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A new and rapid colorimetric determination of acetylcholinesterase activity.
The PI3K pathway as drug target in human cancer.
This review will discuss how PI3K signaling affects the growth and survival of tumor cells and consider how inhibitors of this pathway, either alone or in combination with other therapeutics, can be used for the treatment of cancer.
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis
- D. Anastasiou, Yimin Yu, M. V. Vander Heiden
- Biology, ChemistryNature Chemical Biology
- 7 September 2012
It is shown that expression of PKM1, the pyruvate kinase isoform with high constitutive activity, or exposure to published small molecule PKM2 activators inhibit growth of xenograft tumors and support the notion that small molecule activation ofPKM2 can interfere with anabolic metabolism.
Targeting renal cell carcinoma with a HIF-2 antagonist
It is shown that some ccRCCs are HIF-2 independent, and set the stage for biomarker-driven clinical trials, using a tumourgraft/patient-derived xenograft platform to evaluate PT2399, a selective Hif-2 antagonist that was identified using a structure-based design approach.
Hexachlorobenzene (HCB): a review.
- K. Courtney
- BiologyEnvironmental research
- 1 December 1979
Localization and Phosphorylation of Abl-Interactor Proteins, Abi-1 and Abi-2, in the Developing Nervous System
- K. Courtney, M. Grove, H. Vandongen, A. VanDongen, A. LaMantia, A. Pendergast
- BiologyMolecular and Cellular Neuroscience
- 1 September 2000
The Abi adaptors exhibit proper expression patterns and subcellular localization to participate in Abl kinase signaling in the nervous system.
Teratology studies with 2,4,5-trichlorophenoxyacetic acid and 2,3,7,8-tetrachlorodibenzo-p-dioxin.
HIF-2 Complex Dissociation, Target Inhibition, and Acquired Resistance with PT2385, a First-in-Class HIF-2 Inhibitor, in Patients with Clear Cell Renal Cell Carcinoma
Findings demonstrate a core dependency on Hif-2 in metastatic ccRCC and establish PT2385 as a highly specific HIF-2 inhibitor in humans and establish new approaches will be required to target mutant H IF-2 beyondPT2385 or the closely related PT2977.
The effects of pentachloronitrobenzene, hexachlorobenzene, and related compounds on fetal development.
Phase I Dose-Escalation Trial of PT2385, a First-in-Class Hypoxia-Inducible Factor-2α Antagonist in Patients With Previously Treated Advanced Clear Cell Renal Cell Carcinoma.
PT2385 has a favorable safety profile and is active in patients with heavily pretreated ccRCC, validating direct HIF-2α antagonism for the treatment of patients withccRCC.