Molecule Information

General Information of the Molecule (ID: Mol02088)

• Name: Aquaporin 2/3 (AQP2/3) ,Trypanosoma
• Synonyms: AQP2/3
• Molecule Type: Protein
• Gene Name: AQP2/3
• Sequence:
  MQSQPDNVAYPMELQAVNKDGTVEVRVQGNDDSSNRKHEVAEAQEEVPGGINFWAPRELR
  LNYRDYMGELLGTFVLLFMGNGVVATVIIDGKLGFLSITLGWGIAVTMALYVSLGISSGH
  LNPAVTVGNAVFGDFPWRKVPGYIAAQMLGAFLGAACAYGVFADLLKAHGGGELIAFGEK
  GIAWVFAMYPAEGNGIFYPIFAELISTAVLLLCVCGIFDPNNSPAKGYETVAIGALVFVM
  VNNFGLASPLAMNPSLDFGPRVFGAILLGGEVFSHANYYFWVPLVVPFFGAILGLFLYKY
  FLPH
• Uniprot ID: A0A0H4BF23_9TRYP

Kingdom: N.A.
Phylum: Euglenozoa
Class: Kinetoplastea
Order: Trypanosomatida
Family: Trypanosomatidae
Genus: .
Species: Trypanosoma

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

Melarsoprol

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Disease Class: African trypanosomiasis [1]

• Resistant Disease: African trypanosomiasis [ICD-11: 1F51.0]
• Resistant Drug: Melarsoprol
• Molecule Alteration: Expression; Up-regulation
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: African trypanosomiasis strain; .
• Mechanism Description: The laboratory studies above showed that uptake of both melarsoprol and pentamidine by trypanosomes is under the control of both the P2 adenosine transporter and AQP2. These studies were extended to additional T. b. brucei, T. b. gambiense, and T. b. rhodesiense cross-resistant laboratory-selected strains, which all revealed either chimeric AQP2/3 genes or complete loss of AQP2.

Pentamidine

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Disease Class: African trypanosomiasis [1]

• Resistant Disease: African trypanosomiasis [ICD-11: 1F51.0]
• Resistant Drug: Pentamidine
• Molecule Alteration: Expression; Up-regulation
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: African trypanosomiasis strain; .
• Mechanism Description: The laboratory studies above showed that uptake of both melarsoprol and pentamidine by trypanosomes is under the control of both the P2 adenosine transporter and AQP2. These studies were extended to additional T. b. brucei, T. b. gambiense, and T. b. rhodesiense cross-resistant laboratory-selected strains, which all revealed either chimeric AQP2/3 genes or complete loss of AQP2.

References

• Ref 1: Melarsoprol Resistance in African Trypanosomiasis .Trends Parasitol. 2018 Jun;34(6):481-492. doi: 10.1016/j.pt.2018.04.002. Epub 2018 Apr 25. 10.1016/j.pt.2018.04.002