Nucleic Acid-Templated Energy Transfer Leading to a Photorelease Reaction and its Application to a System Displaying a Nonlinear Response, M. Röthlingshöfer, G. Gorska. N. Winssinger, J. Am. Chem. Soc.2011, 133, 18110–18113.
The photo-cleavage of nitrobenzyl type linker (NPPOC) at 405 nm wavelength was enabled by nucleic acid templated energy transfer from a sentitizer (thioxanthenone) to the linker. This strategy was used to release pro-fluorescent rhodamine which facilitated reaction monitoring via fluorescence measur
Synthesis of deguelin-biotin conjugates and investigation into deguelin's interactions, J. Garcia, S. Barluenga, K. Gorska, F. Sasse, N. Winssinger, Bioorg. Med. Chem.2012, 20, 672-680.
Deguelin, a rotenoid, has emerged as anattractive pharmacophore for chemoprenvention showing in vivo activity in several xenografts. Recently, several lines of evidence have suggested its mode of action may involve inhibition of HSP90, however biding in a different mode than known pharmacophores. To
Selection of a Synthetic Glycan Oligomer from a Library of DNA-Templated Fragments Against DC-SIGN and Inhibition of HIV gp120 Binding to Dendritic Cells, M. Ciobanu, K.-T. Huang, J.-P. Daguer, S. Barluenga, O. Chaloin, E. Schaeffer, C. G. Mueller, D.A. Mitchell, Nicolas Winssinger, ChemCommun, 2011, 47, 9321-9323
We report the synthesis of a nucleic acid-encoded carbohydrate library, its combinatorial self-assembly into 37485 pairs and a screen against DC-SIGN leading to the identification of consensus ligand motifs. A prototypical example from the selected pairs was shown to have enhanced binding. A dendrim
Rapid Fluorescence Imaging of miR-21 in Cells Using Templated Staudinger Reaction, K. Gorska, I. Keklikoglou, U. Tschulena, N. Winssinger Chem. Sci.2011, 2, 1969-1975.
It is generally accepted that microRNAs (miRNAs) play a crucila role in gene expression regulation and that their aberrant expression is intimately linked with pathologies, most notably cancer. There is thus significant interest in detecting and quantifying these important regulators. Herein, we rep
Translating Instructions Into Function by Nucleic Acid Programmed Self-Assembly, N. Winssinger, Actualité Chimique 2011 , 348 , 42-48
The predictable nature of nucleic acid hybridization offers a simple platform to program assemblies with emerging function. The review will highlight some examples from our laboratory towards the use of this concept in chemical biology. These developments capitalize on peptide nucleic acids (PNAs),
Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors, Emeline Leproult, Sofia Barluenga, Dino Moras, Jean-Marie Wurtz, and Nicolas Winssinger*, J. Med. Chem. 2011 , 54 , 1347-55
Kinases have emerged as one of the most prolific therapeutic targets. An important criterion in the therapeutic success of inhibitors targeting the nucleotide binding pocket of kinases is the inhibitor residence time. Recently, covalent kinase inhibitors have attracted attention since they confer te
DNA-templated release Q5 of functional molecules with an Q1 azide-reduction-triggered immolative linker, Katarzyna Gorska, Alex Manicardi, Sofia Barluenga and Nicolas Winssinger, Chem Commun. 2011, 47, 4364-67.
Nucleic acid templated reactions have attracted significant attention for nucleic acid sensing. Herein we report a general design which extends the potential of nucleic acid templated reactions to unleash the function of a broad diversity of small molecules such as a transcription factor agonist, a
DNA-templated combinatorial assembly of small molecule fragments amenable to selection/amplification cycles, Jean Pierre Daguer, Mihai Ciobanu, Susana Alvarez, Sofia Barluenga and Nicolas Winssinger, Chem. Sci., 2011 , 2 625-632
The discovery of small molecule probes which selectively modulate biological pathways is a cornerstone in the development of new therapeutics. Progress in our ability to access libraries of biologically relevant small molecules in conjunction with streamlined sc
Combinatorial Self-Assembly of Glycan Fragments into Microarrays, Kuo-Ting Huang, Katarzyna Gorska, Suzana Alvarez, Sofia Barluenga, Nicolas Winssinger ChemBioChem, 2011, 12 , 56–60.
Glycan arrays have had a tremendous impact in glycoscience. While a number of different chemistries can be used to immobilize the carbohydrate, a
The molecular chaperone Hsp90 is required for meiotic progression of spermatocytes beyond pachytene in the mouse, Grad, I., Cederroth, C. R., Walicki, J., Grey, C., Barluenga, S., Winssinger, N., De Massy, B., Nef, S., and Picard, D. PLoS ONE, 2010, 5, e15770.
The molecular chaperone Hsp90 has been found to be essential for viability in all tested eukaryotes, from the budding yeast to Drosophila. In mammals, two genes encode the two highly similar and functionally largely redundant isoforms Hsp90α and Hsp90β. Although they are co
