An image contrast agent selectively activated by prostate specific antigen.
A family of image contrast agent conjugates designed to undergo enzymatic activation has been synthesized. The agents underwent activation both with enzymatically active prostate specific antigen (PSA) and alpha-chymotrypsin, releasing free fluorophore via cleavage of a three-component system. A hexapeptide derivative showed exclusive activation by PSA and constitutes a method for tracking PSA activity in vitro.
Jones
Graham B
GB
Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, USA. gr.jones@neu.edu
Crasto
Curtis F
CF
Mathews
Jude E
JE
Xie
Longfei
L
Mitchell
Miguel O
MO
El-Shafey
Ahmed
A
D'Amico
Anthony V
AV
Bubley
Glenn J
GJ
D002918:Chymotrypsin / Q000737:chemistry; D003287:Contrast Media / Q000737:chemistry*; D004789:Enzyme Activation; D009682:Magnetic Resonance Spectroscopy; D017430:Prostate-Specific Antigen / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization
D003287:Contrast Media; D002918:Chymotrypsin; D017430:Prostate-Specific Antigen