scholarly journals Molecular Origin of the Binding of WWOX Tumor Suppressor to ErbB4 Receptor Tyrosine Kinase

Biochemistry ◽  
2013 ◽  
Vol 52 (51) ◽  
pp. 9223-9236 ◽  
Author(s):  
Brett J. Schuchardt ◽  
Vikas Bhat ◽  
David C. Mikles ◽  
Caleb B. McDonald ◽  
Marius Sudol ◽  
...  
Keyword(s):  
Tumor Suppressor ◽  
Tyrosine Kinase ◽  
Receptor Tyrosine Kinase ◽  
Erbb4 Receptor ◽  
Molecular Origin

Abstract 1245: Screening methodologies for the discovery of small molecule melanoma therapeutics targeted at the ErbB4 receptor tyrosine kinase

2017 ◽  
Author(s):  
Richard L. Cullum ◽  
John T. Piazza ◽  
Jared I. Senfeld ◽  
Logan T. Neel ◽  
Ram B. Gupta ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Small Molecule ◽  
Receptor Tyrosine Kinase ◽  
Erbb4 Receptor

scholarly journals Receptor tyrosine kinase activation of RhoA is mediated by AKT phosphorylation of DLC1

2017 ◽  
Vol 216 (12) ◽  
pp. 4255-4270 ◽  
Author(s):  
Brajendra K. Tripathi ◽  
Tiera Grant ◽  
Xiaolan Qian ◽  
Ming Zhou ◽  
Philipp Mertins ◽  
...  
Keyword(s):  
Tumor Suppressor ◽  
Tyrosine Kinase ◽  
Cell Line ◽  
Receptor Tyrosine Kinase ◽  
Rho Gtpase ◽  
Focal Adhesions ◽  
Cancer Cell Line ◽  
Suppressor Activity ◽  
Akt Phosphorylation ◽  
Transformed Cell Lines

We report several receptor tyrosine kinase (RTK) ligands increase RhoA–guanosine triphosphate (GTP) in untransformed and transformed cell lines and determine this phenomenon depends on the RTKs activating the AKT serine/threonine kinase. The increased RhoA-GTP results from AKT phosphorylating three serines (S298, S329, and S567) in the DLC1 tumor suppressor, a Rho GTPase-activating protein (RhoGAP) associated with focal adhesions. Phosphorylation of the serines, located N-terminal to the DLC1 RhoGAP domain, induces strong binding of that N-terminal region to the RhoGAP domain, converting DLC1 from an open, active dimer to a closed, inactive monomer. That binding, which interferes with the interaction of RhoA-GTP with the RhoGAP domain, reduces the hydrolysis of RhoA-GTP, the binding of other DLC1 ligands, and the colocalization of DLC1 with focal adhesions and attenuates tumor suppressor activity. DLC1 is a critical AKT target in DLC1-positive cancer because AKT inhibition has potent antitumor activity in the DLC1-positive transgenic cancer model and in a DLC1-positive cancer cell line but not in an isogenic DLC1-negative cell line.

scholarly journals The Receptor Tyrosine Kinase Regulator Sprouty1 Is a Target of the Tumor Suppressor WT1 and Important for Kidney Development

2003 ◽  
Vol 278 (42) ◽  
pp. 41420-41430 ◽  
Author(s):  
Isabelle Gross ◽  
Debra J. Morrison ◽  
Deborah P. Hyink ◽  
Kylie Georgas ◽  
Milton A. English ◽  
...  
Keyword(s):  
Tumor Suppressor ◽  
Tyrosine Kinase ◽  
Receptor Tyrosine Kinase ◽  
Kidney Development

scholarly journals Molecular basis of the binding of YAP transcriptional regulator to the ErbB4 receptor tyrosine kinase

Biochimie ◽  
2014 ◽  
Vol 101 ◽  
pp. 192-202 ◽  
Author(s):  
Brett J. Schuchardt ◽  
Vikas Bhat ◽  
David C. Mikles ◽  
Caleb B. McDonald ◽  
Marius Sudol ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Receptor Tyrosine Kinase ◽  
Molecular Basis ◽  
Transcriptional Regulator ◽  
Erbb4 Receptor
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