Ran Guan

TL;DR: ABT-888 is a potent inhibitor of PARP, has good oral bioavailability, can cross the blood-brain barrier, and potentiates temozolomide, platinums, cyclophosphamide, and radiation in syngeneic and xenograft tumor models.

TL;DR: The development of a series of potent and selective indazole-pyridine based Akt inhibitors is reported, which inhibit Akt-dependent signal transduction in cells and in vivo in a dose-responsive manner and slow the progression of tumors when used as monotherapy or in combination with paclitaxel or rapamycin.

TL;DR: Analysis with isogenic pairs of cell lines revealed that Plk1 depletion preferentially induced mitotic arrest, aneuploidy, and reduced cell survival in the p53-defective cell lines, validating the episodic inhibition of PlK1 as a very useful approach for cancer treatment.

TL;DR: In an attempt to improve the potency and selectivity of the indazole-pyridine series of Akt inhibitors over PKA, efforts have focused on the incorporation of a chemical functionality to interact with the hydroxy group of Thr-211.

TL;DR: It is shown that cells treated with temozolomide need to be exposed to ABT-888 for at least 17 to 24 hours to achieve maximal cytotoxicity, and the extent of cytot toxicity correlates with the level of double-stranded DNA breaks as indicated by γH2AX levels.