175724-30-8Relevant articles and documents
Regulation of Macrocycle Shuttling Rates in [2]Rotaxanes by Amino-Acid Speed Bumps in Organic–Aqueous Solvent Mixtures
Douarre, Maxime,Martí-Centelles, Vicente,McClenaghan, Nathan D.,Pianet, Isabelle,Rossy, Cybille
, (2020)
A homologous series of two-station [2]rotaxanes incorporating amino-acid units in the molecular thread has been developed. The degenerate [2]rotaxanes exhibit amino-acid specific shuttling rates between two fumaric stations related to the steric factor associated to the amino-acid side chain, as demonstrated by variable-temperature 1H NMR spectroscopy and exchange spectroscopy (EXSY). This allows tuning of the macrocycle shuttling rate over 4 orders of magnitude, which has a relatively small solvent dependency.
Esterified dendritic TAM radicals with very high stability and enhanced oxygen sensitivity
Song, Yuguang,Liu, Yangping,Hemann, Craig,Villamena, Frederick A.,Zweier, Jay L.
, p. 1271 - 1276 (2013)
In this work, we have developed a new class of dendritic TAM radicals (TG, TdG, and dTdG) through a convergent method based on the TAM core CT-03 or its deuterated analogue dCT-03 and trifurcated Newkome-type monomer. Among these radicals, dTdG exhibits the best EPR properties with sharpest EPR singlet and highest O2 sensitivity due to deuteration of both the ester linker groups and the TAM core CT-03. Like the previous dendritic TAM radicals, these new compounds also show extremely high stability toward various reactive species owing to the dendritic encapsulation. The highly charged nature of these molecules resulting from nine carboxylate groups prevents concentration- dependent EPR line broadening at physiological pH. Furthermore, we demonstrate that these TAM radicals can be easily derivatized (e.g., PEGylation) at the nine carboxylate groups and the resulting PEGylated analogue dTdG-PEG completely inhibits the albumin binding, thereby enhancing suitability for in vivo applications. These new dendritic TAM radicals show great potential for in vivo EPR oximetric applications and provide insights on approaches to develop improved and targeted EPR oximetric probes for biomedical applications.
Tuning the pH-triggered self-assembly of dendritic peptide amphiphiles using fluorinated side chains
Appel, Ralph,Tacke, Sebastian,Klingauf, Jürgen,Besenius, Pol
, p. 1030 - 1039 (2015)
We report the synthesis of a series of anionic dendritic peptide amphiphiles of increasing hydrophobic character. By establishing state diagrams we describe their pH and ionic strength triggered self-assembly into supramolecular nanorods in water and highlight the impact of hydrophobic shielding in the supramolecular polymerisation process. Via the incorporation of fluorinated peptide side chains the pH-triggered monomer to polymer transition at physiological ionic strength is shifted from pH 5.0 to pH 7.4. We thereby show that compensating attractive non-covalent interactions and hydrophobic effects with repulsive electrostatic forces, a concept we refer to as frustrated growth, is a sensitive tool in order to manipulate one-dimensional supramolecular polymerisation processes in water.
An improved synthesis of a trifurcated newkome-type monomer and orthogonally protected two-generation dendrons
Cardona, Claudia M.,Gawley, Robert E.
, p. 1411 - 1413 (2002)
The one-step synthesis of amino-polyether tritert-butyl ester monomer 2, by condensation of TRIS with tert-butyl acrylate, is reported. The nitrogen of the monomer can be protected with a Cbz group; subsequent removal of the tert-butyl esters with formic
GALNAC-TGFBR1 INHIBITOR CONJUGATES FOR THE TREATMENT OF LIVER DISEASES
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Page/Page column 319-322, (2021/04/17)
Conjugates comprising GalNAc moiety and a TGFβR1 inhibitor are provided. In some embodiments, the conjugates are useful for the treatment of viral infections, cancer, and fibrosis.
TARGETED PLASMA PROTEIN DEGRADATION
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Page/Page column 172; 182-183, (2021/08/14)
The present invention is directed to the bifunctional compounds and the use of such bifunctional compounds to lower plasma levels of extracellular target molecules by lysosomal degradation. Such bifunctional compounds have a cell surface receptor ligand covalently linked to a ligand that is capable of binding to an extracellular target molecule (such as a ligand for a growth factor, a cytokine, a chemokine, a hormone, a neurotransmitter, a capsid, a soluble receptor, an extracellular secreted protein, an antibody, a lipoprotein, an exosome, a virus, a cell, or a plasma membrane protein), where the cell surface receptor is associated with receptor mediated endocytosis, including asialoglycoprotein receptor (ASGPR) mediated lysosomal degradation and mannose-6-phosphate (M6PR) mediated lysosomal degradation. Pharmaceutical compositions comprising such bifunctional compounds and methods of treating a disease or disorder mediated by an extracellular molecule using such bifunctional compounds are also provided herein.