Molecular Playground/C-Raf: Difference between revisions
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>One of the [[CBI Molecules]] being studied in the [http://www.umass.edu/cbi/ University of Massachusetts Amherst Chemistry-Biology Interface Program] at UMass Amherst in the Peyton group and on display at the [http://www.molecularplayground.org Molecular Playground]. | >One of the [[CBI Molecules]] being studied in the [http://www.umass.edu/cbi/ University of Massachusetts Amherst Chemistry-Biology Interface Program] at UMass Amherst in the Peyton group and on display at the [http://www.molecularplayground.org Molecular Playground]. | ||
<applet load='3omv' size='[450,338]' frame='true' align='right' | <applet load='3omv' size='[450,338]' frame='true' align='right' | ||
caption='C-Raf [[3omv]]' scene=''User:Thuy V. Nguyen/Sandbox103/Loadedfrompdb/4'/> | caption='C-Raf complex with inhibitor [[3omv]]' scene=''User:Thuy V. Nguyen/Sandbox103/Loadedfrompdb/4'/> | ||
'''C-Raf''' (Raf1) is one of the isoforms of Raf serine/threonine kinase. The others are A-Raf and B-Raf. The Raf-kinase is activated by Ras protein. Activated Raf will trigger the phosphorylation of MEK and ERK, which regulates some transcription factors that induce gene expression required for cell proliferation. Raf1 activation is found in 50% of renal cell carcinoma and 100% of hepatocellular carcinoma (Scott Wilhelm et al., 2006). [[Sorafenib]] is an FDA approval small molecule for Raf1 inhibitor. | '''C-Raf''' (Raf1) is one of the isoforms of Raf serine/threonine kinase. The others are A-Raf and B-Raf. The Raf-kinase is activated by Ras protein. Activated Raf will trigger the phosphorylation of MEK and ERK, which regulates some transcription factors that induce gene expression required for cell proliferation. Raf1 activation is found in 50% of renal cell carcinoma and 100% of hepatocellular carcinoma (Scott Wilhelm et al., 2006). [[Sorafenib]] is an FDA approval small molecule for Raf1 inhibitor. Sorafenib also binds to B-Raf. | ||
<scene name='Molecular_Playground/C-Raf/B-raf/2'>THE COMPLEX OF WILD TYPE B-RAF AND BAY439006 (Sorafenib)</scene> | |||
==3D structures of C-Raf== | |||
[[1rfa]] – hCRAF-1 Ras-binding domain – human – NMR<br /> | |||
[[3omv]] - hCRAF-1 kinase domain <br /> | |||
[[1gua]] - hCRAF-1 Ras-binding domain + Rap1A (mutant) + guanosyl-imido-triphosphate<br /> | |||
[[3kuc]] - hCRAF-1 Ras-binding domain + Rap1A (mutant)<br /> | |||
[[3kud]] - hCRAF-1 Ras-binding domain + GTPase Hras | |||