Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α.
Sign Up to like & getrecommendations! Published in 2018 at "Chemical communications"
DOI: 10.1039/c8cc06128a
Abstract: Conformational transitions in protein kinases are crucial for the biological function of these enzymes. Here, we characterize and assess conformational equilibria of the activation loop and the effect of small molecule inhibitors in the MAP… read more here.
Keywords: equilibria activation; kinase p38; conformational equilibria; activation loop ... See more keywords
Induction of FGFR4 by H. pylori via STAT3 with a feedforward activation loop involving SRC signaling in gastric cancer.
Sign Up to like & getrecommendations! Published in 2022 at "Gastroenterology"
DOI: 10.1053/j.gastro.2022.05.016
Abstract: BACKGROUND & AIMS Helicobacter pylori (H. pylori) infection is the main risk factor for gastric cancer. The role of Fibroblast Growth Factor Receptors in H. pylori-mediated gastric tumorigenesis remains largely unknown. This study investigated the… read more here.
Keywords: activation loop; fgfr4; feedforward activation; gastric cancer ... See more keywords
Kincore: a web resource for structural classification of protein kinases and their inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Nucleic acids research"
DOI: 10.1093/nar/gkab920
Abstract: The active form of kinases is shared across different family members, as are several commonly observed inactive forms. We previously performed a clustering of the conformation of the activation loop of all protein kinase structures… read more here.
Keywords: protein; kincore web; resource structural; web resource ... See more keywords
PKD autoinhibition in trans regulates activation loop autophosphorylation in cis
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1101/2022.05.05.490744
Abstract: Phosphorylation is a ubiquitous mechanism by which signals are transduced in cells. Protein kinases, enzymes that catalyze the phospho-transfer reaction are, themselves, often regulated by phosphorylation. Paradoxically, however, a substantial fraction of the more than… read more here.
Keywords: activation loop; phosphorylation; activation; loop autophosphorylation ... See more keywords
The KLDpT activation loop motif is critical for MARK kinase activity
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DOI: 10.1371/journal.pone.0225727
Abstract: MAP/microtubule-affinity regulating kinases (MARK1-4) are members of the AMPK family of Ser/Thr-specific kinases, which phosphorylate substrates at consensus LXRXXSXXXL motifs. Within microtubule-associated proteins, MARKs also mediate phosphorylation of variant KXGS or ζXKXGSXXNΨ motifs, interfering with… read more here.
Keywords: loop motif; kldpt activation; kinase; activity ... See more keywords
Evolutionary divergence in the conformational landscapes of tyrosine vs serine/threonine kinases
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DOI: 10.7554/elife.83368
Abstract: Inactive conformations of protein kinase catalytic domains where the DFG motif has a “DFG-out” orientation and the activation loop is folded present a druggable binding pocket that is targeted by FDA-approved “type-II inhibitors” in the… read more here.
Keywords: threonine kinases; loop; energy; activation loop ... See more keywords