Drug Transporter (DT) Information

General Information of DT
DT ID DTD0051
Gene Name ABCB5
Protein Name ATP-binding cassette sub-family B member 5
Gene ID
340273
UniProt ID
Q2M3G0
TCDB ID
3.A.1.201.13
3D Structure

Modelled DT Structure

Method:homology modeling

Template PDB:6QEX_A

Identity:55.788%

Minimized Score:-2936.873 kcal/mol

Detail: Structure Info

Synonyms ABCB5; ABCB5 P-gp; ABCB5alpha; ABCB5beta; EST422562; P-glycoprotein ABCB5
DT Family ATP-Binding Cassette (ABC) Superfamily
Multidrug Resistance Exporter (MDR) Family (ABCB)
Tissue Specificity Expressed by CD133-expressing progenitor cellsamong epidermal melanocytes (at protein level). Widely expressedwith specific expression in pigment cells. Highly expressed inseveral malignant tissues: highly expressed in clinical melanomas,with low expression in normal skin. In melanoma, marks malignantmelanoma-initiating cells (MMIC), in which clinical virulenceresides as a consequence of unlimited self-renewal capacity,resulting in inexorable tumor progression and metastasis. Alsohighly expressed in a number of leukemia cells. Expressed in basallimbal epithelium.
Function This drug efflux transporter present in a number of stem cells that acts as a regulator of cellular differentiation. Able to mediate efflux from cells of the rhodamine dye and of the therapeutic drug doxorubicin.
Disease(s) Non-small cell lung cancer [ICD-11:2C25]
Rheumatoid arthritis [ICD-11:FA20]
Variability Data of This Drug Transporter (DT)

Regulatory Variability Data of This DT (VARIDT 4.0)

(α) Tissue Distribution Level of ATP-binding cassette sub-family B member 5
Tissue Distribution Level (TD)

(β) Cell Distribution Level of ATP-binding cassette sub-family B member 5
Cell Distribution Level (CD)

(γ) Organelle Distribution Level of ATP-binding cassette sub-family B member 5
Organelle Distribution Level (Subc)

Regulatory Variability Data of This DT

(β) Post-translational Modification of ATP-binding cassette sub-family B member 5
Post-translational Modification (PTM)

(γ) Transcriptional Regulation of ATP-binding cassette sub-family B member 5
Transcriptional Regulation (TSR)

(δ) Epigenetic Regulation of ATP-binding cassette sub-family B member 5
Epigenetic Regulation (EGR)

(ε) Exogenous Modulation of ATP-binding cassette sub-family B member 5
Exogenous Modulation (EGM)

Structural Variability Data of This DT

(α) Mutation-induced Structural Variation
Mutation-induced Structural Variation (MSV)

(β) Inter-species Structural Differences
Inter-species Structural Differences (ISD)

(δ) Xenobiotics-regulated Structural Variability
Xenobiotics-regulated Structural Variability (XSV)

General Variability Data of This DT

(α) Genetic Polymorphisms of ATP-binding cassette sub-family B member 5
Genetic Polymorphisms of This DT (GPD)

(β) Disease-specific Protein Abundances of ATP-binding cassette sub-family B member 5
Disease-specific Protein Abundances of This DT (DPAD)

(γ) Species- and Tissue-specific DT Abundances
Species/Tissue-specific Protein Abundances of This DT (S/TPAD)
Molecular Transporting Profile of This DT

Full List of Drug(s) Transported by This DT

 Approved Drug

 Click to Show/Hide the Full List of Drug:           3 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
Brigatinib
 Approved Drug Info Non-small cell lung cancer 2C25 [1]
Doxorubicin
 Approved Drug Info Leukemia 2A60-2B33 [2]
Fostamatinib
 Approved Drug Info Rheumatoid arthritis FA20 [3]

Endogenous Metabolites (EMs) Handled by This DT

 Endogenous Metabolites (EMs)

 Click to Show/Hide the Full List of EMs:           4 EMs in Total
EM Name PubChem CID Detail Experimental Material Ref
Glycerophosphocholine
657272
EM Info Identified using ABCB5 knockdown G3361 melanoma cells [4]
Glycerophosphoethanolamine
123874
EM Info Identified using ABCB5 knockdown G3361 melanoma cells [4]
Phospholipid degradation product unspecific N.A. EM Info Identified using ABCB5 knockdown G3361 melanoma cells [4]
Water-soluble metabolite unspecific N.A. EM Info Identified using ABCB5 knockdown G3361 melanoma cells [4]
References
1 NDA/BLA Multidisciplinary Review and Evaluation of ALUNBRIG (brigatinib) From FDA.
2 ABCB5-mediated doxorubicin transport and chemoresistance in human malignant melanoma. Cancer Res. 2005 May 15;65(10):4320-33.
3 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB12010)
4 Expression of Cell-Surface Marker ABCB5 Causes Characteristic Modifications of Glucose, Amino Acid and Phospholipid Metabolism in the G3361 Melanoma-Initiating Cell Line. PLoS One. 2016 Aug 25;11(8):e0161803.

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