scholarly journals E-Pharmacophore Mapping Combined with Virtual Screening and Molecular Docking to Identify Potent and Selective Inhibitors of P90 Ribosomal S6 Kinase (RSK)

2018 ◽  
Author(s):  
Abdulilah Ece
Keyword(s):  
Molecular Docking ◽  
Virtual Screening ◽  
Selective Inhibitors ◽  
Pharmacophore Mapping ◽  
S6 Kinase ◽  
P90 Ribosomal S6 Kinase ◽  
Ribosomal S6 Kinase

Novel Potent and Selective Inhibitors of p90 Ribosomal S6 Kinase Reveal the Heterogeneity of RSK Function in MAPK-Driven Cancers

2014 ◽  
Vol 12 (5) ◽  
pp. 803-812 ◽  
Author(s):  
Ida Aronchik ◽  
Brent A. Appleton ◽  
Stephen E. Basham ◽  
Kenneth Crawford ◽  
Mercedita Del Rosario ◽  
...  
Keyword(s):  
Selective Inhibitors ◽  
S6 Kinase ◽  
P90 Ribosomal S6 Kinase ◽  
Ribosomal S6 Kinase

scholarly journals p90 ribosomal S6 kinase 3 contributes to cardiac insufficiency in α-tropomyosin Glu180Gly transgenic mice

2013 ◽  
Vol 305 (7) ◽  
pp. H1010-H1019 ◽  
Author(s):  
Catherine L. Passariello ◽  
Marjorie Gayanilo ◽  
Michael D. Kritzer ◽  
Hrishikesh Thakur ◽  
Zoharit Cozacov ◽  
...  
Keyword(s):  
Heart Failure ◽  
Transgenic Mice ◽  
Cardiac Function ◽  
Interstitial Fibrosis ◽  
Cardiac Insufficiency ◽  
S6 Kinase ◽  
Transgenic Expression ◽  
P90 Ribosomal S6 Kinase ◽  
Ribosomal S6 Kinase

Myocardial interstitial fibrosis is an important contributor to the development of heart failure. Type 3 p90 ribosomal S6 kinase (RSK3) was recently shown to be required for concentric myocyte hypertrophy under in vivo pathological conditions. However, the role of RSK family members in myocardial fibrosis remains uninvestigated. Transgenic expression of α-tropomyosin containing a Glu180Gly mutation (TM180) in mice of a mixed C57BL/6:FVB/N background induces a cardiomyopathy characterized by a small left ventricle, interstitial fibrosis, and diminished systolic and diastolic function. Using this mouse model, we now show that RSK3 is required for the induction of interstitial fibrosis in vivo. TM180 transgenic mice were crossed to RSK3 constitutive knockout ( RSK3−/−) mice. Although RSK3 knockout did not affect myocyte growth, the decreased cardiac function and mild pulmonary edema associated with the TM180 transgene were attenuated by RSK3 knockout. The improved cardiac function was consistent with reduced interstitial fibrosis in the TM180; RSK3−/− mice as shown by histology and gene expression analysis, including the decreased expression of collagens. The specific inhibition of RSK3 should be considered as a potential novel therapeutic strategy for improving cardiac function and the prevention of sudden cardiac death in diseases in which interstitial fibrosis contributes to the development of heart failure.

scholarly journals An Intracellular Calcium Signal Activates p70 but Not p90 Ribosomal S6 Kinase in Liver Epithelial Cells

1997 ◽  
Vol 272 (3) ◽  
pp. 1920-1928 ◽  
Author(s):  
Lee M. Graves ◽  
Yaqin He ◽  
John Lambert ◽  
Deborah Hunter ◽  
Xiong Li ◽  
...  
Keyword(s):  
Epithelial Cells ◽  
Intracellular Calcium ◽  
Calcium Signal ◽  
S6 Kinase ◽  
Liver Epithelial Cells ◽  
P90 Ribosomal S6 Kinase ◽  
Ribosomal S6 Kinase

scholarly journals Inhibition of p90 ribosomal S6 kinase potentiates cisplatin activity in A549 human lung adenocarcinoma cells

2020 ◽  
Vol 72 (11) ◽  
pp. 1536-1545
Author(s):  
Nabeel Abdulrahman ◽  
Kodappully Sivaraman Siveen ◽  
Jensa Mariam Joseph ◽  
Aisha Osman ◽  
Huseyin C. Yalcin ◽  
...  
Keyword(s):  
Lung Adenocarcinoma ◽  
Human Lung ◽  
S6 Kinase ◽  
Human Lung Adenocarcinoma ◽  
Adenocarcinoma Cells ◽  
Human Lung Adenocarcinoma Cells ◽  
Lung Adenocarcinoma Cells ◽  
P90 Ribosomal S6 Kinase ◽  
Ribosomal S6 Kinase

scholarly journals Human melanoma cells resistant to MAPK inhibitors can be effectively targeted by inhibition of the p90 ribosomal S6 kinase

Oncotarget ◽  
2017 ◽  
Vol 8 (22) ◽  
pp. 35761-35775 ◽  
Author(s):  
Corinna Kosnopfel ◽  
Tobias Sinnberg ◽  
Birgit Sauer ◽  
Heike Niessner ◽  
Anja Schmitt ◽  
...  
Keyword(s):  
Melanoma Cells ◽  
Human Melanoma ◽  
S6 Kinase ◽  
Human Melanoma Cells ◽  
P90 Ribosomal S6 Kinase ◽  
Mapk Inhibitors ◽  
Ribosomal S6 Kinase
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