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1.  One-step and one-pot-two-step radiosynthesis of cyclo-RGD-18F-aryltrifluoroborate conjugates for functional imaging 
Arylboronates capture aqueous 18F-fluoride in one step to afford a highly polar 18F-labeled aryltrifluoroborate anion (18F-ArBF3 -) that clears rapidly in vivo. To date however, there is little data to show that a ligand labeled with a prosthetic 18F-ArBF3 - will provide functional images. RGD, a high-affinity ligand for integrins that are present on the cell surface of numerous tumors, has been labeled in many formats with many different radionuclides, and as such represents a well-established ligand that can be used to evaluate new labeling methods. Herein we have labeled RGD with a prosthetic 18F-ArBF3 - via two approaches for the first time: 1) a RGD-boronate bioconjugate is directly labeled in one step and 2) an alkyne-modified arylborimidine is first converted to the corresponding 18F-ArBF3 - which is then conjugated to an RGD-azide via Cu+-mediated [2+3] dipolar cycloaddition in one pot over two steps. RGD-18F-ArBF3 - bionconjugates were produced in reasonable radiochemical yields using low amounts of 18F-fluoride anion (10-50 mCi). Despite relatively low specific activities, good tumor images are revealed in each case.
PMCID: PMC3545361  PMID: 23342300
One-step 18F-labeling; click labeling; RGD; PET imaging
2.  Design of “smart” probes for optical imaging of apoptosis 
Apoptosis is a mode of programmed cell death in multicellular organisms and plays a central role in controlling embryonic development, growth and differentiation and monitoring the induction of tumor cell death through anticancer therapy. Since the most effective chemotherapeutics rely on apoptosis, imaging apoptotic processes can be an invaluable tool to monitor therapeutic intervention and discover new drugs modulating apoptosis. The most attractive target for developing specific apoptosis imaging probes is caspases, crucial mediators of apoptosis. Up to now, various optical imaging strategies for apoptosis have been developed as an easy and economical modality. However, current optical applications are limited by poor sensitivity and specificity. A subset of molecular imaging contrast agents known as “activatable” or “smart” molecular probes allow for very high signal-to-background ratios compared to conventional targeted contrast agents and open up the possibility of imaging intracellular targets. In this review, we will discuss the unique design strategies and applications of activatable probes recently developed for fluorescence and bioluminescence imaging of caspase activity.
PMCID: PMC3327302  PMID: 22514789
Activatable probes; apoptosis; bioluminescence; caspases; optical imaging
3.  Design of “smart” probes for optical imaging of apoptosis 
Apoptosis is a mode of programmed cell death in multicellular organisms and plays a central role in controlling embryonic development, growth and differentiation and monitoring the induction of tumor cell death through anticancer therapy. Since the most effective chemotherapeutics rely on apoptosis, imaging apoptotic processes can be an invaluable tool to monitor therapeutic intervention and discover new drugs modulating apoptosis. The most attractive target for developing specific apoptosis imaging probes is caspases, crucial mediators of apoptosis. Up to now, various optical imaging strategies for apoptosis have been developed as an easy and economical modality. However, current optical applications are limited by poor sensitivity and specificity. A subset of molecular imaging contrast agents known as “activatable” or “smart” molecular probes allow for very high signal-to-background ratios compared to conventional targeted contrast agents and open up the possibility of imaging intracellular targets. In this review, we will discuss the unique design strategies and applications of activatable probes recently developed for fluorescence and bioluminescence imaging of caspase activity.
PMCID: PMC3327302  PMID: 22514789
Activatable probes; apoptosis; bioluminescence; caspases; optical imaging

Results 1-3 (3)