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Badarau E.,Aston University | Badarau E.,European Institute of Chemistry and Biology | Wang Z.,Aston University | Rathbone D.L.,Aston University | And 6 more authors.
Chemistry and Biology

Potent-selective peptidomimetic inhibitors of tissue transglutaminase (TG2) were developed through a combination of protein-ligand docking and molecular dynamic techniques. Derivatives of these inhibitors were made with the aim of specific TG2 targeting to the intra- and extracellular space. A cell-permeable fluorescently labeled derivative enabled detection of in situ cellular TG2 activity in human umbilical cord endothelial cells and TG2-transduced NIH3T3 cells, which could be enhanced by treatment of cells with ionomycin. Reaction of TG2 with this fluorescent inhibitor in NIH3T3 cells resulted in loss of binding of TG2 to cell surface syndecan-4 and inhibition of translocation of the enzyme into the extracellular matrix, with a parallel reduction in fibronectin deposition. In human umbilical cord endothelial cells, this same fluorescent inhibitor also demonstrated a reduction in fibronectin deposition, cell motility, and cord formation in Matrigel. Use of the same inhibitor in a mouse model of hypertensive nephrosclerosis showed over a 40% reduction in collagen deposition. © 2015 Elsevier Ltd All rights reserved. Source

McCusker D.,European Institute of Chemistry and Biology | McCusker D.,Institut Universitaire de France | Kellogg D.R.,University of California at Santa Cruz
Current Opinion in Cell Biology

Growth of the plasma membrane is as fundamental to cell reproduction as DNA replication, chromosome segregation and ribosome biogenesis, yet little is known about the underlying mechanisms. Membrane growth during the cell cycle requires mechanisms that control the initiation, location, and extent of membrane growth, as well as mechanisms that coordinate membrane growth with cell cycle progression. Recent experiments have established links between membrane growth and core cell cycle regulators. Further analysis of these links will yield insights into conserved and fundamental mechanisms of cell growth. A better understanding of the post-Golgi pathways by which membrane growth occurs will be essential for future progress. © 2012. Source

Harmand L.,CNRS Institute of Molecular Sciences | Cadet S.,CNRS Institute of Molecular Sciences | Kauffmann B.,European Institute of Chemistry and Biology | Scarpantonio L.,CNRS Institute of Molecular Sciences | And 5 more authors.
Angewandte Chemie - International Edition

PET cat. While the copper(II) tren ketoprofenate precatalyst 1 (see picture) is inactive at room temperature in methanol, it is quantitatively and rapidly reduced to its cuprous state upon light irradiation to provide a highly reactive click catalyst. By simply introducing air into the reaction medium the catalysis can be switched off and then switched on again by bubbling argon followed by irradiation. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source

Grosjean A.,CNRS Laboratory of Condensed Matter Chemistry, Bordeaux | Daro N.,CNRS Laboratory of Condensed Matter Chemistry, Bordeaux | Kauffmann B.,European Institute of Chemistry and Biology | Kaiba A.,CNRS Laboratory of Condensed Matter Chemistry, Bordeaux | And 2 more authors.
Chemical Communications

The first single crystal-based description of a spin transition compound from the patented [Fe(Rtrz) 3]X 2·nH 2O family is reported, properly the compound with Rtrz = 4-amino-1,2,4-triazole, X = NO 3 and n = 2. This study definitively proves the 1-D polymeric nature of the crystal structure and allows a description of the [Fe(Rtrz) 3] chains, as well as of the anions and water implementation within the crystal lattice opening the possibility of subsequent investigations of the structure-property correlation within this peculiar family of spin transition compounds. © 2011 The Royal Society of Chemistry. Source

Azema L.,French Institute of Health and Medical Research | Azema L.,University of Bordeaux 1 | Bathany K.,University of Bordeaux 1 | Bathany K.,European Institute of Chemistry and Biology | And 2 more authors.

Stability leads to selection: Cationic appending groups on a triplex-forming oligonucleotide (TFO) designed to bind a DNA target can be rapidly selected from a small library of various amines and polyamines for their capacity to stabilize triple-helix formation. © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source

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