Guarino G, Strollo F, Carbone L, Della Corte T, Letizia M, Marino G, et al
Chen, J., Cui, L., Lu, S
The down-regulation of influx transporters of 6-mercaptopurine including SLC28A2 (CNT2), SLC28A3 (CNT3), SLC29A1 (ENT1) and SLC29A2 (ENT2) has been shown to render lymphocyte-derived cell-lines resistant to thiopurines, owing to decreased uptake of thiopurine metabolites into the cells ( thiopurine cellular circulation , whereby thiopurine nucleotides extruded by ABCC4 will be salvaged by an extracellular enzyme NT5E through hydrolysis into nucleosides, before being transported back into the cells by nucleoside transporters ( Finally, several genetic markers and enzymes have been reported to cause thiopurine resistance, but the mechanisms are obscure
CJC-1295 with DAC carries a Drug Affinity Complex that binds it to albumin, extending half-life to 5.8-8.1 days (Teichman 2006, JCEM)
Morali G, Polatti F, Metelitsa EN, Mascarucci P, Magnani P, Marre GB
10.1194/jlr.M090969 103 LiY.ZhouY.SiN.HanL.RenW.XinS.et al (2017)