Discontinued in Phase 3 | Hyperlipidaemia | [20] | |
2 | Bervastatin | Drug Info | Discontinued in Phase 2 | Thrombosis | [21] | |
3 | BMY-21950 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [22], [23] | |
4 | GLENVASTATIN | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [24] | |
5 | RBx10558 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [25] | |
6 | PF-3052334 | Drug Info | Discontinued in Phase 1 | Arteriosclerosis | [26] | |
7 | BMY-22089 | Drug Info | Terminated | Hyperlipidaemia | [27], [28] | |
8 | CP-83101 | Drug Info | Terminated | Arteriosclerosis | [29] | |
9 | GT-16-239 | Drug Info | Terminated | Arteriosclerosis | [30] | |
10 | SQ-33600 | Drug Info | Terminated | Hyperlipidaemia | [31] | |
11 | SR12813 | Drug Info | Terminated | Arteriosclerosis | [32], [33] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Inhibitor | [+] 126 Inhibitor drugs | + | ||||
1 | Aspirin | Drug Info | [1] | |||
2 | Atorvastatin | Drug Info | [34] | |||
3 | Cerivastatin | Drug Info | [7], [35], [36] | |||
4 | Crestor/TriLipix | Drug Info | [37] | |||
5 | Fluvastatin | Drug Info | [34] | |||
6 | Lovastatin | Drug Info | [38] | |||
7 | PITAVASTATIN CALCIUM | Drug Info | [39], [40] | |||
8 | Pravastatin | Drug Info | [41] | |||
9 | Rosuvastatin | Drug Info | [42] | |||
10 | Simvastatin | Drug Info | [34] | |||
11 | Teriflunomide | Drug Info | [1] | |||
12 | TOCOTRIENOL | Drug Info | [43], [3] | |||
13 | LAROPIPRANT | Drug Info | [44], [45] | |||
14 | CRILVASTATIN | Drug Info | [46], [3] | |||
15 | NCX-6560 | Drug Info | [17] | |||
16 | 2-cyclopropyl-4-substituted-phenoxy-quinoline derivative 1 | Drug Info | [48] | |||
17 | Atorvastatin lactole derivative 1 | Drug Info | [48] | |||
18 | Hexahydro naphthalene derivative 1 | Drug Info | [48] | |||
19 | Hexahydro naphthalene derivative 2 | Drug Info | [48] | |||
20 | Hexahydro naphthalene derivative 3 | Drug Info | [48] | |||
21 | Lactol derivative 1 | Drug Info | [48] | |||
22 | Lactol derivative 2 | Drug Info | [48] | |||
23 | Pitavastatin derivative 1 | Drug Info | [48] | |||
24 | PMID27537201-Compound-Figure11 | Drug Info | [48] | |||
25 | PMID27537201-Compound-Figure13b | Drug Info | [48] | |||
26 | PMID27537201-Compound-Figure13c | Drug Info | [48] | |||
27 | PMID27537201-Compound-Figure15a | Drug Info | [48] | |||
28 | PMID27537201-Compound-Figure15b | Drug Info | [48] | |||
29 | PMID27537201-Compound-Figure17 | Drug Info | [48] | |||
30 | Poly-substituted azoles statin lactone derivative 1 | Drug Info | [48] | |||
31 | Poly-substituted azoles statin lactone derivative 2 | Drug Info | [48] | |||
32 | Poly-substituted miazine derivative 1 | Drug Info | [48] | |||
33 | Pravastatin derivative 1 | Drug Info | [48] | |||
34 | Quinoline derivative 1 | Drug Info | [48] | |||
35 | Quinoline derivative 16 | Drug Info | [48] | |||
36 | Quinoline derivative 17 | Drug Info | [48] | |||
37 | Sterol derivative 1 | Drug Info | [48] | |||
38 | Sterol derivative 2 | Drug Info | [48] | |||
39 | Sterol derivative 3 | Drug Info | [48] | |||
40 | Dalvastatin | Drug Info | [49] | |||
41 | Bervastatin | Drug Info | [50] | |||
42 | BMY-21950 | Drug Info | [51], [3] | |||
43 | GLENVASTATIN | Drug Info | [52], [3] | |||
44 | RBx10558 | Drug Info | [53] | |||
45 | PF-3052334 | Drug Info | [54] | |||
46 | BMY-22089 | Drug Info | [51], [3] | |||
47 | CP-83101 | Drug Info | [55] | |||
48 | SQ-33600 | Drug Info | [58] | |||
49 | (E)-5-octadecen-7,9-diynoic acid | Drug Info | [60] | |||
50 | (E)-octadecan-9-ynoic acid | Drug Info | [60] | |||
51 | (R)-Mevalonate | Drug Info | [61] | |||
52 | (Z)-5-octadecen-7,9-diynoic acid | Drug Info | [60] | |||
53 | (Z)-7-octedecan-9-ynoic acid | Drug Info | [60] | |||
54 | 1,4-Dithiothreitol | Drug Info | [61] | |||
55 | 2'-Monophosphoadenosine 5'-Diphosphoribose | Drug Info | [61] | |||
56 | 3-(1,3 dodecadiynyl)-6-oxiranebutanoic acid | Drug Info | [60] | |||
57 | 3-Hydroxy-3-Methyl-Glutaric Acid | Drug Info | [61], [62] | |||
58 | 5-ketodihydromevinolin | Drug Info | [63] | |||
59 | 6-hydroxy-7,9-octadecadiynoic acid | Drug Info | [60] | |||
60 | 7,9-octadecadiynoic acid | Drug Info | [60] | |||
61 | 7,9-tetradecadiynoic acid | Drug Info | [60] | |||
62 | 9-octadecynoic acid | Drug Info | [60] | |||
63 | BPL-001 | Drug Info | [64] | |||
64 | Brutieridin | Drug Info | [64] | |||
65 | Coenzyme A | Drug Info | [61] | |||
66 | DFGYVAE | Drug Info | [65] | |||
67 | F(4-Fluoro)VAE | Drug Info | [66] | |||
68 | FPYVAE peptide | Drug Info | [65] | |||
69 | GFPDGG | Drug Info | [66] | |||
70 | GFPEGG | Drug Info | [66] | |||
71 | GFPTGG | Drug Info | [66] | |||
72 | GLPDGG peptide | Drug Info | [65] | |||
73 | GLPTGG | Drug Info | [66] | |||
74 | Nicotinamide-Adenine-Dinucleotide | Drug Info | [61] | |||
75 | o-hydroxyatorvastatin | Drug Info | [67] | |||
76 | PMID1527791C29 | Drug Info | [68] | |||
77 | PMID15686906C17 | Drug Info | [69] | |||
78 | PMID15686906C29 | Drug Info | [69] | |||
79 | PMID1656041C11dd | Drug Info | [70] | |||
80 | PMID1656041C11ff | Drug Info | [70] | |||
81 | PMID1656041C11jj | Drug Info | [70] | |||
82 | PMID1656041C11nn | Drug Info | [70] | |||
83 | PMID1656041C4ff | Drug Info | [70] | |||
84 | PMID1656041C4rr | Drug Info | [70] | |||
85 | PMID1656041C74 | Drug Info | [70] | |||
86 | PMID17560788C29f | Drug Info | [71] | |||
87 | PMID17574411C41 | Drug Info | [72] | |||
88 | PMID17574411C42 | Drug Info | [72] | |||
89 | PMID17574412C33 | Drug Info | [73] | |||
90 | PMID18072721C50 | Drug Info | [54] | |||
91 | PMID18155906C16f | Drug Info | [74] | |||
92 | PMID18412317C13b | Drug Info | [75] | |||
93 | PMID1875346C18 | Drug Info | [76] | |||
94 | PMID1895299C1 | Drug Info | [77] | |||
95 | PMID1895299C4p | Drug Info | [77] | |||
96 | PMID1895299C6v | Drug Info | [77] | |||
97 | PMID19502059C25d | Drug Info | [78] | |||
98 | PMID1992138C8b | Drug Info | [79] | |||
99 | PMID1992149C13 | Drug Info | [80] | |||
100 | PMID1992149C9 | Drug Info | [81] | |||
101 | PMID2153213C13b | Drug Info | [82] | |||
102 | PMID2153213C13g | Drug Info | [82] | |||
103 | PMID2153213C1a | Drug Info | [82] | |||
104 | PMID2153213C1e | Drug Info | [82] | |||
105 | PMID2153213C1f | Drug Info | [82] | |||
106 | PMID2153213C2c | Drug Info | [82] | |||
107 | PMID2153213C2d | Drug Info | [82] | |||
108 | PMID2153213C2f | Drug Info | [82] | |||
109 | PMID2231594C3j | Drug Info | [83] | |||
110 | PMID2231594C3k | Drug Info | [83] | |||
111 | PMID2231594C3q | Drug Info | [83] | |||
112 | PMID2231594C3u | Drug Info | [83] | |||
113 | PMID2296027C25 | Drug Info | [84] | |||
114 | PMID2296027C29 | Drug Info | [84] | |||
115 | PMID2296036C2g | Drug Info | [85] | |||
116 | PMID2296036C2t | Drug Info | [85] | |||
117 | PMID2296036C4d | Drug Info | [85] | |||
118 | PMID2296036C4i | Drug Info | [85] | |||
119 | PMID2909732C7 | Drug Info | [86] | |||
120 | PMID7932551C9 | Drug Info | [87] | |||
121 | PMID8246233C28 | Drug Info | [88] | |||
122 | PMID8246233C35 | Drug Info | [88] | |||
123 | PMID8246233C5ab | Drug Info | [88] | |||
124 | PMID8246234C3h | Drug Info | [89] | |||
125 | PMID8246237C18t | Drug Info | [90] | |||
126 | PMID8426367C18 | Drug Info | [91] | |||
Modulator | [+] 8 Modulator drugs | + | ||||
1 | Premarin/Pravachol | Drug Info | [17] | |||
2 | XZK-monascus | Drug Info | [47] | |||
3 | GT-16-239 | Drug Info | [56] | |||
4 | SR12813 | Drug Info | [59] | |||
5 | MT-001 | Drug Info | [64] | |||
6 | NCX-1067 | Drug Info | [64] | |||
7 | rawsonol | Drug Info | [92] | |||
8 | Statin | Drug Info | [64] | |||
Antagonist | [+] 1 Antagonist drugs | + | ||||
1 | Mevastatin | Drug Info | [57] |
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
BioCyc | [+] 3 BioCyc Pathways | + | ||||
1 | Superpathway of geranylgeranyldiphosphate biosynthesis I (via mevalonate) | |||||
2 | Superpathway of cholesterol biosynthesis | |||||
3 | Mevalonate pathway | |||||
KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
1 | Terpenoid backbone biosynthesis | |||||
2 | Metabolic pathways | |||||
3 | Biosynthesis of antibiotics | |||||
4 | AMPK signaling pathway | |||||
5 | Bile secretion | |||||
NetPath Pathway | [+] 3 NetPath Pathways | + | ||||
1 | IL5 Signaling Pathway | |||||
2 | TGF_beta_Receptor Signaling Pathway | |||||
3 | TSH Signaling Pathway | |||||
Panther Pathway | [+] 1 Panther Pathways | + | ||||
1 | Cholesterol biosynthesis | |||||
Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
1 | Steroid Biosynthesis | |||||
WikiPathways | [+] 7 WikiPathways | + | ||||
1 | Statin Pathway | |||||
2 | Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha) | |||||
3 | Activation of Gene Expression by SREBP (SREBF) | |||||
4 | SREBF and miR33 in cholesterol and lipid homeostasis | |||||
5 | Integrated Breast Cancer Pathway | |||||
6 | SREBP signalling | |||||
7 | Cholesterol Biosynthesis |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. | |||||
REF 2 | URL: 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: 4139). | |||||
REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 4 | URL: 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 5 | 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 6 | URL: 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 7 | Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. | |||||
REF 8 | URL: 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 9 | 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 10 | URL: 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 11 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 12 | URL: 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 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | |||||
REF 14 | URL: 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 15 | Vitamin E: tocopherols and tocotrienols as potential radiation countermeasures. J Radiat Res. 2013 Nov 1;54(6):973-88. | |||||
REF 16 | ClinicalTrials.gov (NCT01126073) A Double Blind, Randomized Study to Compare Influence of Niacin/Laropiprant on Functional and Morphological Characteristics of Arterial Wall and Parameters of Inflammation in Subjects With Coronary Heart Disease Already Treated With a Statin in Miran Sebestjen, University Medical Centre Ljubljana. | |||||
REF 17 | Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26. | |||||
REF 18 | 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 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036391) | |||||
REF 20 | 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 21 | 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 22 | URL: 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 23 | 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 24 | 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 25 | 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 26 | 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 27 | URL: 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 28 | 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 29 | 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 30 | 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 31 | 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 32 | URL: 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 33 | 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 34 | Equally 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 35 | Emerging antidyslipidemic drugs. Expert Opin Emerg Drugs. 2008 Jun;13(2):363-81. | |||||
REF 36 | HMG-CoA reductase inhibitor has protective effects against stroke events in stroke-prone spontaneously hypertensive rats. Stroke. 2003 Jan;34(1):157-63. | |||||
REF 37 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
REF 38 | Microarray and biochemical analysis of lovastatin-induced apoptosis of squamous cell carcinomas. Neoplasia. 2002 Jul-Aug;4(4):337-46. | |||||
REF 39 | Cholesterol-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. | |||||
REF 40 | Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents. Bioorg Med Chem. 2007 Dec 15;15(24):7809-29. | |||||
REF 41 | A randomized, double-blind trial comparing the efficacy and safety of pitavastatin versus pravastatin in patients with primary hypercholesterolemia. Atherosclerosis. 2002 Jun;162(2):373-9. | |||||
REF 42 | New dimension of statin action on ApoB atherogenicity. Clin Cardiol. 2003 Jan;26(1 Suppl 1):I7-10. | |||||
REF 43 | 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 44 | A 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 45 | Selective Targeting of CTNBB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs. PLoS One. 2015 May 27;10(5):e0125021. | |||||
REF 46 | Differences 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 47 | NMR evaluation of total statin content and HMG-CoA reductase inhibition in red yeast rice (Monascus spp.) food supplements. Chin Med. 2012 Mar 22;7:8. | |||||
REF 48 | HMG-CoA Reductase inhibitors: an updated review of patents of novel compounds and formulations (2011-2015).Expert Opin Ther Pat. 2016 Nov;26(11):1257-1272. | |||||
REF 49 | RG 12561 (dalvastatin): a novel synthetic inhibitor of HMG-CoA reductase and cholesterol-lowering agent. Pharmacology. 1993;46(1):13-22. | |||||
REF 50 | Effects of simvastatin, an HMG-CoA reductase inhibitor, in patients with hypertriglyceridemia. Clin Cardiol. 2003 Jan;26(1):18-24. | |||||
REF 51 | Selective inhibition of cholesterol synthesis in liver versus extrahepatic tissues by HMG-CoA reductase inhibitors. J Lipid Res. 1990 Jul;31(7):1271-82. | |||||
REF 52 | Bile acid derived HMG-CoA reductase inhibitors. Biochim Biophys Acta. 1994 Nov 29;1227(3):137-54. | |||||
REF 53 | New Frontiers in the Treatment of Diabetic Dyslipidemia. Rev Diabet Stud. 2013 Summer-Fall; 10(2-3): 204-212. | |||||
REF 54 | Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylca... J Med Chem. 2008 Jan 10;51(1):31-45. | |||||
REF 55 | Efficacy, 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 56 | Studies of cholesterol and bile acid metabolism, and early atherogenesis in hamsters fed GT16-239, a novel bile acid sequestrant (BAS). Atherosclerosis. 1998 Oct;140(2):315-24. | |||||
REF 57 | Regulation of CYP2B6 and CYP3A expression by hydroxymethylglutaryl coenzyme A inhibitors in primary cultured human hepatocytes. Drug Metab Dispos. 2002 Dec;30(12):1400-5. | |||||
REF 58 | 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 59 | The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A r... J Biol Chem. 1996 Jun 14;271(24):14376-82. | |||||
REF 60 | Novel 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 61 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
REF 62 | Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase. Bioorg Med Chem Lett. 2005 Feb 15;15(4):989-94. | |||||
REF 63 | Total synthesis and biological evaluation of structural analogues of compactin and dihydromevinolin. J Med Chem. 1987 Oct;30(10):1858-73. | |||||
REF 64 | URL: 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 65 | Peptide 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 66 | Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone. Bioorg Med Chem. 2008 Feb 1;16(3):1309-18. | |||||
REF 67 | 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 68 | 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 69 | 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 70 | 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 71 | Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase. Bioorg Med Chem. 2007 Aug 15;15(16):5576-89. | |||||
REF 72 | Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4531-7. | |||||
REF 73 | Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4538-44. | |||||
REF 74 | 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. | |||||
REF 75 | (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 76 | 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 77 | 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 78 | 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 79 | 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. | |||||
REF 80 | Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase. J Med Chem. 1991 Jan;34(1):463-6. | |||||
REF 81 | 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 82 | Synthesis 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 83 | Phosphorus-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 84 | Inhibitors 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 85 | Synthesis 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 86 | Synthesis and biological evaluation of a monocyclic, fully functional analogue of compactin. J Med Chem. 1989 Jan;32(1):197-202. | |||||
REF 87 | Synthesis 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 88 | Inhibitors 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 89 | Inhibitors 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 90 | HMG-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 91 | 32-Methyl-32-oxylanosterols: dual-action inhibitors of cholesterol biosynthesis. J Med Chem. 1993 Feb 5;36(3):410-6. | |||||
REF 92 | Bromophenols in Marine Algae and Their Bioactivities |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.