Acetylene derivatives of phenylalanine, phenethylamine and the multifunctional unnatural amino acids, phenyl-bis-alanine and phenyl-tris-alanine, were synthesized and functionalized with 2-azidoethyl beta-D-galactopyranosyl-(1-->4)-beta-D-glucopyranoside via regioselective copper(I)-mediated 1,3-dipolar cycloaddition to give a panel of mono-, di- and trivalent lactoside derivatives. Evaluation of the compounds as inhibitors against the tumour- and inflammation-related galectin-1, -3, -4N, -4C, -4, -7, -8N and -9N revealed a divalent compound with a Kd value as low as 3.2 microM for galectin-1, which corresponded to a relative potency of 30 per lactose unit as compared to the natural disaccharide ligand lactose. This divalent compound had at least one order of magnitude higher affinity for galectin-1 than for any of the other galectins investigated.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.carres.2006.04.028 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Layered double hydroxides (LDH) are compounds with unique structures of hydroxide functional groups on their surfaces, and they have the proper arrangement of divalent and trivalent cations to adjust their unique catalytic actions. LDH was synthesized utilizing the co-precipitation technique and was thermally treated at 300 °C. The prepared compounds were chemically and structurally elucidated using FT-IR, XRD, SEM, BET, TG-DTA, and XPS characterization.
View Article and Find Full Text PDFComprehensive Chemical Analysis of the Methyl 3-Nitrogen-2,3-Dideoxysaccharides Derivatives with d--Configuration: Synthesis, Reactivity of HIV-1 Reverse Transcriptase Inhibitors.
J Phys Chem B
January 2025
Intermolecular Interaction Laboratory, Department of Bioinorganic Chemistry, Faculty of Chemistry, University of Gdańsk, Wita Stwosza 63, 80-308 Gdańsk, Poland.
This study extends previous research, particularly focusing on patented scientific objects No. ID: PL 240 353 B1, investigating the physicochemical properties of the methyl 3-azido- and 3-amino-2,3-dideoxysaccharides with a nucleoside scaffold similar to 3'-azidothymidine (AZT). The study utilizes multiwavelength spectrophotometric and potentiometric methods to evaluate the ionization of the saccharide units in aqueous solutions.
View Article and Find Full Text PDFMix-Charged Nanofiltration Membrane for Efficient Organic Removal from High-Salinity Wastewater: The Role of Charge Spatial Distribution.
Environ Sci Technol
January 2025
State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Beijing 100190, PR China.
The efficient removal of organic contaminants from high-salinity wastewater is crucial for resource recovery and achieving zero discharge. Nanofiltration (NF) membranes are effective in separating organic compounds and monovalent salts, but they typically exhibit an excessive rejection of divalent salts. Modifying the charge characteristics of NF membranes can improve salt permeation; however, the role of charge spatial distribution in governing salt transport behavior is not fully understood.
View Article and Find Full Text PDFLuminescence Properties of M(AlCl):Yb (M = Ca, Sr, Ba): Ideal Materials for the Investigation of Structure-Luminescence Relationships.
Materials (Basel)
December 2024
Inorganic Chemistry, University of Siegen, 57076 Siegen, Germany.
In this work, the chloride system M(AlCl) (M = Ca, Sr, Ba) doped with Yb is investigated in greater detail. The influence of the [AlCl] ion on the position of the emission band of Yb is investigated and the emission spectra are recorded. The emission spectra of the Yb-doped materials are characterized by broad 4f5d (HS) ↔ 4f transitions with maxima in the range between 416 nm (Ca) and 421 nm (Ba) (24,061-23,738 cm), whereas the Ba compound features an additional 4f5d (LS) ↔ 4f emission band at 397 nm (25,203 cm) at lower temperatures.
View Article and Find Full Text PDFComputational insights into spin-polarized density functional theory applied to actinide-based perovskites XBkO₃ (X = Sr, Ra, Pb).
Sci Rep
January 2025
Water Management Research Institute, National Water Research Center, Shubra El-Kheima 13411, Cairo, Egypt.
The exploration of perovskite compounds incorporating actinide and divalent elements reveals remarkable characteristics. Focusing on PbBkO, RaBkO, and SrBkO, these materials were studied using density functional theory (DFT) via the CASTEP code to analyze their electronic, optical, and mechanical properties. The results show semiconductor behavior, with respective band gaps of 1.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!