TY - JOUR
T1 - Folate-targeted therapeutic and imaging agents for cancer
AU - Low, Philip
AU - Kularatne, Sumith Anurasiri
PY - 2009/6/1
Y1 - 2009/6/1
N2 - Cancer therapies that exploit targeting ligands to deliver attached cytotoxic drugs selectively to malignant cells are currently receiving significant attention. While antibody-targeted drugs have been the first to enter the clinic, recent studies demonstrate that the vitamin folic acid can also be used to deliver attached imaging and therapeutic agents selectively to malignant cells in both animal tumor models and human cancer patients. Thus, folate conjugates bind to folate receptors that are overexpressed on ∼40% of human cancers and mediate internalization of their attached drugs by receptor-mediated endocytosis. With the use of proper linkers, folate-targeted drugs can be released inside their target cells where they can perform their desired cytotoxic functions. Based on this strategy, six folate-targeted drugs are currently in human clinical trials.
AB - Cancer therapies that exploit targeting ligands to deliver attached cytotoxic drugs selectively to malignant cells are currently receiving significant attention. While antibody-targeted drugs have been the first to enter the clinic, recent studies demonstrate that the vitamin folic acid can also be used to deliver attached imaging and therapeutic agents selectively to malignant cells in both animal tumor models and human cancer patients. Thus, folate conjugates bind to folate receptors that are overexpressed on ∼40% of human cancers and mediate internalization of their attached drugs by receptor-mediated endocytosis. With the use of proper linkers, folate-targeted drugs can be released inside their target cells where they can perform their desired cytotoxic functions. Based on this strategy, six folate-targeted drugs are currently in human clinical trials.
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U2 - 10.1016/j.cbpa.2009.03.022
DO - 10.1016/j.cbpa.2009.03.022
M3 - Review article
C2 - 19419901
AN - SCOPUS:67649849650
SN - 1367-5931
VL - 13
SP - 256
EP - 262
JO - Current Opinion in Chemical Biology
JF - Current Opinion in Chemical Biology
IS - 3
ER -