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Coordinate Regulation of Sugar Flux and Translation by PAS Kinase
PAS kinase is a serine/threonine kinase regulated in cis by a PAS domain. A genetic study of the two PAS kinase genes in budding yeast gave evidence of the involvement of these enzymes in the control… Expand
Control of mammalian glycogen synthase by PAS kinase.
- W. Wilson, A. V. Skurat, B. Probst, Anna de Paoli-Roach, P. Roach, J. Rutter
- Biology, Medicine
- Proceedings of the National Academy of Sciences…
- 15 November 2005
Evidence is provided here that PAS kinase is an important regulator of mammalian glycogen synthase and this mode of regulation provides a mechanism for metabolic status to impinge directly on the cellular decision of whether to store or use available energy. Expand
RTA 408, A Novel Synthetic Triterpenoid with Broad Anticancer and Anti-Inflammatory Activity
Semi-synthetic triterpenoids are antioxidant inflammation modulator (AIM) compounds that inhibit tumor cell growth and metastasis. Compounds in the AIM class bind to Keap1 and attenuate Nrf2… Expand
Smac mimetics increase cancer cell response to chemotherapeutics in a TNF-α-dependent manner
Surprisingly, although genotoxic agents typically induce apoptosis through the mitochondrial intrinsic pathway, it is shown that this synergism is mediated through a TNF-α/RIP1-dependent pathway, leading to activation of the extrinsic apoptotic pathway. Expand
Characterization of novel small-molecule NRF2 activators: Structural and biochemical validation of stereospecific KEAP1 binding.
- C. Huerta, Xin Jiang, +9 authors W. C. Wigley
- Chemistry, Medicine
- Biochimica et biophysica acta
- 1 November 2016
This work demonstrates that reversible cyanoenone Michael acceptors, such as the tpAIMs and sA IMs, can be specifically tuned to regulate redox sensitive cysteine residues on key signaling molecules, an approach with significant promise for innovative drug development. Expand
Functional immune mapping with deep-learning enabled phenomics applied to immunomodulatory and COVID-19 drug discovery
Deep-learning-driven analysis of cellular morphology is applied to develop a scalable “phenomics” platform and its ability to identify dose-dependent, high-dimensional relationships among and between immunomodulators, toxins, pathogens, genetic perturbations, and small and large molecules at scale is demonstrated. Expand
Cancer Cell Growth Is Differentially Affected by Constitutive Activation of NRF2 by KEAP1 Deletion and Pharmacological Activation of NRF2 by the Synthetic Triterpenoid, RTA 405
- B. Probst, Lyndsey McCauley, Isaac Treviño, W. C. Wigley, D. Ferguson
- Biology, Medicine
- PloS one
- 24 August 2015
Assessment of basal levels of KEAP1 and NRF2 in a panel of human tumor cell lines and the activity of an AIM demonstrate that pharmacological activation ofNRF2 by AIMs is distinct from genetic activation and does not provide a growth or survival advantage to tumor cells. Expand
Two Distinct High Throughput Screens of PAS Kinase Yield Convergent Insight to Enzyme Function
PAS domain-linked protein kinase enzymes can be tuned to sense environmental cues and rapidly initiate an adaptive biological response. Two high throughput (HT) screens were employed to probe the… Expand
Effect of RTA 405 on survival in cell lines with low, moderate, or high basal NRF2 activity.
Omaveloxolone Increases Nrf2 Activity, Reduces Inflammation, And Improves Mitochondrial Function In Cultured Cell Models Of Friedreich’s Ataxia. (P1.058)
OMAV dose-dependently improved multiple parameters of mitochondrial function, including spare respiratory capacity and maximal respiration, in skeletal muscle cells and in the Frataxin mutant cell line, suggesting that activation of Nrf2 by OMAV may have the potential to improve molecular parameters associated with FA. Expand