191731-21-2Relevant articles and documents
Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside
Anderluh, Marko,Girardi, Benedetta,Leffler, Hakon,Manna, Martina,Mravljak, Janez,Nilsson, Ulf J.,Ricklin, Daniel,Schwardt, Oliver,Van Klaveren, Sjors,Jakopin, ?iga,Toma?i?, Tihomir
supporting information, (2021/10/08)
Galectin-8 has gained attention as a potential new pharmacological target for the treatment of various diseases, including cancer, inflammation, and disorders associated with bone mass reduction. To that end, new molecular probes are needed in order to better understand its role and its functions. Herein we aimed to improve the affinity and target selectivity of a recently published galectin-8 ligand, 3-O-[1-carboxyethyl]-β-d-galactopyranoside, by introducing modifications at positions 1 and 3 of the galactose. Affinity data measured by fluorescence polarization show that the most potent compound reached a KD of 12 μM. Furthermore, reasonable selectivity versus other galectins was achieved, making the highlighted compound a promising lead for the development of new selective and potent ligands for galectin-8 as molecular probes to examine the protein's role in cell-based and in vivo studies.
Substituted Pyrazinone Amides
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Page/Page column 15-16, (2010/08/07)
The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. The variables R1, R2
A simple, stereoselective synthesis of ketomethylene dipeptide isosteres
Hoffman, Robert V.,Tao, Junhua
, p. 7119 - 7126 (2007/10/03)
An exceedingly simple, general, and stereoselective method for the preparation of ketomethylene dipeptide isosteres (5-(carbobenzyloxyamino)-2-alkyl-γ-ketoesers) from Cbz-protected amino acids and scalemic-2-triflyloxy esters has been developed. The method is short (three steps), efficient, and highly diastereoselective and enantioselective.