Galectin
Galectins are a subfamily of lectin proteins with high affinity for β-galactosides. In normal tissue and blood, galectins are expressed at low levels, but they are increased in serum, plasma and urine in neoplastic diseases. Galectins also play an important role in other chronic diseases such as cardiac insufficiency, diabetes, rheumatoid arthritis, asthma and liver cirrhosis. Galectins are present in numerous locations within the cell, such as nucleus, cytoplasm and plasma membrane, but also extracellularly. Gal-1 can recognize N-glycans on VEGFR2 and trigger a VEGF-like signaling response thereby promoting vascular regrowth in absence of VEGF. Galectins are involved in cancer-promoting processes such as proliferation, apoptosis and immune modulation. Galectins produced by tumor cells bind to T-cell glycoprotein receptors like CD45 and CD71. Potential adverse effects of galectin inhibition were observed in human breast carcinoma. In breast cancer cells, Gal-1 and Gal-3 compete for cell surface receptors while generating opposite functions. Gal-3 binds with K-Ras and activates the MEK-ERK signaling pathway, while Gal-1 binds with H-Ras and activates PI3K/AKT cascade hence modulating rather distinct cellular functions.
References
1.Kamil Wdowiak,et al. Int J Mol Sci. 2018 Jan; 19(1): 210.
References
1.Kamil Wdowiak,et al. Int J Mol Sci. 2018 Jan; 19(1): 210.
Cytoskeleton/Cell Adhesion Molecules
Galectin
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Thiodigalactoside
产品货号 : M35002
cas no: 51555-87-4
Thiodigalactoside (TDG) 是一种具有口服活性的,有效的半乳凝素 (GAL) 抑制剂,对于 GAL-1 和 GAL-3 的 Kd 值分别为 24 μM,49 μM。Thiodigalactoside 是一种不可代谢的二糖,具有抗炎和抗癌性。Thiodigalactoside 可显着降低饮食诱发的肥胖大鼠的体重增加。 -
LLS30
产品货号 : M13409
cas no: 2138367-58-3
LLS30 是一种有效的变构半乳糖凝集素-1 (Gal-1) 抑制剂。 -
GB1107
产品货号 : M13093
cas no: 1978336-61-6
GB1107 (GB-1107, GB 1107) 是一种有效的、选择性的、口服活性的 Galectin-3 (Gal-3) 抑制剂,Kd 为 37 nM(人 Galectin-3)。 -
OTX008 (b)
产品货号 : M12472
cas no: 1638140-55-2
OTX008(Calixarene 0118、PTX-008)是一种杯芳烃衍生物,设计用于结合 Galectin-1 (Gal1) 两亲性 β-折叠构象。 -
TD-139
产品货号 : M11938
cas no: 1450824-22-2
TD-139 (TD139) 是一种高效、选择性的 Galectin-3 (Gal-3) 碳水化合物结合域抑制剂,Ki 为 14 nM。