Drug Information
Drug (ID: DG00594) and It's Reported Resistant Information
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
African trypanosomiasis [ICD-11: 1F51]
Drug Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: NADH dehydrogenase [ubiquinone] flavoprotein 1 (TbAT1) | [1] | |||
Molecule Alteration | Expression | Down-regulation |
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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
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