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Significance PI3Kα is a dimeric lipid kinase consisting of a catalytic subunit p110α and a regulatory subunit p85α. It controls cell proliferation and survival and is an important therapeutic target… Click to show full abstract
Significance PI3Kα is a dimeric lipid kinase consisting of a catalytic subunit p110α and a regulatory subunit p85α. It controls cell proliferation and survival and is an important therapeutic target for cancer. However, the development of effective drugs against PI3Kα requires a level of structural information that is currently unavailable, because the extreme flexibility of PI3Kα interferes with structural analysis. Nanobodies were used in conjunction with chemical cross-linking to generate insights into the identity and the positions of the most flexible domains of PI3Kα and into mechanistic aspects of positional flexibility. The studies also reveal the existence of a previously unreported structural conformation of PI3Kα.
Journal Title: Proceedings of the National Academy of Sciences of the United States of America
Year Published: 2022
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