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“The … of suramin was time-dependent and reduced by more … 90% when incubated in the presence of albumin or at 4 degrees C. Suramin uptake was also inhibited when incubated in the presence of filipin and digitonin, both potent cholesterol-binding agents, but not in the presence of probenecid.”
“The deprotonation of histidine and other positively charged residues taking part in salt bridges between suramin and albumin is, in all probability, the main cause of the decrease in affinity of suramin for albumin as the pH is raised from 6 to 9.”
“By means of the Linderstrøm-Lang equation for electrostatic interaction and a two-state model for the N-B transition of albumin, evidence is obtained of a link of the pH dependent binding behaviour of suramin to albumin and the neutral-to-base transition of albumin.”
“Thirdly, preincubation of suramin with albumin alone abrogates drug uptake, consistent with accumulation of the drug via a trypanosomal LDL-receptor and not fluid phase endocytosis, the route of entry for serum albumin [6].”