53bp1

UNC-2170 (UNC2170 Maleate) 是53BP1(IC50=29 µM;Kd=22 µM) 选择性的、功能活性的片段状配体，对 53BP1 的选择性比其他九种甲基赖氨酸读取器蛋白质高出至少17倍。53BP1 是 Kme 结合蛋白，在 DNA 损伤修复途径中起核心作用，并被招募到双链断裂位点。

UNC926 (UNC-926) 抑制 L3MBTL1，还对 L3MBTL3 表现出低微摩尔亲和力。它抑制 3xMBT 结构域与 H4K20me1 的结合，可选择性和剂量依赖性地抑制 L3MBTL13xMBT-H4K20me1 相互作用。

UNC9512是一种针对甲基赖氨酸读取器p53结合蛋白1 (53BP1) 的有效拮抗剂, 适用于探究53BP1在DNA修复、基因编辑及肿瘤发生等生物学过程的功能。

UNC3474为小分子配体，与53BP1相结合。该化合物针对53BP1TT的芳香族甲基赖氨酸结合笼展现出1.0 ± 0.3μM的解离常数（Kd）。UNC3474抑制53BP1募集至DSB，其机制为稳定细胞内预存的53BP1自抑制状态。

53BP1-binding protein 1 (53BP1) engages with dimethylated lysine 20 on histone 4 (H4K20me2) through its tandem tudor domains within a homodimer configuration, crucial for the DNA damage response. UNC2170, a micromolar 53BP1 ligand, selectively interacts with this site, demonstrating at least 17-fold preference for 53BP1 over similar proteins. This interaction occurs in a pocket formed by the 53BP1's tudor domains. Moreover, UNC2170 acts as an antagonist to 53BP1 in cellular lysates, effectively inhibiting class switch recombination, a process dependent on the functional 53BP1 tudor domain, thus confirming its cellular activity.

Tumor protein p53 binding protein (53BP1) has been identified in a yeast two-hybrid screen as a protein that interacts with the central DNA–binding domain of p532. Similar to breast cancer susceptibility gene 13, 4 (BRCA1; 53BP1 enhances p53-dependent tra