Somatic Mutations in PI3Kalpha: Structural Basis for Enzyme Activation and Drug Design
Journal Article
·
· Biochimica et Biophysica Acta
OSTI ID:1041644
The PI3K pathway is a communication hub coordinating critical cell functions including cell survival, cell growth, proliferation, motility and metabolism. Because PI3K{alpha} harbors recurrent somatic mutations resulting in gains of function in human cancers, it has emerged as an important drug target for many types of solid tumors. Various PI3K isoforms are also being evaluated as potential therapeutic targets for inflammation, heart disease, and hematological malignancies. Structural biology is providing insights into the flexibility of the PI3Ks, and providing basis for understanding the effects of mutations, drug resistance and specificity.
- Research Organization:
- Brookhaven National Lab. (BNL), Upton, NY (United States)
- Sponsoring Organization:
- USDOE SC OFFICE OF SCIENCE (SC)
- DOE Contract Number:
- DE-AC02-98CH10886
- OSTI ID:
- 1041644
- Report Number(s):
- BNL-97322-2012-JA; BBACAQ; TRN: US201212%%62
- Journal Information:
- Biochimica et Biophysica Acta, Vol. 1804, Issue 3; ISSN 0006-3002
- Country of Publication:
- United States
- Language:
- English
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