Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase.
- G. Powis, R. Bonjouklian, G. Grindey
- Biology, ChemistryCancer Research
- 1 May 1994
Kinetic analysis demonstrates that wortmannin is a noncompetitive, irreversible inhibitor of phosphatidylinositol-3-kinase, with inactivation being both time- and concentration-dependent.
Thioredoxin reductase.
- D. Mustacich, G. Powis
- BiologyBiochemical Journal
- 2000
The importance of Trx to many aspects of cell function make it likely that TrxRs also play a role in protection against oxidant injury, cell growth and transformation, and the recycling of ascorbate from its oxidized form.
Effect of KRAS oncogene substitutions on protein behavior: implications for signaling and clinical outcome.
Molecular modeling studies showed that different conformations imposed by mutant KRas may lead to altered association with downstream signaling transducers, and implies that therapeutic interventions may need to take into account the specific mutants expressed by the tumor.
Redox Potential of Human Thioredoxin 1 and Identification of a Second Dithiol/Disulfide Motif*
- W. Watson, J. Pohl, Dean P. Jones
- Chemistry, BiologyJournal of Biological Chemistry
- 29 August 2003
Results suggest that the Cys-62-Cys-69 disulfide could provide a means to transiently inhibit Trx1 activity under conditions of redox signaling or oxidative stress, allowing more time for the sensing and transmission of oxidative signals.
Selective inhibition of phosphatidylinositol phospholipase C by cytotoxic ether lipid analogues.
- G. Powis, M. Seewald, C. Gratas, D. Melder, J. Riebow, E. Modest
- Biology, ChemistryCancer Research
- 15 May 1992
The results show that the ether lipid analogues at cytotoxic concentrations are selective inhibitors of PIPLC and that the inhibition of PipLC may be related to the growth inhibitory activity of the ether cholesterol analogues.
Properties and biological activities of thioredoxins.
- G. Powis, W. Montfort
- BiologyAnnual Review of Biophysics and Biomolecular…
- 2001
The mammalian thioredoxins are a family of small redox proteins that undergo NADPH-dependent reduction by thiOREDoxin reductase and in turn reduce oxidized cysteine groups on proteins.
HIF-1 regulation: not so easy come, easy go.
- Mei Yee Koh, T. Spivak-Kroizman, G. Powis
- BiologyTIBS -Trends in Biochemical Sciences. Regular ed
- 1 November 2008
Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer
Single-agent vemurafenib did not show meaningful clinical activity in patients with BRAF V600E mutant CRC, and combination strategies are now under development and may be informed by the presence of intratumor heterogeneity of KRAS and NRAS mutations.
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.
- Y. Hu, L. Qiao, A. Kozikowski
- Biology, ChemistryJournal of Medicinal Chemistry
- 10 August 2000
This work represents the first attempt to examine the effects of 3-modified PI analogues on these two crucial cell signaling proteins, PI3-K and Akt, in an effort to better understand their cell growth inhibitory properties.
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