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

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2018
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Weisner, Jörn
Simard, Jeffrey R.
Rauh, Daniel
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Chemical Communications : ChemComm. 2018, 54(85), pp. 12057-12060. ISSN 1359-7345. eISSN 1364-548X. Available under: doi: 10.1039/c8cc06128a
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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 kinase p38α. Our work experimentally revealed the existence of a two-state equilibrium for p38α while the addition of inhibitors shifts the equilibrium between these two states.

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ISO 690ROSER, Patrick, Jörn WEISNER, Jeffrey R. SIMARD, Daniel RAUH, Malte DRESCHER, 2018. Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α. In: Chemical Communications : ChemComm. 2018, 54(85), pp. 12057-12060. ISSN 1359-7345. eISSN 1364-548X. Available under: doi: 10.1039/c8cc06128a
BibTex
@article{Roser2018-10-23Direc-43852,
  year={2018},
  doi={10.1039/c8cc06128a},
  title={Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α},
  number={85},
  volume={54},
  issn={1359-7345},
  journal={Chemical Communications : ChemComm},
  pages={12057--12060},
  author={Roser, Patrick and Weisner, Jörn and Simard, Jeffrey R. and Rauh, Daniel and Drescher, Malte}
}
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