别名 ATR激酶、ataxia telangiectasia and Rad3 related、Ataxia telangiectasia and Rad3-related protein + [9] |
简介 Serine/threonine protein kinase which activates checkpoint signaling upon genotoxic stresses such as ionizing radiation (IR), ultraviolet light (UV), or DNA replication stalling, thereby acting as a DNA damage sensor. Recognizes the substrate consensus sequence [ST]-Q. Phosphorylates BRCA1, CHEK1, MCM2, RAD17, RPA2, SMC1 and p53/TP53, which collectively inhibit DNA replication and mitosis and promote DNA repair, recombination and apoptosis. Phosphorylates 'Ser-139' of histone variant H2AX at sites of DNA damage, thereby regulating DNA damage response mechanism. Required for FANCD2 ubiquitination. Critical for maintenance of fragile site stability and efficient regulation of centrosome duplication. Positively regulates the restart of stalled replication forks following activation by the KHDC3L-OOEP scaffold complex (By similarity). |
靶点 |
作用机制 ATR抑制剂 |
在研机构 |
原研机构 |
最高研发阶段临床3期 |
首次获批国家/地区- |
首次获批日期1800-01-20 |
靶点 |
作用机制 ATR抑制剂 |
最高研发阶段临床2期 |
首次获批国家/地区- |
首次获批日期1800-01-20 |
靶点 |
作用机制 ATR抑制剂 |
非在研适应症- |
最高研发阶段临床2期 |
首次获批国家/地区- |
首次获批日期1800-01-20 |
开始日期2025-01-01 |
申办/合作机构 |
开始日期2024-08-16 |
开始日期2024-08-07 |