Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T13260 | Target Info | |||
| Target Name | Aromatase (CYP19A1) | ||||
| Synonyms |
P-450AROM; Estrogen synthetase; Estrogen synthase; Cytochrome P450 19A1; Cytochrome P-450AROM; CYPXIX; CYP19; CYAR; ARO1
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| Target Type | Successful Target | ||||
| Gene Name | CYP19A1 | ||||
| Biochemical Class | Paired donor oxygen oxidoreductase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Steroid 11-beta-hydroxylase (CYP11B1) | Successful Target | ||||
| UniProt ID | C11B1_HUMAN | |||||
| Gene Name | CYP11B1 | |||||
| Synonyms |
S11BH; P450C11; P-450c11; CYPXIB1; CYP11B1
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| Representative Drug(s) | Drug Info | IC50 = 6.3 nM | [1] | |||
| Co-Target Name | Steryl-sulfatase (STS) | Successful Target | ||||
| UniProt ID | STS_HUMAN | |||||
| Gene Name | STS | |||||
| Synonyms |
Steryl-sulfate sulfohydrolase; Steroid sulfatase; STS; Estrone sulfatase; Arylsulfatase C; ASC
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| Representative Drug(s) | Drug Info | IC50 = 10 uM tube-1 | [2] | |||
| Co-Target Name | Carbonic anhydrase II (CA-II) | Successful Target | ||||
| UniProt ID | CAH2_HUMAN | |||||
| Gene Name | CA2 | |||||
| Synonyms |
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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| Representative Drug(s) | Drug Info | Ki = 25 nM | [3] | |||
| Co-Target Name | Aldosterone synthase (CYP11B2) | Clinical trial Target | ||||
| UniProt ID | C11B2_HUMAN | |||||
| Gene Name | CYP11B2 | |||||
| Synonyms |
Steroid 18hydroxylase; Cytochrome P450C18; Cytochrome P450Aldo; Cytochrome P450 11B2, mitochondrial; CYPXIB2; CYP11B2; Aldosteronesynthesizing enzyme; ALDOS
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| Representative Drug(s) | Drug Info | IC50 = 0.8 nM | [4] | |||
| Co-Target Name | Cytochrome P450 24 (CYP24A1) | Clinical trial Target | ||||
| UniProt ID | CP24A_HUMAN | |||||
| Gene Name | CYP24A1 | |||||
| Synonyms |
Vitamin D(3) 24hydroxylase; Cytochrome P450CC24; CYP24A1; 24OHase; 1,25dihydroxyvitamin D(3) 24hydroxylase, mitochondrial
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| Representative Drug(s) | LIAROZOLE | Drug Info | IC50 = 2.3 nM | [5] | ||
| Co-Target Name | Cytochrome P450 26 (CYP26A1) | Clinical trial Target | ||||
| UniProt ID | CP26A_HUMAN | |||||
| Gene Name | CYP26A1 | |||||
| Synonyms |
Retinoic acid-metabolizing cytochrome; Retinoic acid inducible enzyme; Retinoic acid 4-hydroxylase; P450RAI; P450 retinoic acid-inactivating 1; HP450RAI; Cytochrome P450RAI; CYP26A1
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| Representative Drug(s) | LIAROZOLE | Drug Info | IC50 = 540 nM | [6] | ||
| Co-Target Name | Albendazole monooxygenase (CYP3A4) | Clinical trial Target | ||||
| UniProt ID | CP3A4_HUMAN | |||||
| Gene Name | CYP3A4 | |||||
| Synonyms |
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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| Representative Drug(s) | LIAROZOLE | Drug Info | IC50 = 690 nM | [7] | ||
| Co-Target Name | Cytochrome P450 26B1 (CYP26B1) | Co-Target | ||||
| UniProt ID | CP26B_HUMAN | |||||
| Gene Name | CYP26B1 | |||||
| Synonyms |
Cytochrome P450 26A2; Cytochrome P450 retinoic acid-inactivating 2; Cytochrome P450RAI-2; Retinoic acid-metabolizing cytochrome
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| Representative Drug(s) | LIAROZOLE | Drug Info | IC50 = 18 nM | [8] | ||
| References | Top | ||||
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| REF 1 | Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability. J Med Chem. 2015 Mar 12;58(5):2530-7. | ||||
| REF 2 | Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES). Bioorg Med Chem Lett. 2002 May 20;12(10):1343-6. | ||||
| REF 3 | Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5192-6. | ||||
| REF 4 | Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases. J Med Chem. 2013 Aug 8;56(15):6101-7. | ||||
| REF 5 | Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation. J Med Chem. 2014 Sep 25;57(18):7702-15. | ||||
| REF 6 | Synthesis and biological evaluation of 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-[4-(naphthalen-2-ylamino)phenyl]propyl derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26). J Med Chem. 2011 Oct 13;54(19):6803-11. | ||||
| REF 7 | Design, synthesis, and biological evaluation of amide imidazole derivatives as novel metabolic enzyme CYP26A1 inhibitors. Bioorg Med Chem. 2015 Oct 15;23(20):6763-73. | ||||
| REF 8 | Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase. J Med Chem. 2016 Mar 24;59(6):2579-95. | ||||
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