Discovery and synthesis of the first selective BAG domain modulator of BAG3 as an attractive candidate for the development of a new class of chemotherapeutics†,Chemical Communications

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Discovery and synthesis of the first selective BAG domain modulator of BAG3 as an attractive candidate for the development of a new class of chemotherapeutics†
Chemical Communications ( IF 4.9 ) Pub Date : 2018-06-11 00:00:00 , DOI: 10.1039/c8cc03399d
Stefania Terracciano _{1,

2,

3} , Gianluigi Lauro _{1,

2,

3} , Alessandra Russo _{1,

2,

3} , Maria Carmela Vaccaro _{1,

2,

3} , Antonio Vassallo _{3,

4,

5} , Margot De Marco _{3,

6,

7,

8,

9} , Bianca Ranieri _{3,

8,

9} , Alessandra Rosati _{3,

6,

7,

8,

9} , Maria Caterina Turco _{3,

6,

7,

8,

9} , Raffaele Riccio _{1,

2,

3} , Giuseppe Bifulco _{1,

2,

3} , Ines Bruno _{1,

2,

3}

Affiliation

BAG3 protein has emerged as a key regulator of important cellular processes and its expression is increased in some tumor types; however, despite its potential value for future chemotherapeutics, no selective BAG3 modulators have been yet reported. Here we report the 2,4-thiazolidinedione derivative 28 as the first BAG3 protein modulator.

中文翻译：

发现和合成BAG3的第一个选择性BAG结构域调节剂，作为开发新型化学疗法的有吸引力的候选药物†

BAG3蛋白已成为重要细胞过程的关键调节剂，在某些肿瘤类型中其表达增加。然而，尽管其对未来化学疗法具有潜在价值，但尚未报道选择性BAG3调节剂。在这里，我们报告2，4-噻唑烷二酮衍生物28作为第一个BAG3蛋白调节剂。

更新日期：2018-06-11

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