PI3K/AKT/mTOR通路
PTEN公司
小分子
P110α
基因亚型
化学
激酶
磷脂酰肌醇
磷酸肌醇3激酶
计算生物学
药理学
生物化学
癌症研究
生物
信号转导
基因
作者
Yi Yu,Dongyan Gu,Lvtao Cai,Hui Yang,Rong Sheng
标识
DOI:10.1016/j.drudis.2023.103854
摘要
Phosphatidylinositol-3 kinase (PI3K) β, a subtype of class I PI3Ks, has an essential role in PTEN-deficient tumors and links to thrombosis, male fertility, and Fragile X syndrome. PI3Kβ-specific targeting therapy could be an efficacious treatment for diseases highly dependent on PI3Kβ, while mitigating the severe toxicity of pan-PI3K inhibitors. Achieving selectivity can be accomplished through three primary strategies, namely, binding to the induced lipophilic pocket, targeting the unique amino acid residue of PI3Kβ, or using atropisomerism to lock conformation. In this review, we focus on advances in the development of these β-isoform-selective PI3K inhibitors, providing potential guidance for the further development of novel clinical candidates.
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