General Information of the Molecule (ID: Mol01162)
Name
ATP-binding cassette sub-family B5 (ABCB5) ,Pichia pastoris
Molecule Type
Protein
Gene Name
P-gp
        Click to Show/Hide the Complete Species Lineage
Kingdom: Fungi
Phylum: Ascomycota
Class: Saccharomycetes
Order: Saccharomycetales
Family: Phaffomycetaceae
Genus: Komagataella
Species: Komagataella pastoris
Type(s) of Resistant Mechanism of This Molecule
  IDUE: Irregularity in Drug Uptake and Drug Efflux
Drug Resistance Data Categorized by Drug
Approved Drug(s)
2 drug(s) in total
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Loperamide
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Irregularity in Drug Uptake and Drug Efflux (IDUE) Click to Show/Hide
Disease Class: Pain [1]
Sensitive Disease Pain [ICD-11: MG30.0]
Sensitive Drug Loperamide
Molecule Alteration Expression
Down-regulation
Experimental Note Revealed Based on the Cell Line Data
Experiment for
Molecule Alteration
ATPase activity assay
Mechanism Description P-glycoprotein (Pgp) is a multidrug resistance transporter that limits the penetration of a wide range of neurotherapeutics into the brain including opioids. Pgp-knockout mice had more than a 10-fold higher level of loperamide in their brains than wild-type. Both rats and humans have shown elevated levels of loperamide in the presence of the Pgp-specific inhibitor cyclosporine A.
Methadone
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Irregularity in Drug Uptake and Drug Efflux (IDUE) Click to Show/Hide
Disease Class: Pain [1]
Sensitive Disease Pain [ICD-11: MG30.0]
Sensitive Drug Methadone
Molecule Alteration Expression
Down-regulation
Experimental Note Revealed Based on the Cell Line Data
Experiment for
Molecule Alteration
ATPase activity assay
Mechanism Description P-glycoprotein (Pgp) is a multidrug resistance transporter that limits the penetration of a wide range of neurotherapeutics into the brain including opioids. Pgp-knockout mice had more than a 10-fold higher level of loperamide in their brains than wild-type. Both rats and humans have shown elevated levels of loperamide in the presence of the Pgp-specific inhibitor cyclosporine A.
References
Ref 1 A Conformationally Gated Model of Methadone and Loperamide Transport by P-Glycoprotein. J Pharm Sci. 2018 Jul;107(7):1937-1947. doi: 10.1016/j.xphs.2018.02.019. Epub 2018 Feb 28.

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