32085-73-7Relevant articles and documents
Synthesis of conformationally constrained peptidomimetics using multicomponent reactions
Scheffelaar, Rachel,Klein Nijenhuis, Roel A.,Paravidino, Monica,Lutz, Martin,Spek, Anthony L.,Ehlers, Andreas W.,De Kanter, Frans J. J.,Groen, Marinus B.,Orru, Romano V. A.,Ruijter, Eelco
, p. 660 - 668 (2009)
A novel modular synthetic approach toward constrained peptidomimetics is reported. The approach involves a highly efficient three-step sequence including two multicomponent reactions, thus allowing unprecedented diversification of both the peptide moietie
A paramagnetic chemical exchange-based MRI probe metabolized by cathepsin D: Design, synthesis and cellular uptake studies
Suchy, Mojmir,Ta, Robert,Li, Alex X.,Wojciechowski, Filip,Pasternak, Stephen H.,Bartha, Robert,Hudson, Robert H.E.
experimental part, p. 2560 - 2566 (2010/07/16)
Overexpression of the aspartyl protease cathepsin D is associated with certain cancers and Alzheimer's disease; thus, it is a potentially useful imaging biomarker for disease. A dual fluorescence/MRI probe for the potential detection of localized cathepsin D activity has been synthesized. The probe design includes both MRI and optical reporter groups connected to a cell penetrating peptide by a cathepsin D cleavable sequence. This design results in the selective intracellular deposition (determined fluorimetrically) of the MRI and optical reporter groups in the presence of overexpressed cathepsin D. The probe also provided clearly detectable in vitro MRI contrast by the mechanism of paramagnetic chemical exchange effects (OPARACHEE). The Royal Society of Chemistry 2010.
