Drug (ID: DG00594) and It's Reported Resistant Information
Name
Melamine-based arsenicals
Drug Resistance Disease(s)
Disease(s) with Resistance Information Validated by in-vivo Model for This Drug (1 diseases)
African trypanosomiasis [ICD-11: 1F51]
[1]
Target . NOUNIPROTAC [1]
Type(s) of Resistant Mechanism of This Drug
  UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-01: Infectious/parasitic diseases
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African trypanosomiasis [ICD-11: 1F51]
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Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: NADH dehydrogenase [ubiquinone] flavoprotein 1 (TbAT1) [1]
Molecule Alteration Expression
Down-regulation
Resistant Disease African trypanosomiasis [ICD-11: 1F51.0]
Experimental Note Discovered Using In-vivo Testing Model
In Vitro Model Trypanosoma brucei strain 5691
Mechanism Description Reduced uptake and cross-resistance were apparently explained by the findings that melamine-based arsenicals and diamidines are imported into trypanosomes by the same transporter, and that this transporter is defective in drug-resistant cells. The transporter was called P2 (purine transporter 2) as its physiological substrates are adenine and adenosine, both of which compete with melarsoprol for uptake and can protect trypanosomes from melarsoprol-induced lysis.
References
Ref 1 Drug resistance in African trypanosomiasis: the melarsoprol and pentamidine story .Trends Parasitol. 2013 Mar;29(3):110-8. doi: 10.1016/j.pt.2012.12.005. Epub 2013 Jan 30. 10.1016/j.pt.2012.12.005

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