Therapeutic Targets Database
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TTD Target ID: TTDS00373

Target Information
NameTyrosine oxidase    
Type of targetSuccessful target    
SynonymsLB24-AB    
Monophenol monooxygenase    
SK29-AB    
Tumor rejection antigen AB    
Tyrosinase    
DiseaseSkin diseases[1]
Drug(s)MonobenzoneApprovedVitiligo[2]
BioChemical ClassOxidoreductases acting on paired donors    
EC NumberEC 1.10.3.1
EC 1.14.18.1
PathwayAlkaloid biosynthesis I
Melanogenesis
Metabolic pathways
Riboflavin metabolism
Tyrosine metabolism
UniProt IDP14679
FunctionThis is a copper-containing oxidase that functions in the formation of pigments such as melanins and other polyphenolic compounds. Catalyzes the rate-limiting conversions of tyrosine to dopa, dopa to dopa-quinone and possibly 5,6-dihydroxyindole to indole.    
SequenceMLLAVLYCLLWSFQTSAGHFPRACVSSKNLMEKECCPPWSGDRSPCGQLSGRGSCQNILL SNAPLGPQFPFTGVDDRESWPSVFYNRTCQCSGNFMGFNCGNCKFGFWGPNCTERRLLVR RNIFDLSAPEKDKFFAYLTLAKHTISSDYVIPIGTYGQMKNGSTPMFNDINIYDLFVWMH YYVSMDALLGGSEIWRDIDFAHEAPAFLPWHRLFLLRWEQEIQKLTGDENFTIPYWDWRD AEKCDICTDEYMGGQHPTNPNLLSPASFFSSWQIVCSRLEEYNSHQSLCNGTPEGPLRRN PGNHDKSRTPRLPSSADVEFCLSLTQYESGSMDKAANFSFRNTLEGFASPLTGIADASQS SMHNALHIYMNGTMSQVQGSANDPIFLLHHAFVDSIFEQWLRRHRPLQEVYPEANAPIGH NRESYMVPFIPLYRNGDFFISSKDLGYDYSYLQDSDPDSFQDYIKSYLEQASRIWSWLLG AAMVGAVLTALLAGLVSLLCRHKRKQLPEEKQPLLMEKEDYHSLYQSHL
Related US Patent6,521,267
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-Daedalin A[3]
1'- (4-Methyl-benzyl)-[1,4']bipiperidinyl[4]
1- (1,4-diacetylphenyl)dithiosemicarbazide[5]
1- (1-[5]
1- (1-[5]
1- (1-[5]
1- (1-[5]
1- (1-[5]
1- (1-p-tolylethylidene)thiosemicarbazide[5]
1- (1-phenylethylidene)thiosemicarbazide[5]
1- (2,5-Dimethyl-1H-pyrrol-1-yl)thiourea[6]
1- (3-Methylbutylidene)thiosemicarbazide[6]
1- (3-Oxocyclohexylidene)thiosemicarbazide[6]
1- (3-Phenylallylidene)thiosemicarbazide[6]
1- (3-phenoxypropyl)-4-[4]
1- (4-[7]
1- (4-Methylpent-3-en-2-ylidene)thiosemicarbazide[6]
1- (4-bromophenyl)-3-hydroxyurea[7]
1- (But-2-enylidene)thiosemicarbazide[6]
1- (Butan-2-ylidene)thiosemicarbazide[6]
1- (Propan-2-ylidene)thiosemicarbazide[6]
1-Cyclohexylidenethiosemicarbazide[6]
1-Cyclopentylidenethiosemicarbazide[6]
1-Ethylidenethiosemicarbazide[6]
1-Propylidenethiosemicarbazide[6]
1-hydroxy-3- (4-[7]
1-hydroxy-3- (4-nitrophenyl)urea[7]
1-hydroxy-3-phenylurea[7]
2,2',4,4',6'-pentahydroxychalcone[8]
2,2',4,4'-tetrahydroxy-6'-methoxychalcone[8]
2,2',4,4'-tetrahydroxychalcone[8]
2,2'-bi (1,3,4-thiadiazole)-5,5'[9]
2,4,3',5'-tetrahydroxybibenzyl[10]
2- (butylthiomethyl)-5-hydroxy-4H-pyran-4-one[11]
2- (cyclohexylthiomethyl)-5-hydroxy-4H-pyran-4-one[11]
2- (ethylthiomethyl)-5-hydroxy-4H-pyran-4-one[11]
2- (heptylthiomethyl)-5-hydroxy-4H-pyran-4-one[11]
2- (hexylthiomethyl)-5-hydroxy-4H-pyran-4-one[11]
2-hydroxy-3-isopropyl-2,4,6-cycloheptatrien-1-one[12]
2-hydroxy-5-isopropyl-2,4,6-cycloheptatrien-1-one[12]
2-hydroxyphenethyl 3,4,5-trihydroxybenzoate[13]
3,4-dihydroxybenzaldehyde-O-ethyloxime[14]
3- (2,4-dihydroxyphenyl)-propionic acid ethylester[15]
3- (2,4-dihydroxyphenyl)-propionic acid octylester[15]
3- (2,4-dihydroxyphenyl)propionic acid[15]
3-hydroxyphenethyl 3,4,5-trihydroxybenzoate[13]
3hydroxy-1-methyl-1-phenylurea[7]
4',4-Dihydroxychalcone[16]
4'- (4-Aminobenzensulfonamide)-4-hydroxychalcone[16]
4'- (4-Fluorobenzensulfonamide)-4-hydroxychalcone[16]
4'- (4-Nitrobenzensulfonamide)-4-hydroxychalcone[16]
4'- (Benzensulfonamide)-4-hydroxychalcone[16]
4'- (p-Toluenesulfonamide)-4-hydroxychalcone[16]
4'-Amino-4-hydroxychalcone[16]
4,4'- (ethane-1,2-diyl)dibenzene-1,3-diol[17]
4- (6-hydroxynaphthalen-2-yl)benzene-1,3-diol[18]
4-adamantyl resorcinol[19]
4-hexyl resorcinol[20]
4-hydroxyphenethyl 3,4,5-trihydroxybenzoate[13]
5,5'-methylenebis (1,3,4-oxadiazole-2[9]
5,5'-methylenebis (1,3,4-thiadiazole-2[9]
5- (3-hydroxyphenyl)-1,3,4-oxadiazole-2[9]
5- (4-hydroxyphenyl)-1,3,4-oxadiazole-2[9]
5- (6-hydroxy-2-naphthyl)-1,2,3-benzenetriol[21]
5- (6-hydroxynaphthalen-2-yl)benzene-1,3-diol[18]
5- (pyridin-4-yl)-1,3,4-oxadiazole-2[9]
5- (pyridin-4-yl)-1,3,4-thiadiazole-2[9]
5-benzhydryl-1,3,4-oxadiazole-2 (3H)-thione[9]
5-benzhydryl-1,3,4-thiadiazole-2 (3H)-thione[9]
5-benzyl-1,3,4-oxadiazole-2 (3H)-thione[9]
5-cyclohexyl-1,3,4-oxadiazole-2 (3H)-thione[9]
5-hydroxy-2- (pentylthiomethyl)-4H-pyran-4-one[11]
5-hydroxy-2- (propylthiomethyl)-4H-pyran-4-one[11]
5-phenyl-1,3,4-oxadiazole-2 (3H)-thione[9]
5-phenyl-1,3,4-thiadiazole-2 (3H)-thione[9]
5-{8 (Z),-pentadecenyl}resorcinol[22]
5-{8 (Z),11[22]
5-{8 (Z),11[22]
6- (3-hydroxyphenyl)naphthalen-2-ol[18]
7,3',4'-trihydroxyisoflavone[23]
7,8,4'-trihydroxyisoflavone[23]
7- (3,5-dihydroxyphenyl)naphthalene-1,3-diol[18]
ASKENDOSIDE B[24]
Crocusatin-K[25]
DAEDALIN A[3]
ETHISTERONE[26]
HINOKITIOL[12]
Hydroquinone[2]
KAZINOL S[27]
KOJIC ACID[28]
Kojic acid-phenylalanine amide[29]
Monobenzone[2]
N- (2,4-dihydroxybenzyl)-3,4,5-trihydroxybenzamide[30]
N- (2,4-dihydroxybenzyl)-3,4-dihydroxybenzamide[30]
N- (2,4-dihydroxybenzyl)-3,5-dihydroxybenzamide[30]
N-butylresorcinol[19]
OXYRESVERATROL[10]
PHENYLTHIOUREA[7]
ROSMARINIC ACID[28]
S-2- (o-toluidino)-2-oxoethyl carbamothioate[31]
SODIUM ZINC DIHYDROLIPOYLHISTIDINATE[32]
SRI-224[14]
TROPOLONE[14]
broussonin C[27]
kazinol C[27]
kazinol F[27]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Mechanism of tyrosinase inhibition by deoxyArbutin and its second-generation derivatives. Br J Dermatol. 2008 Dec;159(6):1267-74. Epub 2008 Sep 20. To Reference
Ref 2Identification of an Alkylhydroquinone from Rhus succedanea as an Inhibitor of Tyrosinase and Melanogenesis. J Agric Food Chem. 2009 Mar 25;57(6):2200-5. To Reference
Ref 3Bioorg Med Chem Lett. 2010 Feb 1;20(3):1063-4. Epub 2009 Dec 11.Asymmetric syntheses of daedalin A and quercinol and their tyrosinase inhibitory activity. To Reference
Ref 4Eur J Med Chem. 2007 Nov-Dec;42(11-12):1370-81. Epub 2007 Feb 23.Dragon method for finding novel tyrosinase inhibitors: Biosilico identification and experimental in vitro assays. To Reference
Ref 5Bioorg Med Chem. 2008 Feb 1;16(3):1096-102.1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors. To Reference
Ref 6Eur J Med Chem. 2009 Apr;44(4):1773-8. Epub 2008 Apr 27.A class of potent tyrosinase inhibitors: alkylidenethiosemicarbazide compounds. To Reference
Ref 7Bioorg Med Chem Lett. 2008 Jun 15;18(12):3607-10. Epub 2008 May 4.Analogues of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea as inhibitors of tyrosinase and melanin formation. To Reference
Ref 8Bioorg Med Chem. 2007 Mar 15;15(6):2396-402. Epub 2007 Jan 17.Synthesis and evaluation of 2',4',6'-trihydroxychalcones as a new class of tyrosinase inhibitors. To Reference
Ref 9Bioorg Med Chem. 2010 Jun 1;18(11):4042-8. Epub 2010 Apr 13.New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. To Reference
Ref 10Bioorg Med Chem Lett. 2006 Nov 1;16(21):5650-3. Epub 2006 Aug 17.Chemical transformations of oxyresveratrol (trans-2,4,3',5'-tetrahydroxystilbene) into a potent tyrosinase inhibitor and a strong cytotoxic agent. To Reference
Ref 11Bioorg Med Chem Lett. 2010 Nov 15;20(22):6569-71. Epub 2010 Sep 21.Kojyl thioether derivatives having both tyrosinase inhibitory and anti-inflammatory properties. To Reference
Ref 12Bioorg Med Chem. 2010 Nov 15;18(22):8112-8. Epub 2010 Oct 12.Structural insights into the hot spot amino acid residues of mushroom tyrosinase for the bindings of thujaplicins. To Reference
Ref 13Bioorg Med Chem Lett. 2007 Oct 1;17(19):5462-4. Epub 2007 Jul 25.Synthetic tyrosyl gallate derivatives as potent melanin formation inhibitors. To Reference
Ref 14Bioorg Med Chem Lett. 2009 Nov 1;19(21):6157-60. Epub 2009 Sep 10.Discovery of 4-functionalized phenyl-O-beta-D-glycosides as a new class of mushroom tyrosinase inhibitors. To Reference
Ref 15J Med Chem. 2007 May 31;50(11):2676-81. Epub 2007 Apr 21.Enhanced substituted resorcinol hydrophobicity augments tyrosinase inhibition potency. To Reference
Ref 16Eur J Med Chem. 2010 May;45(5):2010-7. Epub 2010 Jan 28.Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone. To Reference
Ref 17Bioorg Med Chem Lett. 2008 Oct 1;18(19):5252-4. Epub 2008 Aug 22.Molecular design of potent tyrosinase inhibitors having the bibenzyl skeleton. To Reference
Ref 18Bioorg Med Chem Lett. 2007 Jan 15;17(2):461-4. Epub 2006 Oct 12.Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase. To Reference
Ref 19Bioorg Med Chem Lett. 2009 Mar 1;19(5):1532-3. Epub 2009 Jan 1.Studies on depigmenting activities of dihydroxyl benzamide derivatives containing adamantane moiety. To Reference
Ref 20Bioorg Med Chem Lett. 2009 Jan 1;19(1):36-9. Epub 2008 Nov 13.PEG-immobilization of cardol and soluble polymer-supported synthesis of some cardol-coumarin derivatives: preliminary evaluation of their inhibitory activity on mushroom tyrosinase. To Reference
Ref 21Bioorg Med Chem Lett. 2010 Aug 15;20(16):4882-4. Epub 2010 Jun 19.A newly synthesized, potent tyrosinase inhibitor: 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol. To Reference
Ref 22J. Nat. Prod. 57(4):545-551 (1994) To Reference
Ref 23Bioorg Med Chem Lett. 2010 Feb 1;20(3):1162-4. Epub 2009 Dec 6.Natural ortho-dihydroxyisoflavone derivatives from aged Korean fermented soybean paste as potent tyrosinase and melanin formation inhibitors. To Reference
Ref 24Bioorg Med Chem Lett. 2006 Jan 15;16(2):324-30. Epub 2005 Nov 3.New tyrosinase inhibitors selected by atomic linear indices-based classification models. To Reference
Ref 25J Nat Prod. 2004 Mar;67(3):437-40.Antityrosinase principles and constituents of the petals of Crocus sativus. To Reference
Ref 26Bioorg Med Chem. 2007 Feb 1;15(3):1483-503. Epub 2006 Nov 2.TOMOCOMD-CARDD descriptors-based virtual screening of tyrosinase inhibitors: evaluation of different classification model combinations using bond-based linear indices. To Reference
Ref 27Bioorg Med Chem. 2009 Jan 1;17(1):35-41. Epub 2008 Nov 18.Tyrosinase inhibitory effects of 1,3-diphenylpropanes from Broussonetia kazinoki. To Reference
Ref 28Bioorg Med Chem Lett. 2010 Dec 15;20(24):7393-6. Epub 2010 Oct 14.A novel ring-expanded product with enhanced tyrosinase inhibitory activity from classical Fe-catalyzed oxidation of rosmarinic acid, a potent antioxidative Lamiaceae polyphenol. To Reference
Ref 29Bioorg Med Chem Lett. 2009 Oct 1;19(19):5586-9. Epub 2009 Aug 14.Kojic acid-amino acid conjugates as tyrosinase inhibitors. To Reference
Ref 30Bioorg Med Chem Lett. 2006 May 15;16(10):2682-4. Epub 2006 Mar 2.N-Benzylbenzamides: a new class of potent tyrosinase inhibitors. To Reference
Ref 31Bioorg Med Chem Lett. 2007 Dec 15;17(24):6871-5. Epub 2007 Oct 12.Discovery of small-molecule inhibitors of tyrosinase. To Reference
Ref 32Bioorg Med Chem. 2007 Mar 1;15(5):1967-75. Epub 2006 Dec 31.Modulating effects of a novel skin-lightening agent, alpha-lipoic acid derivative, on melanin production by the formation of DOPA conjugate products. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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