1104806-97-4Relevant academic research and scientific papers
TETRAHYDROPYRIDO[3',2':4,5]PYRROLO[1,2-a]PYRAZINE-2-CARBOXAMIDE DERIVATIVES USEFUL AS RSK INHIBITORS
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Paragraph 0749; 0750, (2017/09/07)
Described herein are carboxamide derivatives that are useful as inhibitors of p90 ribosomal S6 kinase (RSK), pharmaceutical compositions comprising the derivatives, and methods of using the derivatives in treating diseases or conditions associated with RSK activity.
Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branch
Gallagher, Ciara M.,Garri, Carolina,Cain, Erica L.,Ang, Kenny Kean-Hooi,Wilson, Christopher G.,Chen, Steven,Hearn, Brian R.,Jaishankar, Priyadarshini,Aranda-Diaz, Andres,Arkin, Michelle R.,Renslo, Adam R.,Walter, Peter
, (2016/08/02)
The membrane-bound transcription factor ATF6α plays a cytoprotective role in the unfolded protein response (UPR), required for cells to survive ER stress. Activation of ATF6α promotes cell survival in cancer models. We used cell-based screens to discover and develop Ceapins, a class of pyrazole amides, that block ATF6α signaling in response to ER stress. Ceapins sensitize cells to ER stress without impacting viability of unstressed cells. Ceapins are highly specific inhibitors of ATF6α signaling, not affecting signaling through the other branches of the UPR, or proteolytic processing of its close homolog ATF6β or SREBP (a cholesterol-regulated transcription factor), both activated by the same proteases. Ceapins are first-in-class inhibitors that can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings. The discovery of Ceapins now enables pharmacological modulation all three UPR branches either singly or in combination.
SODIUM CHANNEL INHIBITORS
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Page/Page column 53, (2009/02/11)
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, composition
