Receptor targeting to cancer cells

Left: CT-SPECT image of mouse 4 hours following tail vein injection of 111In-DTPA-folate, a radioimaging agent that binds to folate receptors over-expressed on cancer cells (see solid KB cell tumors on both shoulders).  Kidneys also capture any folate-targeted imaging agent that is filtered into the urine and transcytose it from the urine back to the blood.  Folate-targeted drugs are therefore not toxic to kidneys.  Image courtesy of Cristina Mueller. Right: Whole-body imaging of a balB/C mouse with a KB tumor implantation of the shoulder with intravenous injection of fluorescent folate-Dylight 680 conjugates.

 

 

 

 

 

 

 

 

 

Folate receptor-targeted radioimaging in human subjects with breast (Left), brain tumors (Middle) and ovarian cancer (Right).

 

 

 

 

 

 

 

 

 

Trafficking of folate-rhodamine containing endosomes on GFP-abeled microtubules in cancer cells (Left), cover of Biophysics Journal, 2007; a video that recorded the endocytosis of folate-rhodamine conjugates captured in real time.

Optical imaging of liver metastases labeled by tail vein injection of folate-FITC;

 

 

 

 

 

 

 

Images of human prostate tumors with prostate targeting

ligand-99mTc conjugate.  Image on right shows complete
competition upon addition of excess free ligand

Z-series video of high dose of folate-rhodamine shows uptake in every cancer cell but not in any normal cells

Cancer cell uptakes folate conjugates cho-clst-12-08-2004.avi