Design, Synthesis, and Anticancer Activity of a Selenium-Containing Galectin-3 and Galectin-9N Inhibitor.
Design, Synthesis, and Anticancer Activity of a Selenium-Containing Galectin-3 and Galectin-9N Inhibitor.
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DOI：
10.3390/ijms23052581
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发表时间：
2022-02-25
影响因子：
5.6
通讯作者：
Capasso D
中科院分区：
文献类型：
--
作者：
Di Gaetano S;Pirone L;Galdadas I;Traboni S;Iadonisi A;Pedone E;Saviano M;Gervasio FL;Capasso D
Galectins是一种可溶性的β-D-半乳糖苷结合蛋白，其在癌症进展和疾病结局中的作用使其成为治疗干预的重要靶点。在这一框架中，开发选择性阻断Galectins活性的小分子抑制剂代表着癌症治疗的一项重要战略，然而，这一战略仍然相对不发达。为此，我们设计了一种合理而有效的新型二糖基化化合物，其特征是在两个糖基上都存在一个糖苷键和一个亲脂性的苄基。新化合物与Galectin 3和Galectin 9的糖识别域具有较高的亲和力，对黑色素瘤细胞具有良好的抗增殖和抗迁移活性，以及抗血管生成的特性，为其作为抗癌药物的进一步开发奠定了基础。
Galectins are soluble β-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.
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影响因子：
16.6
作者：
Cumpstey, I;Sundin, A;Nilsson, UJ
通讯作者：
Nilsson, UJ
影响因子：
3.2
作者：
Cumpstey, I;Carlsson, S;Nilsson, UJ
通讯作者：
Nilsson, UJ
影响因子：
5.2
作者：
Hill, Billy Samuel;Sarnella, Annachiara;Zannetti, Antonella
通讯作者：
Zannetti, Antonella
影响因子：
10.7
作者：
Houzelstein, D;Gonçalves, IR;Poirier, F
通讯作者：
Poirier, F
影响因子：
4.3
作者：
Dange, Manohar C.;Agarwal, Akhil Kumar;Kalraiya, Rajiv D.
通讯作者：
Kalraiya, Rajiv D.