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Alexander R. Shoemaker

Researcher at Abbott Laboratories

Publications -  29
Citations -  7401

Alexander R. Shoemaker is an academic researcher from Abbott Laboratories. The author has contributed to research in topics: Cancer & Kinase. The author has an hindex of 18, co-authored 28 publications receiving 6912 citations. Previous affiliations of Alexander R. Shoemaker include Neurocrine Biosciences & Idun Pharmaceuticals.

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ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

TL;DR: The biological properties and rationale for clinical trials evaluating ABT-263 in small-cell lung cancer and B-cell malignancies are provided and the oral efficacy should provide dosing flexibility to maximize clinical utility both as a single agent and in combination regimens are reported.
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Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.

TL;DR: Targeted modifications at three key positions of 1 resulted in a 20-fold improvement in the pharmacokinetic/pharmacodynamic relationship (PK/PD) between oral exposure (AUC) and in vitro efficacy in human tumor cell lines (EC 50).
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Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.

TL;DR: Compound 2 demonstrated single agent efficacy against human follicular lymphoma cell lines that overexpress Bcl-2, and efficacy in a murine xenograft model of lymphoma when given both as a single agent and in combination with etoposide.