Specific binding of folate conjugated PGA to FR-positive tumor cells / 中国药理学通报

ABSTRACT

Aim To investigate the specific binding of folate conjugated PGA to FR-positive tumor cells.Method Folate-PGA and PGA were radiolabeled with 125I by the Iodogen method to examine the binding of PGA to FR positive HeLa cells and SKOV3 cells, or FR negative A549 cells. Results 125I-folate-PGA showed specific bound to HeLa cells and SKOV3 cells; Scatchard analysis of the data estimated the Kd of binding to be 0.11 nmol?L-1 and 0.25 nmol?L-1 respectively. 125I-folate-PGA showed virtually little specific binding to A549 cells which lack folate receptors. Conclusions folate-PGA displayed high affinity and good targeting activities for FR-positive tumor cells and the data warranted further studies for enzyme prodrug therapy.