Target Information

Target General Infomation
Target ID
T13260
Former ID
TTDS00252
Target Name
Cytochrome P450 19
Gene Name
CYP19A1
Synonyms
Aromatase; CYPXIX; Estrogen synthetase; P-450AROM; CYP19A1
Target Type
Successful
Disease Advanced breast cancer [ICD9: 174, 175; ICD10: C50]
Bladder cancer [ICD9: 188; ICD10: C67]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Cushing's disease; Metastatic breast cancer [ICD9: 174, 175, 255.0; ICD10: C50, E24]
Dermatological disease [ICD10: L00-L99]
Endometriosis [ICD9: 617; ICD10: N80]
Hormonally-responsive breast cancer [ICD9: 174, 175; ICD10: C50]
Painful diabetic neuropathy [ICD9: 250.6,338,780; ICD10: E10.4, E11.4, E13.4, G89, R52]
Prostate disease [ICD10: N42.9]
Unspecified [ICD code not available]
Function
Catalyzesthe formation of aromatic C18 estrogens from C19 androgens.
BioChemical Class
Oxidoreductases acting on paired donors
Target Validation
T13260
UniProt ID
P11511
EC Number
EC 1.14.14.1
Sequence
MVLEMLNPIHYNITSIVPEAMPAATMPVLLLTGLFLLVWNYEGTSSIPGPGYCMGIGPLI
SHGRFLWMGIGSACNYYNRVYGEFMRVWISGEETLIISKSSSMFHIMKHNHYSSRFGSKL
GLQCIGMHEKGIIFNNNPELWKTTRPFFMKALSGPGLVRMVTVCAESLKTHLDRLEEVTN
ESGYVDVLTLLRRVMLDTSNTLFLRIPLDESAIVVKIQGYFDAWQALLIKPDIFFKISWL
YKKYEKSVKDLKDAIEVLIAEKRRRISTEEKLEECMDFATELILAEKRGDLTRENVNQCI
LEMLIAAPDTMSVSLFFMLFLIAKHPNVEEAIIKEIQTVIGERDIKIDDIQKLKVMENFI
YESMRYQPVVDLVMRKALEDDVIDGYPVKKGTNIILNIGRMHRLEFFPKPNEFTLENFAK
NVPYRYFQPFGFGPRGCAGKYIAMVMMKAILVTLLRRFHVKTLQGQCVESIQKIHDLSLH
PDETKNMLEMIFTPRNSDRCLEH
Drugs and Mode of Action
Drug(s) Aminoglutethimide Drug Info Approved Cushing's disease; Metastatic breast cancer [1], [2]
Anastrozole Drug Info Approved Breast cancer [3], [4]
Exemestane Drug Info Approved Hormonally-responsive breast cancer [5], [6]
FADROZOLE Drug Info Approved Breast cancer [7], [8], [9]
Letrozole Drug Info Approved Hormonally-responsive breast cancer [10], [4]
Testolactone Drug Info Approved Advanced breast cancer [5], [11]
Atamestane-plus- Toremifene Drug Info Phase 3 Breast cancer [12]
LIAROZOLE Drug Info Phase 2/3 Dermatological disease [13], [14]
BGS-649 Drug Info Phase 2 Endometriosis [15]
COUMATE Drug Info Phase 2 Breast cancer [16]
Dextromethorphan+quinidine Drug Info Phase 2 Painful diabetic neuropathy [17]
NARINGENIN Drug Info Phase 1 Discovery agent [18]
FORMESTANE Drug Info Withdrawn from market Breast cancer [19], [9]
FINROZOLE Drug Info Discontinued in Phase 2 Prostate disease [20]
NKS-01 Drug Info Discontinued in Phase 2 Bladder cancer [21]
VOROZOLE Drug Info Discontinued in Phase 2 Discovery agent [22]
YM-511 Drug Info Discontinued in Phase 2 Breast cancer [23]
MINAMESTANE Drug Info Terminated Bladder cancer [24]
Rogletimide Drug Info Terminated Breast cancer [25]
Inhibitor (+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Drug Info [26]
(+/-)-7-methoxy-2-phenylchroman-4-one Drug Info [27]
(2S)-5,7,2',4'-tetrahydroxyflavanone Drug Info [28]
(2S)-abyssinone II Drug Info [28]
(2S)-euchrenone a7 Drug Info [28]
1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole Drug Info [29]
1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole Drug Info [30]
1-(2-phenoxybenzyl)-1H-imidazole Drug Info [31]
1-(3-(4-fluorophenyl)propyl)-1H-imidazole Drug Info [32]
1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole Drug Info [33]
1-(4-Aminophenyl)-2-(1H-imidazol-1-yl)ethanone Drug Info [34]
1-(4-Cyanobenzyl)-5-methyl-1H-imidazole Drug Info [35]
1-(4-nitro-2-phenoxybenzyl)-1H-imidazole Drug Info [31]
1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole Drug Info [31]
1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole Drug Info [36]
1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole Drug Info [30]
1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole Drug Info [32]
1-(9H-fluoren-9-yl)-1H-imidazole Drug Info [30]
1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole Drug Info [37]
1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one Drug Info [38]
1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole Drug Info [39]
1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one Drug Info [38]
1-Imidazol-1-ylmethylxanthen-9-one Drug Info [31]
1-Naphthalen-2-yl-1H-imidazole Drug Info [33]
1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole Drug Info [32]
10-EPI-8-DEOXY-CUMAMBRIN B Drug Info [32]
11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B Drug Info [32]
2,3,4-Trimethoxy-4'-amino-trans-stilbene Drug Info [34]
2,3,5-Trimethoxy-4'-amino-trans-stilbene Drug Info [34]
2,3-Dimethoxy-4'-amino-trans-stilbene Drug Info [34]
2,4-Dimethoxy-3'-amino-trans-stilbene Drug Info [34]
2,4-Dimethoxy-4'-amino-trans-stilbene Drug Info [34]
2,5-Dimethoxy-4'-amino-trans-stilbene Drug Info [34]
2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone Drug Info [34]
2-(3-hydroxyphenyl)-7-methoxychroman-4-one Drug Info [27]
2-(4-hydroxyphenyl)-7-methoxychroman-4-one Drug Info [27]
2-Imidazol-1-yl-7-methoxy-3-phenyl-chromen-4-one Drug Info [40]
2-Imidazol-1-ylmethylxanthen-9-one Drug Info [31]
2-phenyl-2,3-dihydrobenzo[h]chromen-4-one Drug Info [27]
2-Phenyl-3-pyridin-4-ylmethylene-chroman-4-one Drug Info [41]
2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol Drug Info [36]
3,4'-(Ethane-1,2-diyl)dibenzenamine Drug Info [34]
3,4,5-Trimethoxy-3'-amino-trans-stilbene Drug Info [34]
3,4,5-Trimethoxy-4'-amino-trans-stilbene Drug Info [34]
3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one Drug Info [32]
3,4-Dimethoxy-4'-amino-trans-stilbene Drug Info [34]
3,5-Diacetoxy-4'-amino-trans-stilbene Drug Info [34]
3,5-Diamino-4'-amino-trans-stilbene Drug Info [34]
3,5-Dihydroxyl-4'-amino-trans-stilbene Drug Info [34]
3,5-Dimethoxy-4'-amino-trans-stilbene Drug Info [34]
3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one Drug Info [31]
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info [42]
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info [42]
3-(2,2-Diphenyl-vinyl)-pyridine Drug Info [43]
3-(3,4-dihydronaphthalen-2-yl)pyridine Drug Info [42]
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info [42]
3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione Drug Info [44]
3-(4-Amino-phenyl)-3-butyl-piperidine-2,6-dione Drug Info [45]
3-(4-Amino-phenyl)-3-ethyl-pyrrolidine-2,5-dione Drug Info [44]
3-(4-Amino-phenyl)-3-heptyl-piperidine-2,6-dione Drug Info [45]
3-(4-Amino-phenyl)-3-hexyl-piperidine-2,6-dione Drug Info [45]
3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione Drug Info [44]
3-(4-Amino-phenyl)-3-pentyl-piperidine-2,6-dione Drug Info [45]
3-(4-Amino-phenyl)-3-propyl-piperidine-2,6-dione Drug Info [45]
3-(4-Amino-phenyl)-pyrrolidine-2,5-dione Drug Info [44]
3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info [42]
3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine Drug Info [33]
3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine Drug Info [33]
3-(6-Ethoxy-naphthalen-2-yl)-pyridine Drug Info [33]
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Drug Info [42]
3-(6-methoxynaphthalen-2-yl)pyridine Drug Info [46]
3-(imidazolylmethyl)-4'-methoxyflavone Drug Info [47]
3-(imidazolylmethyl)-4'-nitroflavone Drug Info [47]
3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone Drug Info [47]
3-(imidazolylmethyl)flavone Drug Info [47]
3-(naphthalen-2-yl)pyridine Drug Info [46]
3-Amino-4'-amino-trans-stilbene Drug Info [34]
3-Fluoren-9-ylidenemethyl-pyridine Drug Info [43]
3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Drug Info [48]
3-Indan-(1E)-ylidenemethyl-pyridine Drug Info [43]
3-Indan-(1Z)-ylidenemethyl-pyridine Drug Info [43]
3-Methoxyl-4'-amino-trans-stilbene Drug Info [34]
3-Nitro-4'-nitro-trans-stilbene Drug Info [34]
3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[3-Phenyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
3-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Drug Info [48]
4'-(Pyridin-4-ylmethyl)biphenyl-3-amine Drug Info [48]
4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone Drug Info [47]
4'-bromo-3-(imidazolylmethyl)flavone Drug Info [47]
4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone Drug Info [47]
4'-cyano-3-(imidazolylmethyl)flavone Drug Info [47]
4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info [30]
4-((1H-imidazol-1-yl)methyl)benzonitrile Drug Info [35]
4-(1-Imidazol-1-yl-vinyl)-benzonitrile Drug Info [49]
4-(2,2-Diphenyl-vinyl)-pyridine Drug Info [43]
4-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Drug Info [30]
4-(3,4,5-Trimethoxyphenethyl)aniline Drug Info [34]
4-(3,4-Dimethoxyphenethyl)aniline Drug Info [34]
4-(3,5-Dimethoxyphenethyl)benzenamine Drug Info [34]
4-ANDROSTENE-3-17-DIONE Drug Info [50]
4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one Drug Info [38]
4-Fluoren-9-ylidenemethyl-pyridine Drug Info [43]
4-Imidazol-1-yl-2-phenyl-chroman-7-ol Drug Info [36]
4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one Drug Info [38]
4-Imidazol-1-ylmethyl-1-nitrothioxanthen-9-one Drug Info [31]
4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one Drug Info [31]
4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one Drug Info [31]
4-Imidazol-1-ylmethylthioxanthen-9-one Drug Info [31]
4-Imidazol-1-ylmethylxanthen-9-one Drug Info [31]
4-Indan-(1E)-ylidenemethyl-pyridine Drug Info [43]
4-Indan-(1Z)-ylidenemethyl-pyridine Drug Info [43]
4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info [48]
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info [48]
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [43]
4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [43]
5-((1H-imidazol-1-yl)methyl)-7,8-dihydroquinoline Drug Info [30]
5-(2-(1H-imidazol-1-yl)ethyl)quinoline Drug Info [30]
5-Bromo-8-imidazol-1-ylmethyl-chromen-4-one Drug Info [38]
5-Indan-(1E)-ylidenemethyl-1H-imidazole Drug Info [51]
5-Indan-(1Z)-ylidenemethyl-1H-imidazole Drug Info [51]
5-Pyridin-3-yl-1,3-dihydro-2H-indol-2-one Drug Info [46]
5-Pyridin-3-yl-2,3-dihydro-1H-inden-1-one Drug Info [46]
5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole Drug Info [51]
5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole Drug Info [51]
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Drug Info [43]
5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine Drug Info [43]
5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole Drug Info [43]
5-[5-Methoxy-indan-(1Z)-ylidenemethyl]-thiazole Drug Info [43]
6-((1H-imidazol-1-yl)methyl)-2H-chromene-2-thione Drug Info [30]
6-Imidazol-1-yl-isoquinoline Drug Info [30]
7,4'-Dihydroxyflavone Drug Info [32]
7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info [30]
7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one Drug Info [30]
7-((1H-imidazol-1-yl)methyl)isoquinoline Drug Info [30]
7-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Drug Info [52]
7-hydroxy-2-(3-hydroxyphenyl)chroman-4-one Drug Info [27]
7-hydroxy-2-phenylchroman-4-one Drug Info [27]
7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one Drug Info [38]
8-Imidazol-1-ylmethyl-5-nitro-chromen-4-one Drug Info [38]
9-Hydroxy-7,8-benzoflavone Drug Info [32]
ALBANOL A Drug Info [28]
ALPHA-NAPHTHOFLAVONE Drug Info [32]
Aminoglutethemide Drug Info [53]
Aminoglutethimide Drug Info [54]
Anastrozole Drug Info [55], [56]
ANDROSTENEDIONE Drug Info [57]
ANDROSTENEDONE Drug Info [58]
APIGENIN Drug Info [32]
Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine Drug Info [29]
BGS-649 Drug Info [59]
BIOCHANIN Drug Info [32]
Broussoflavonol F Drug Info [28]
CGS-18320B Drug Info [32]
CHRYSIN Drug Info [32]
COUMATE Drug Info [37]
DEHYDROLEUCODIN Drug Info [32]
Dextromethorphan+quinidine Drug Info [60]
Docosapentaenoic acid Drug Info [61]
Exemestane Drug Info [62]
FADROZOLE Drug Info [63]
FINROZOLE Drug Info [64], [9]
FORMESTANE Drug Info [65]
Gamma-mangostin Drug Info [66]
GARCINONE D Drug Info [66]
GOSSYPETIN Drug Info [67]
Isogemichalcone C Drug Info [28]
ISOLICOFLAVONOL Drug Info [28]
Letrozole Drug Info [62]
LIAROZOLE Drug Info [32]
LIQUIRTIGENIN Drug Info [67]
LUDARTIN Drug Info [32]
MDL-18962 Drug Info [68]
MINAMESTANE Drug Info [69], [9]
MONODICTYOCHROMONE B Drug Info [70]
MORACHALCONE A Drug Info [28]
MR-16089 Drug Info [32]
MR-20492 Drug Info [32]
MR-20494 Drug Info [32]
MR-20496 Drug Info [71]
MR-20814 Drug Info [71]
N-(2-benzyloxy-4-nitrophenyl)methanesulfonamide Drug Info [72]
N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide Drug Info [73]
N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide Drug Info [73]
N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide Drug Info [73]
N-[2-(4'-Nitrophenyl)ethyl]-imidazole Drug Info [32]
NARINGENIN Drug Info [32]
NKS-01 Drug Info [74], [9]
NSC-122427 Drug Info [75]
NSC-12999 Drug Info [30]
NSC-131736 Drug Info [30]
NSC-19028 Drug Info [32]
NSC-289311 Drug Info [30]
NSC-356483 Drug Info [30]
NSC-356781 Drug Info [30]
NSC-368272 Drug Info [30]
NSC-368280 Drug Info [30]
NSC-369087 Drug Info [30]
NSC-613604 Drug Info [75]
NSC-625409 Drug Info [30]
NSC-666292 Drug Info [30]
NSC-683634 Drug Info [30]
NSC-75308 Drug Info [30]
NSC-93358 Drug Info [75]
NSC-94258 Drug Info [32]
NSC-94891 Drug Info [75]
Rogletimide Drug Info [76]
Testolactone Drug Info [55], [77]
VOROZOLE Drug Info [78]
YM-511 Drug Info [79]
Modulator Atamestane-plus- Toremifene Drug Info [80]
Org-33201 Drug Info
Pathways
BioCyc Pathway Superpathway of steroid hormone biosynthesis
Estradiol biosynthesis II
Estradiol biosynthesis I
KEGG Pathway Steroid hormone biosynthesis
Metabolic pathways
Ovarian steroidogenesis
NetPath Pathway FSH Signaling Pathway
PANTHER Pathway Androgen/estrogene/progesterone biosynthesis
PathWhiz Pathway Androgen and Estrogen Metabolism
Reactome Endogenous sterols
WikiPathways Metapathway biotransformation
Tryptophan metabolism
Oxidation by Cytochrome P450
Ovarian Infertility Genes
Metabolism of steroid hormones and vitamin D
FSH signaling pathway
Integrated Breast Cancer Pathway
Phase 1 - Functionalization of compounds
References
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REF 12ClinicalTrials.gov (NCT00044291) Phase III Study of Atamestane Plus Toremifene Versus Letrozole in Advanced Breast Cancer. U.S. National Institutes of Health.
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REF 14ClinicalTrials.gov (NCT00282724) Efficacy and Safety of Two Doses of Liarozole vs. Placebo for the Treatment of Lamellar Ichthyosis. U.S. National Institutes of Health.
REF 15ClinicalTrials.gov (NCT01190475) BGS649 Monotherapy in Moderate to Severe Endometriosis Patients. U.S. National Institutes of Health.
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REF 18ClinicalTrials.gov (NCT01091077) A Pilot Study of the Grapefruit Flavonoid Naringenin for HCV Infection. U.S. National Institutes of Health.
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