@misc{10481/44744, year = {2016}, url = {http://hdl.handle.net/10481/44744}, abstract = {The in situ detection of caspase-3 activity has applications in the imaging and monitoring of multiple pathologies, notably cancer. A series of cell penetrating FRET-based fluorogenic substrates were designed and synthesised for the detection of caspase-3 in live cells. A variety of modifications of the classical caspase-3 and caspase-7 substrate sequence Asp-Glu-Val-Asp were carried out in order to increase caspase-3 affinity and eliminate caspase-7 cross-reactivity. To allow cellular uptake and good solubility, the substrates were conjugated to a cationic peptoid. The most selective fluorogenic substrate 27, FAM-Ahx-Asp-Leu-Pro-Asp-Lys(MR)-Ahx, conjugated to the cell penetrating peptoid at the C-terminus, was able to detect and quantify caspase-3 activity in apoptotic cells without cross-reactivity by caspase-7.}, organization = {This work was supported by the Ramon Areces and Caja Madrid Foundations to AMPL and Spanish Ministry of Economy and Competitiveness to MLSG (graduate student fellowships FPI BES-2010-030257 and EEBB-I-13-07131).}, publisher = {Public Library of Science (PLOS)}, keywords = {Apoptosis}, keywords = {Fluorescence imaging}, keywords = {Flow cytometry}, keywords = {Cross reactivity}, keywords = {Peptide synthesis}, keywords = {Apoptotic signaling cascade}, keywords = {High performance liquid chromatography}, title = {Fluorogenic Substrates for In Situ Monitoring of Caspase-3 Activity in Live Cells}, doi = {10.1371/journal.pone.0153209}, author = {Pérez-López, Ana M. and Soria-Gila, M. Lourdes and Marsden, Emma R. and Lilienkampf, Annamaria and Bradley, Mark}, }