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   Articles with "activation loop" as a keyword



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Cocrystallization of the Src-Family Kinase Hck with the ATP-Site Inhibitor A-419259 Stabilizes an Extended Activation Loop Conformation

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recommendations! Published in 2024 at "Biochemistry"

DOI: 10.1021/acs.biochem.4c00323

Abstract: Hematopoietic cell kinase (Hck) is a member of the Src kinase family and is a promising drug target in myeloid leukemias. Here, we report the crystal structure of human Hck in complex with the pyrrolopyrimidine… read more here.

Keywords: conformation; site; inhibitor; activation loop ... See more keywords

Ruxolitinib mediated paradoxical JAK2 hyperphosphorylation is due to the protection of activation loop tyrosines from phosphatases

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recommendations! Published in 2025 at "Leukemia"

DOI: 10.1038/s41375-025-02594-7

Abstract: Myelofibrosis (MF) in 50% of cases is driven by an activating JAK2 mutation, mostly V617F. Ruxolinitib is approved for the treatment of MF. Responses to ruxolitinib in MF are of limited duration. Unexpectedly, treatment of… read more here.

Keywords: jak2 hyperphosphorylation; jak2; ruxolitinib; activation loop ... See more keywords

Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α.

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recommendations! 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.

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recommendations! 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.

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recommendations! 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

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recommendations! 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

Abstract 4144: PTPTF negatively regulates c-Src kinase through the dephosphorylation of the activation loop

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recommendations! Published in 2025 at "Cancer Research"

DOI: 10.1158/1538-7445.am2025-4144

Abstract: Kinases and phosphatases play a dynamic role in the regulation of signaling propagation. c-Src is an oncogenic kinase that plays multifunctional roles in the initiation and progression of many cancers, including breast, colorectal and lung… read more here.

Keywords: src kinase; phosphorylation; activation loop; kinase ... See more keywords

The KLDpT activation loop motif is critical for MARK kinase activity

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recommendations! Published in 2019 at "PLoS ONE"

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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recommendations! Published in 2022 at "eLife"

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