GSK-3α regulates production of Alzheimer's disease amyloid-β peptides

Nature, Journal Year: 2003, Volume and Issue: 423(6938), P. 435 - 439

Published: May 1, 2003

Language: Английский

---

A Rapid, Reversible, and Tunable Method to Regulate Protein Function in Living Cells Using Synthetic Small Molecules

Cell, Journal Year: 2006, Volume and Issue: 126(5), P. 995 - 1004

Published: Sept. 1, 2006

Language: Английский

---

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

Nature Biotechnology, Journal Year: 2011, Volume and Issue: 29(11), P. 1039 - 1045

Published: Oct. 30, 2011

Language: Английский

---

GSK-3-Selective Inhibitors Derived from Tyrian Purple Indirubins

Chemistry & Biology, Journal Year: 2003, Volume and Issue: 10(12), P. 1255 - 1266

Published: Dec. 1, 2003

Language: Английский

---

GSK3 inhibitors: development and therapeutic potential

Nature Reviews Drug Discovery, Journal Year: 2004, Volume and Issue: 3(6), P. 479 - 487

Published: June 1, 2004

Language: Английский

---

Systematic Discovery of In Vivo Phosphorylation Networks

Cell, Journal Year: 2007, Volume and Issue: 129(7), P. 1415 - 1426

Published: June 1, 2007

Language: Английский

---

PF00299804, an Irreversible Pan-ERBB Inhibitor, Is Effective in Lung Cancer Models withEGFRandERBB2Mutations that Are Resistant to Gefitinib

Cancer Research, Journal Year: 2007, Volume and Issue: 67(24), P. 11924 - 11932

Published: Dec. 15, 2007

Abstract Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors gefitinib and erlotinib are effective treatments for a subset of non–small cell lung cancers. In particular, cancers with specific EGFR-activating mutations seem to be the most sensitive these agents. However, despite their initial response, such almost invariably develop resistance. 50% cancers, secondary EGFR mutation, T790M, has been identified that renders ineffective activity. Thus, there is clinical need novel can effectively inactivate T790M-containing proteins. this study, we evaluate effectiveness compound, PF00299804, an irreversible pan-ERBB inhibitor. The results from studies show PF00299804 potent inhibitor as well T790M resistance mutation both in vitro vivo. Additionally, highly wild-type ERBB2 gefitinib-resistant oncogenic These preclinical evaluations support further development and/or amplifications ERBB family members. [Cancer Res 2007;67(24):11924–32]

Language: Английский

---

Mitogen-Activated Protein Kinase Signaling in the Heart: Angels Versus Demons in a Heart-Breaking Tale

Physiological Reviews, Journal Year: 2010, Volume and Issue: 90(4), P. 1507 - 1546

Published: Oct. 1, 2010

Among the myriad of intracellular signaling networks that govern cardiac development and pathogenesis, mitogen-activated protein kinases (MAPKs) are prominent players have been focus extensive investigations in past decades. The four best characterized MAPK subfamilies, ERK1/2, JNK, p38, ERK5, targets pharmacological genetic manipulations to uncover their roles development, function, diseases. However, information reported literature from these efforts has not yet resulted a clear view about specific pathways heart. Rather, controversies contradictive results led perception MAPKs ambiguous characters heart with both protective detrimental effects. primary object this review is provide comprehensive overview current progress, an effort highlight areas where consensus established verses ones controversy remains. hypertrophy, ischemia/reperfusion injury, pathological remodeling main focuses as represent most critical issues for evaluating viable therapeutic development. studies presented will help reveal major challenges field limitations approaches point need future gain better understanding fundamental mechanisms function regulation

Language: Английский

---

LTP Inhibits LTD in the Hippocampus via Regulation of GSK3β

Neuron, Journal Year: 2007, Volume and Issue: 53(5), P. 703 - 717

Published: March 1, 2007

Language: Английский

---

Redox regulation of FoxO transcription factors

Redox Biology, Journal Year: 2015, Volume and Issue: 6, P. 51 - 72

Published: July 5, 2015

Transcription factors of the forkhead box, class O (FoxO) family are important regulators cellular stress response and promote antioxidant defense. On one hand, FoxOs stimulate transcription genes coding for proteins located in different subcellular compartments, such as mitochondria (i.e. superoxide dismutase-2, peroxiredoxins 3 5) peroxisomes (catalase), well found extracellularly plasma (e.g., selenoprotein P ceruloplasmin). other reactive oxygen species (ROS) stressful stimuli that elicit formation ROS, may modulate FoxO activity at multiple levels, including posttranslational modifications (such phosphorylation acetylation), interaction with coregulators, alterations localization, protein synthesis stability. Moreover, transcriptional posttranscriptional control expression is sensitive to ROS. Here, we review these aspects biology focusing on redox regulation signaling, emphasis interplay between ROS under various physiological pathophysiological conditions. Of particular interest dual role played by cancer development their key whole body nutrient homeostasis, modulating metabolic adaptations and/or disturbances low vs. high intake. Examples discussed here include calorie restriction starvation adipogenesis, obesity type 2 diabetes.

Language: Английский

---