Article
Identification and Characterization of a B-Raf Kinase α-Helix Critical for the Activity of MEK Kinase in MAPK Signaling.
Biochemistry - 22 Dec 2020
Nguyen Diep, Lin Linda Yingqi, Zhou Jeffrey O, Kibby Emily, Sia Twan W, Tillis Tiara D, Vapuryan Narine, Xu Ming-Ray, Potluri Rajiv, Shin YongJoon, Erler Elizabeth A, Bronkema Naomi, Boehlmer Daniel J, Chung Christopher D, Burkhard Caroline, Zeng Shirley H, Grasso Michael, Acevedo Lucila A, Marmorstein Ronen, Fera Daniela
Abstract excerpt
In the MAPK pathway, an oncogenic V600E mutation in B-Raf kinase causes the enzyme to be constitutively active, leading to aberrantly high phosphorylation levels of its downstream effectors, MEK and ERK kinases. The V600E mutation in B-Raf accounts for more than half of all melanomas and ∼3% of all cancers, and many drugs target the ATP binding site of the enzyme for its inhibition. Because B-Raf can develop...
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