Lusong Luo

TL;DR: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3- pyridinyl}benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.

TL;DR: The characterization of SB-590885 is reported, a novel triarylimidazole that selectively inhibits Raf kinases with more potency towards B-Raf than c-Rafa, and provides the first evidence of a correlation between the expression of oncogenic BRAF alleles and a positive response to a selective B- Raf inhibitor.

TL;DR: Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of C Enp-E to microtubules is insufficient to satisfy the mitotic checkpoint.

TL;DR: In this paper, the authors disclose the discovery and preclinical characterization of a potent, selective, and irreversible BTK inhibitor as their clinical candidate by using in vitro potency, selectivity, pharmacokinetics (PK), and in vivo pharmacodynamic for prioritizing compounds.

TL;DR: EGCG, a major component of green tea, is an ATP-competitive inhibitor of both phosphoinositide-3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with K(i) values of 380 and 320nM respectively.