Ontology highlight
ABSTRACT:
SUBMITTER: Zhao Y
PROVIDER: S-EPMC4027628 | biostudies-literature | 2014 Feb
REPOSITORIES: biostudies-literature
Zhao Yanlong Y Zhang Xi X Chen Yingyi Y Lu Shaoyong S Peng Yuefeng Y Wang Xiang X Guo Chengliang C Zhou Aiwu A Zhang Jingmiao J Luo Yu Y Shen QianCheng Q Ding Jian J Meng Linghua L Zhang Jian J
ACS medicinal chemistry letters 20131210 2
The phosphatidylinositol 3-kinase (PI3K) signaling pathway plays important roles in cell proliferation, growth, and survival. Hyperactivated PI3K is frequently found in a wide variety of human cancers, validating it as a promising target for cancer therapy. We determined the crystal structure of the human PI3Kα-PI103 complex to unravel molecular interactions. Based on the structure, substitution at the R1 position of the phenol portion of PI103 was demonstrated to improve binding affinity via fo ...[more]