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CAL-101, a p110δ selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability
Open accessAbstract
Phosphatidylinositol-3-kinase p110δ serves as a central integration point for signaling from cell surface receptors known to promote malignant B-cell proliferation and survival. This provides a rationale for the development of small molecule inhibitors that selectively target p110δ as a treatment approach for patients with B-cell malignancies. We thus identified 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one (CAL-101), a highly selective and potent p110δ small molecule inhibitor (half-maximal effective concentration [EC50] = 8nM). Using tumor cell lines and primary patient samples representing multiple B-cell malignancies, we have demonstrated that constitutive phosphatidylinositol-3-kinase pathway activation is p110δ-dependent. CAL-101 blocked constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis. These effects have been observed across a broad range of immature and mature B-cell malignancies, thereby providing a rationale for the ongoing clinical evaluation of CAL-101.
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Metadata
- Authors
- Lannutti, B. J., Meadows, S. A., Herman, S. E. M., Kashishian, A., Steiner, B., Johnson, A. J., Byrd, J. C., Tyner, J. W., Loriaux, M. M., Deininger, M., Druker, B. J., Puri, K. D., Ulrich, R. G., & Giese, N. A.
- Venue
- Blood
- Publisher
- American Society of Hematology
- Published
- 2011-01-13
- Volume
- 117
- Issue
- 2
- Pages
- 591-594
- ISSN
- 0006-4971 (ISSN-L)
- 1528-0020
- OpenAlex
- W2027971058
- Cited by
- 720
- References
- 1
- FWCI
- 22.09
- Type
- journal article
- Language
- en
- Open access
- bronze
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