Hydroquinone

Identification

Summary

Hydroquinone is a topical brightening agent used for the treatment of skin disorders associated with hyperpigmentation including melasma, post-inflammatory hyperpigmentation, sunspots, and freckles.

Brand Names
Active 4, Glytone, Melamin, Melamix, Neova Complex Hq Plus, Tri-luma
Generic Name
Hydroquinone
DrugBank Accession Number
DB09526
Background

Hydroquinone is a topical lightening product found in OTC products, and is used to correct skin discoloration associated with disorders of hyperpigmentation including melasma, post-inflammatory hyperpigmention, sunspots, and freckles. It can be used alone, but is more frequently found in combination with other agents such as alpha-hydroxy acids, corticosteroids, retinoids, or sunscreen.

Hydroquinone has come under scrutiny due to several complications associated with its use, including dermal irritation, exogenous onchronosis, and carginogenicity. As a result of these concerns, hydroquinone has been banned in the EU and UK.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 110.1106
Monoisotopic: 110.036779436
Chemical Formula
C6H6O2
Synonyms
  • 1,4-benzenediol
  • 1,4-dihydroxybenzene
  • 4-Hydroxyphenol
  • benzene-1,4-diol
  • Hydroquinone
  • p-Benzenediol
  • p-Hydroquinone
  • p-hydroxyphenol
  • Quinol
External IDs
  • NCI-C55834
  • NSC-9247

Pharmacology

Indication

Hydroquinone is used as an OTC topical lightening agent for disorders of hyperpigmentation including melasma, post-inflammatory hyperpigmention, sunspots and freckles.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatAcne vulgarisCombination Product in combination with: Tretinoin (DB00755)•••••••••••••••••
Treatment ofMelasma••• •••
Used in combination to treatSkin hyperpigmentationCombination Product in combination with: Tretinoin (DB00755)•••••••••••••••••
Used in combination to treatSkin hyperpigmentationCombination Product in combination with: Tretinoin (DB00755)•••••••••••••••••
Used in combination to treatSkin hyperpigmentationCombination Product in combination with: Tretinoin (DB00755)•••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

Hydroquinone reduces melanin pigment production through inhibition of the tyrosinase enzyme, which is involved in the initial step of the melanin pigment biosynthesis pathway. Hydroquinone takes several months to take effect.

TargetActionsOrganism
ATyrosinase
inhibitor
Humans
AIntegrin beta-3
antagonist
Humans
AIntegrin alpha-IIb
antagonist
Humans
UCysteinyl leukotriene receptor 1
activator
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
No interactions found.

Products

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Active Moieties
NameKindUNIICASInChI Key
Phenolunknown339NCG44TV108-95-2ISWSIDIOOBJBQZ-UHFFFAOYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
141010 Hydroquinone 4%Emulsion4 g/100gTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141011 Hydroquinone 6%Emulsion6 g/100gTopicalSincerus Florida, LLC2020-07-03Not applicableUS flag
141030 Hydroquinone 8%Emulsion8 g/100gTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141055 Hydroquinone 6%Emulsion6 g/100gTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141067 Hydroquinone 8%Emulsion8 g/100gTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Accelerated Dark Spot CorrectorCream2 g/100mLTopicalCosmetic Enterprises2017-06-122021-12-17US flag
Activator LightLotion2 g/100mLTopicalVivier Pharma2013-09-01Not applicableUS flag
Active 4Cream4 g/100mLTopicalVivier Pharma2014-05-30Not applicableUS flag
Advanced Dual Complex Fade Maximum Strength PlusGel2 g/100gTopicalBiocosmetics Research Labs2009-02-25Not applicableUS flag
Advanced Skin Lightening CreamLotion2 g/100mLTopicalVivier Pharma2016-06-012016-12-02US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Advanced LightningHydroquinone (0.02 g/1g) + Octinoxate (0.02 g/1g)CreamTopicalCBI Laboratories, Inc2005-07-01Not applicableUS flag
African Formula Skin LighteningHydroquinone (1 g/50g) + Octinoxate (.25 g/50g)CreamTopicalInternational Beauty Exchange2011-01-01Not applicableUS flag
African Formula Skin LighteningHydroquinone (5 mL/250mL) + Octinoxate (1.25 mL/250mL)LotionTopicalInternational Beauty Exchange2012-01-01Not applicableUS flag
ALBAVANCE FHydroquinone (0.05 %) + Fluocinolone acetonide (4 %) + Tretinoin (0.01 %)CreamImmortal Pharmaceutical Laboratories2017-09-182027-04-19Indonesia flag
Ambi Fade Normal SkinHydroquinone (20 mg/1g) + Octinoxate (20 mg/1g)CreamTopicalJohnson & Johnson Consumer Products Company, Division Of Johnson Consumer Companies, Inc.2012-05-302013-07-01US flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
141010 Hydroquinone 4%Hydroquinone (4 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141011 Hydroquinone 6%Hydroquinone (6 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-03Not applicableUS flag
141016 Hydrocortisone 0.5% / Hydroquinone 4% / Tretinoin 0.025%Hydroquinone (4 g/100g) + Hydrocortisone (0.5 g/100g) + Tretinoin (0.025 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141017 Hydrocortisone 0.5% / Hydroquinone 6% / Tretinoin 0.025%Hydroquinone (6 g/100g) + Hydrocortisone (0.5 g/100g) + Tretinoin (0.025 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141030 Hydroquinone 8%Hydroquinone (8 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag

Categories

ATC Codes
D11AX11 — Hydroquinone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as hydroquinones. These are compounds containing a hydroquinone moiety, which consists of a benzene ring with a hydroxyl groups at positions 1 and 4.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenols
Sub Class
Benzenediols
Direct Parent
Hydroquinones
Alternative Parents
1-hydroxy-2-unsubstituted benzenoids / Benzene and substituted derivatives / Organooxygen compounds / Hydrocarbon derivatives
Substituents
1-hydroxy-2-unsubstituted benzenoid / Aromatic homomonocyclic compound / Hydrocarbon derivative / Hydroquinone / Monocyclic benzene moiety / Organic oxygen compound / Organooxygen compound
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
hydroquinones, benzenediol (CHEBI:17594) / an electron-transfer-related quinol, a benzenediol (HYDROQUINONE)
Affected organisms
Not Available

Chemical Identifiers

UNII
XV74C1N1AE
CAS number
123-31-9
InChI Key
QIGBRXMKCJKVMJ-UHFFFAOYSA-N
InChI
InChI=1S/C6H6O2/c7-5-1-2-6(8)4-3-5/h1-4,7-8H
IUPAC Name
benzene-1,4-diol
SMILES
OC1=CC=C(O)C=C1

References

General References
  1. Matsumoto M, Todo H, Akiyama T, Hirata-Koizumi M, Sugibayashi K, Ikarashi Y, Ono A, Hirose A, Yokoyama K: Risk assessment of skin lightening cosmetics containing hydroquinone. Regul Toxicol Pharmacol. 2016 Aug 10. pii: S0273-2300(16)30226-4. doi: 10.1016/j.yrtph.2016.08.005. [Article]
  2. Chen Y, Chen J, Yun L, Xu L, Liu J, Xu Y, Yang H, Liang H, Tang H: Hydroquinone-induced malignant transformation of TK6 cells by facilitating SIRT1-mediated p53 degradation and up-regulating KRAS. Toxicol Lett. 2016 Aug 8. pii: S0378-4274(16)33093-4. doi: 10.1016/j.toxlet.2016.08.006. [Article]
  3. Gbetoh MH, Amyot M: Mercury, hydroquinone and clobetasol propionate in skin lightening products in West Africa and Canada. Environ Res. 2016 Jul 1;150:403-410. doi: 10.1016/j.envres.2016.06.030. [Article]
  4. Findlay GH, Morrison JG, Simson IW: Exogenous ochronosis and pigmented colloid milium from hydroquinone bleaching creams. Br J Dermatol. 1975 Dec;93(6):613-22. [Article]
Human Metabolome Database
HMDB0002434
KEGG Drug
D00073
KEGG Compound
C00530
PubChem Compound
785
PubChem Substance
310265227
ChemSpider
764
BindingDB
26190
RxNav
5509
ChEBI
17594
ChEMBL
CHEMBL537
ZINC
ZINC000005133378
PharmGKB
PA449924
PDBe Ligand
HQE
Drugs.com
Drugs.com Drug Page
Wikipedia
Hydroquinone
PDB Entries
3zod / 3zof / 4e3h / 4qop / 5fse / 5i3a / 5i3b / 7niy / 7nmp / 7nnx
show 1 more
FDA label
Download (1.15 MB)

Clinical Trials

Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
Not AvailableCompletedPreventionSolar Lentigines1somestatusstop reasonjust information to hide
Not AvailableCompletedTreatmentMelasma2somestatusstop reasonjust information to hide
Not AvailableTerminatedNot AvailableMetastatic Renal Cell Carcinoma ( mRCC)1somestatusstop reasonjust information to hide
Not AvailableUnknown StatusNot AvailableRheumatoid Arthritis1somestatusstop reasonjust information to hide
Not AvailableUnknown StatusTreatmentMelasma1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CreamTopical4 %
GelTopical2 g/100g
GelTopical2 % w/w
GelTopical20 mg/1mL
GelTopical5 g
CreamTopical4 g
SolutionTopical5 g
Cream20 mg/g
CreamTopical20 mg/1g
CreamTopical0.02 g/1mL
LotionTopical20 mg/1mL
GelTopical2 g/100mL
LotionTopical2 g/14.25g
CreamTopical4 g/100mL
CreamCutaneous10 mL/500mL
LotionCutaneous10 mL/500mL
LotionTopical2 g/100g
CreamTopical.02 g/1g
LotionTopical.02 g/1g
CreamTopical40 mg/1g
KitTopical
GelTopical2 %
CreamTopical2 g/100mL
CreamTopical4 % w/w
CreamTopical2 g
CreamTopical2.5 g
CreamTopical400000 g
CreamTopical
Cream
SolutionTopical0.04 G/ML
LotionTopical0.02 g/1
SolutionTopical2 g/100mL
LotionTopical5 g/250mL
Cream; kitTopical0.5 g/25g
LotionTopical.02 mg/1g
LotionTopical2.0 g/100mL
EmulsionTopical2.0 g/100mL
LotionTopical40 mg/1g
CreamTopical2 %
CreamTopical4 g/100g
CreamTopical4 mg/1g
GelTopical50 MG
GelTopical4 % w/w
CreamTopical1.5 %
CreamCutaneous4 mL/200mL
LotionCutaneous4 mL/200mL
LotionTopical2 %
CreamTopical0.95 g/50mL
GelTopical0.57 g/30mL
LotionTopical9.5 g/500mL
GelTopical40 mg/1g
CreamTopical100 mg/5mg
CreamTopical5 mg/100mL
CreamTopical5 mg/100mg
CreamTopical8 mg/100mL
CreamTopical5 g
GelTopical4 %w/w
CreamTopical1 g/50mL
CreamTopical2 g/50mL
EmulsionTopical
Cream20 mg
EmulsionTopical4 g/100g
EmulsionTopical6 g/100g
EmulsionTopical8 g/100g
CreamTopical40 mg/1mL
CreamCutaneous2.000 g
LotionTopical2 g/100mL
CreamTopical1.9 g/100g
LotionTopical3.18 g
SolutionTopical3 g
EmulsionTopical0.02 g/1g
EmulsionTopical0.04 g/1g
CreamTopical2 mg/100mL
CreamTopical20 mg/1mL
Cream5 %
CreamTopical2 g/100g
ClothTopical2 g/100mL
GelTopical
CreamTopical0.04 g/1g
Cream2 %
Cream40 mg
CreamTopical4 %w/w
LiquidTopical30 mg/1mL
GelTopical
CreamTopical1.695 g/113g
CreamTopical1 g/50g
GelTopical10 g/100mL
GelTopical0.02 g/1g
EmulsionTopical40 mg/1g
LotionTopical7.6 g/400mL
SolutionTopical20 mg/1mL
Cream; kit; lotionTopical
Cream4 %
LiquidTopical40 mg/1g
LiquidTopical40 mg/1mL
SolutionTopical40 mg/1mL
CreamTopical2000 mg
Cream; kit; liquid; lotionTopical
GelTopical2.0 g/100g
LotionTopical0.05 mg/2.5mL
LotionTopical1.95 1/100mL
OintmentTopical
CreamTopical3 g
GelTopical.6 g/30g
LotionTopical2 mg/100mL
LotionTopical0.015 g/1g
Cream2.000 g
Cream50 mg
Cream
LotionTopical0.04 g/1g
Cream0.1 mg/g
LotionTopical1.2 mL/60mL
LotionTopical3 g
CreamTopical2.0 g/100mL
CreamTopical0.02 mg/100mL
LiquidTopical20 mg/1mL
LiquidTopical2 g/100mL
LiquidTopical4 g/100mL
GelTopical4 %
GelTopical1 g/50g
CreamTopical0.02 g/1g
LiquidTopical2 mL/100mL
LiquidTopical8 g/100g
LiquidTopical0.02 g/1g
LiquidTopical0.08 g/1g
LotionTopical0.02 g/1g
CreamTopical4 mg/100mg
LotionTopical20 g/1mL
GelTopical20 mg/1g
CreamTopical19 mg/1g
LotionTopical
CreamCutaneous
CreamTopical0.1 mg/g
Cream40 MG/G
Cream50 MG/G
CreamTopical1 g/51g
GelTopical0.2 g/10mL
LiquidTopical2.0 g/100mL
LiquidTopical2.0 mL/100mL
LiquidTopical40 g/2mL
EmulsionTopical40 mg/1mL
EmulsionTopical0.04 g/1mL
EmulsionTopical0.04 mg/1mL
Emulsion; kitTopical
GelTopical2 %w/w
Cream4 %w/w
Cream2 %w/w
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8247395No2012-08-212022-10-22US flag
US8653053No2014-02-182022-10-25US flag
US7939516No2011-05-102025-05-04US flag
US7915243No2011-03-292026-03-22US flag

Properties

State
Not Available
Experimental Properties
PropertyValueSource
melting point (°C)170-171O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 891
boiling point (°C)285-287O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 891
water solubility6.72g/L at 20 deg CYalkowsky, S.H., He, Yan, Jain, P. Handbook of Aqueous Solubility Data Second Edition. CRC Press, Boca Raton, FL 2010, p. 254
logP0.59Hansch, C., Leo, A., D. Hoekman. Exploring QSAR - Hydrophobic, Electronic, and Steric Constants. Washington, DC: American Chemical Society., 1995., p. 20
Predicted Properties
PropertyValueSource
Water Solubility95.5 mg/mLALOGPS
logP0.71ALOGPS
logP1.37Chemaxon
logS-0.06ALOGPS
pKa (Strongest Acidic)9.68Chemaxon
pKa (Strongest Basic)-5.9Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area40.46 Å2Chemaxon
Rotatable Bond Count0Chemaxon
Refractivity30.02 m3·mol-1Chemaxon
Polarizability10.75 Å3Chemaxon
Number of Rings1Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-MS (2 TMS)GC-MSsplash10-0f79-2490000000-6b4fec222a3499d93790
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-03di-5900000000-954dc96d8e3eb85b8324
GC-MS Spectrum - EI-BGC-MSsplash10-03di-9800000000-c90fd4986fea9691ecbf
GC-MS Spectrum - EI-BGC-MSsplash10-03e9-9300000000-f8b11742557329691e8a
GC-MS Spectrum - GC-MSGC-MSsplash10-0f79-2490000000-6b4fec222a3499d93790
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-0f79-2690000000-7306adcc7121a11d67cc
Mass Spectrum (Electron Ionization)MSsplash10-03di-9500000000-1fa8477944a662535e76
MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)LC-MS/MSsplash10-03di-9600000000-e670ba090cb27367db12
MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)LC-MS/MSsplash10-01p6-9000000000-5fc32c7688c1612df1e7
MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)LC-MS/MSsplash10-000i-9000000000-c5853ce8ef225ea5c353
MS/MS Spectrum - EI-B (Unknown) , PositiveLC-MS/MSsplash10-03di-9800000000-c90fd4986fea9691ecbf
MS/MS Spectrum - , negativeLC-MS/MSsplash10-0a4i-0900000000-5635f0157cd37deb1121
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03di-2900000000-05be113033a709130eed
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0900000000-73ab94187f0e68978809
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-0900000000-a501d72f02551c71a437
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-02t9-9800000000-73a8d5d206d60d1bde47
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-6900000000-2b1d9f9fb564ce80d23b
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0f6x-9000000000-db18c6dc658c0fa2b5f0
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-02t9-9000000000-96df3ca43e39abf8d990
1H NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-116.5166973
predicted
DarkChem Lite v0.1.0
[M-H]-116.3961973
predicted
DarkChem Lite v0.1.0
[M-H]-116.4143973
predicted
DarkChem Lite v0.1.0
[M-H]-116.3864973
predicted
DarkChem Lite v0.1.0
[M-H]-118.13385
predicted
DeepCCS 1.0 (2019)
[M+H]+118.3818973
predicted
DarkChem Lite v0.1.0
[M+H]+120.0080973
predicted
DarkChem Lite v0.1.0
[M+H]+120.9533973
predicted
DarkChem Lite v0.1.0
[M+H]+119.6771973
predicted
DarkChem Lite v0.1.0
[M+H]+121.37287
predicted
DeepCCS 1.0 (2019)
[M+Na]+117.0347973
predicted
DarkChem Lite v0.1.0
[M+Na]+117.1250973
predicted
DarkChem Lite v0.1.0
[M+Na]+117.0778973
predicted
DarkChem Lite v0.1.0
[M+Na]+129.95375
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
This is a copper-containing oxidase that functions in the formation of pigments such as melanins and other polyphenolic compounds. Catalyzes the initial and rate limiting step in the cascade of reactions leading to melanin production from tyrosine (By similarity). In addition to hydroxylating tyrosine to DOPA (3,4-dihydroxyphenylalanine), also catalyzes the oxidation of DOPA to DOPA-quinone, and possibly the oxidation of DHI (5,6-dihydroxyindole) to indole-5,6 quinone (PubMed:28661582)
Specific Function
copper ion binding
Gene Name
TYR
Uniprot ID
P14679
Uniprot Name
Tyrosinase
Molecular Weight
60392.69 Da
References
  1. Patil S, Sistla S, Jadhav J: Interaction of small molecules with human tyrosinase: A surface plasmon resonance and molecular docking study. Int J Biol Macromol. 2016 Aug 9;92:1123-1129. doi: 10.1016/j.ijbiomac.2016.07.043. [Article]
  2. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Willebrand factor. Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. Integrins alpha-IIb/beta-3 and alpha-V/beta-3 recognize the sequence R-G-D in a wide array of ligands. Integrin alpha-IIb/beta-3 recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial surface. Fibrinogen binding enhances SELP expression in activated platelets (By similarity). ITGAV:ITGB3 binds to fractalkine (CX3CL1) and acts as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415, PubMed:24789099). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887). In brain, plays a role in synaptic transmission and plasticity. Involved in the regulation of the serotonin neurotransmission, is required to localize to specific compartments within the synapse the serotonin receptor SLC6A4 and for an appropriate reuptake of serotonin. Controls excitatory synaptic strength by regulating GRIA2-containing AMPAR endocytosis, which affects AMPAR abundance and composition (By similarity). ITGAV:ITGB3 act as a receptor for CD40LG (PubMed:31331973). ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP (PubMed:10640428)
Specific Function
cell adhesion molecule binding
Gene Name
ITGB3
Uniprot ID
P05106
Uniprot Name
Integrin beta-3
Molecular Weight
87056.975 Da
References
  1. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Integrin alpha-IIb/beta-3 is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. It recognizes the sequence R-G-D in a wide array of ligands. It recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial cell surface
Specific Function
extracellular matrix binding
Gene Name
ITGA2B
Uniprot ID
P08514
Uniprot Name
Integrin alpha-IIb
Molecular Weight
113375.96 Da
References
  1. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Activator
General Function
Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4
Specific Function
cysteinyl leukotriene receptor activity
Gene Name
CYSLTR1
Uniprot ID
Q9Y271
Uniprot Name
Cysteinyl leukotriene receptor 1
Molecular Weight
38540.55 Da
References
  1. Hazel BA, O'Connor A, Niculescu R, Kalf GF: Induction of granulocytic differentiation in a mouse model by benzene and hydroquinone. Environ Health Perspect. 1996 Dec;104 Suppl 6:1257-64. doi: 10.1289/ehp.961041257. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Product of
General Function
Essential for the degradation of glycogen in lysosomes (PubMed:14695532, PubMed:18429042, PubMed:1856189, PubMed:7717400). Has highest activity on alpha-1,4-linked glycosidic linkages, but can also hydrolyze alpha-1,6-linked glucans (PubMed:29061980)
Specific Function
alpha-1,4-glucosidase activity
Gene Name
GAA
Uniprot ID
P10253
Uniprot Name
Lysosomal alpha-glucosidase
Molecular Weight
105322.935 Da
References
  1. Wang M, Wang M, Zhang F, Su X: A ratiometric fluorescent biosensor for the sensitive determination of alpha-glucosidase activity and acarbose based on N-doped carbon dots. Analyst. 2020 Aug 24;145(17):5808-5815. doi: 10.1039/d0an01065k. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
Specific Function
antioxidant activity
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Albumin
Molecular Weight
69365.94 Da
References
  1. Sakurai M, Ohsako M, Nagano M, Nakamura C, Tsuzuki O, Ichikawa M, Matsumoto Y: [Effect of human serum albumin on transport of drugs through human erythrocyte membranes]. Yakugaku Zasshi. 1996 Aug;116(8):630-8. [Article]

Drug created at November 30, 2015 19:10 / Updated at October 11, 2024 18:19