Biophysical and structural characterization of mono/di-arylated lactosamine derivatives interaction with human galectin-3

Quantitative characterization of galectin‐3‐C affinity mass spectrometry measurements: Comprehensive data analysis, obstacles, shortcuts and robustness

“…Both qualitative and quantitative data could be obtained and they were in agreement with other analytical techniques, including isothermal titration calorimetry (ITC), which is considered to be the most accurate. Although some human galectin AMS data was previously reported, the technique is seldom used for either discovery or quantitative analysis of biological lectin ligands in the field of galectins, as well as in the lectin glycobiology field in general. Two major nanoESI‐MS‐based methods for studying carbohydrate ligands of various proteins are direct, and catch and release (CaR) ESI‐MS assays.…”

Development of a Sensitive Microarray Platform for the Ranking of Galectin Inhibitors: Identification of a Selective Galectin‐3 Inhibitor

“…Pursuing the development of galectin‐3‐specific inhibitors, the lactosamine core [Gal‐β(1→4)GlcN] was selected on the basis of its intrinsic affinity for this galectin, with a dissociation constant ( K d ) in the 100 μ m range . Moreover, it is known that affinity and specificity for this galectin can be consistently increased upon introducing substituents, noticeably aromatic appendages, at the C2 and C3 positions of the glucosamine and galactose moieties, respectively . Modification at C3 of the galactose has extensively been investigated, and this established the supremacy of aromatic amides and triazolyl groups over the corresponding aryl ethers, thiourea, urea, and sulfonamides .…”

“…Moreover, it is known that affinity and specificity for this galectin can be consistently increased upon introducing substituents, noticeably aromatic appendages, at the C2 and C3 positions of the glucosamine and galactose moieties, respectively . Modification at C3 of the galactose has extensively been investigated, and this established the supremacy of aromatic amides and triazolyl groups over the corresponding aryl ethers, thiourea, urea, and sulfonamides . To our knowledge, such hierarchy remains to be established for the C2 position of the glucosamine/glucose residue, except that the CRD of galectin‐3 seems to bind preferentially to amides over esters .…”

“…However, this technique is rather demanding in terms of materials (though this parameter is strongly correlated with both affinity and enthalpy) and experimental time. Solid‐phase assays such as enzyme‐linked lectin assays (ELLAs), frontal affinity chromatography, capillary electrophoresis, surface plasmon resonance, fluorescence polarization (FP), and native mass spectrometry to measure the galectin‐3–inhibitor interaction are analytical methods that have all been successfully applied for galectin–ligand interaction studies. Microarrays appear as versatile technologies that combine the properties of high detection sensitivity, small working scale, and potentially high throughput screening .…”

Carbohydrate Recognition Mechanism of the Mushroom Galectin ACG

“…In fact, various galectin inhibitors have been developed, with the aim of developing galectin-targeted pharmaceutical drugs (39)(40)(41). As in the cases of galectin-3 and galectin-9 CRDs, affinity enhancement is evident in ACG for the repeating LacNAc unit (i.e., LacNAcβ1-3), while affinity increases for oligolactosamines, such as LacNAc 2 , LacNAc 3 , and LacnAc 5 , are rather modest in ACG.…”