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Review Article

SHP2变构抑制剂：最新专利综述(2015-2020)

卷 28, 期 19, 2021

发表于: 28 September, 2020

页: [3825 - 3842] 页: 18

弟呕挨: 10.2174/1568011817666200928114851

价格: $65

摘要

含Srchomology-2结构域的PTP 2 (SHP2)是由PTPN11基因编码的非受体磷酸酶。SHP2的过度表达与多种人类疾病有关，如努南综合征、LEOPARD综合征和癌症。为了克服现有位阻抑制剂的缺点，目前正在开发具有高选择性和低毒性的靶向SHP2变构位点的新型抑制剂。本文综述了2015-2020年发表在专利中的SHP2变构抑制剂。分子是根据中心核的化学结构分类的。SHP2长期以来被认为是一种“不可消化”的蛋白质。幸运的是，诺华股份有限公司的研究人员取得了重大突破，他们将SHP099确定为一种高效、选择性、可溶性和口服生物可利用的SHP2变构抑制剂。目前，有几种SHP2变构抑制剂正在临床开发中。然而，耐药性仍然是一个重大挑战。SHP2变构抑制剂与免疫治疗药物或分子靶向药物的结合是一种有前途的抗耐药性治疗策略。

关键词: SHP2抑制剂，PTPN11基因，变构，癌症，联合治疗，临床试验。

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