Crystal structure of p110alpha-RBD covalently bound to a breaker compound BBO-10203 via Cys242

Crystal structure of p110alpha-RBD covalently bound to a breaker compound BBO-10203 via Cys242 Descriptor: 1-[(4R,8R)-2-[(4M,7P)-7-[2,4-difluoro-6-(2-methoxyethoxy)phenyl]-4-(1-methyl-1H-indazol-5-yl)thieno[3,2-c]pyridin-6-yl]-4-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-5(4H)-yl]propan-1-one, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Authors: Czyzyk, D.J, Simanshu, D.K. Deposit date: 2024-03-21 Release date: 2025-06-25 Last modified: 2025-08-06 Method: X-RAY DIFFRACTION (2.21 Å) Cite: BBO-10203 inhibits tumor growth without inducing hyperglycemia by blocking RAS-PI3K alpha interaction. Science, 389, 2025通过半胱氨酸242（Cys242）与断裂化合物BBO-10203共价结合的p110α-RBD晶体结构。描述信息：1-[(4R,8R)-2-[(4M,7P)-7-[2,4-二氟-6-(2-甲氧基乙氧基)苯基]-4-(1-甲基-1H-吲唑-5-基)噻吩并[3,2-c]吡啶-6-基]-4-甲基-6,7-二氢吡唑并[1,5-a]吡嗪-5(4H)-基]丙-1-酮，磷脂酰肌醇4,5-二磷酸3-激酶催化亚基α亚型。作者：Czyzyk D.J.、Simanshu D.K.。存档日期：2024年3月21日；发布日期：2025年6月25日；最后修改日期：2025年8月6日。实验方法：X射线衍射（分辨率2.21埃）。引用文献：BBO-10203通过阻断RAS-PI3Kα相互作用抑制肿瘤生长且不引发高血糖症，《科学》，389卷，2025年。