Design, Synthesis, and Anticancer Activity of a Selenium-Containing Galectin-3 and Galectin-9N Inhibitor

被引：9

作者：

Di Gaetano, Sonia ^{[1
,2
]}

Pirone, Luciano ^{[1
,2
]}

Galdadas, Ioannis ^{[3
,4
]}

Traboni, Serena ^{[5
]}

Iadonisi, Alfonso ^{[5
]}

Pedone, Emilia ^{[1
,2
]}

Saviano, Michele ^{[2
,6
]}

Gervasio, Francesco Luigi ^{[4
,7
,8
]}

Capasso, Domenica ^{[2
,9
]}

机构：

[1] CNR, Inst Biostruct & Bioimaging, I-80134 Naples, Italy

[2] Univ Naples Federico II, Interuniv Res Ctr Bioact Peptides CIRPEB, I-80134 Naples, Italy

[3] UCL, Dept Chem, London WC1E 6BT, England

[4] Univ Geneva, Inst Pharmaceut Sci Western Switzerland, CH-1211 Geneva, Switzerland

[5] Univ Naples Federico II, Dept Chem Sci, I-80134 Naples, Italy

[6] CNR, Inst Crystallog, I-70126 Bari, Italy

[7] UCL, Inst Struct & Mol Biol, London WC1E 6BT, England

[8] Univ Geneva, Sch Pharmaceut Sci, CH-1211 Geneva, Switzerland

[9] Univ Naples Federico II, Ctr Life Sci & Technol CESTEV, I-80145 Naples, Italy

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2022年 / 23卷 / 05期

基金：

欧盟地平线“2020”; 美国国家卫生研究院;

关键词：

galectin; digalactoside compounds; drug design; binding affinity melanoma cells; HIGH-AFFINITY; DERIVATIVES; DISELENIDES; LUNG; ORGANOSELENIUM; ANGIOGENESIS; MODULATORS; EFFICIENT; APOPTOSIS; FIBROSIS;

D O I：

10.3390/ijms23052581

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Galectins are soluble beta-D-galactoside-binding proteins whose implication in cancer progression and disease outcome makes them prominent targets for therapeutic intervention. In this frame, the development of small inhibitors that block selectively the activity of galectins represents an important strategy for cancer therapy which is, however, still relatively underdeveloped. To this end, we designed here a rationally and efficiently novel diglycosylated compound, characterized by a selenoglycoside bond and the presence of a lipophilic benzyl group at both saccharide residues. The relatively high binding affinity of the new compound to the carbohydrate recognition domain of two galectins, galectin 3 and galectin 9, its good antiproliferative and anti-migration activity towards melanoma cells, as well as its anti-angiogenesis properties, pave the way for its further development as an anticancer agent.

引用

页数：21

共 71 条

[1] Efficient and direct synthesis of saccharidic 1,2-ethylidenes, orthoesters, and glycals from peracetylated sugars via the in situ generation of glycosyl iodides with I2/Et3SiH [J].