Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α-Reference-Cited by-同舟云学术

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

Published:2018 Issue:85 Volume:54 Page:12057-12060
ISSN:1359-7345
Container-title:Chemical Communications
language:en
Short-container-title:Chem. Commun.

Author:

Roser Patrick¹²³⁴⁵^ORCID,Weisner Jörn⁶⁷⁸⁵,Simard Jeffrey R.⁶⁷⁸⁵,Rauh Daniel⁶⁷⁸⁵^ORCID,Drescher Malte¹²³⁴⁵^ORCID

Affiliation:

1. Department of Chemistry and Konstanz Research School Chemical Biology

2. (KoRS-CB)

3. University of Konstanz

4. 78457 Konstanz

5. Germany

6. Faculty of Chemistry and Chemical Biology

7. TU Dortmund University

8. 44227 Dortmund

Abstract

Roser et al. characterize and assess conformational equilibria of the activation loop and the effect of small molecule inhibitors in the MAP kinase p38α. Their work experimentally revealed the existence of a two-state equilibrium while the addition of inhibitors shifts the equilibrium between these two states.

Funder

Deutsche Forschungsgemeinschaft

Bundesministerium für Bildung und Forschung

Publisher

Royal Society of Chemistry (RSC)

Subject

Materials Chemistry,Metals and Alloys,Surfaces, Coatings and Films,General Chemistry,Ceramics and Composites,Electronic, Optical and Magnetic Materials,Catalysis

Link

http://pubs.rsc.org/en/content/articlepdf/2018/CC/C8CC06128A

Reference28 articles.

1. Mammalian MAP kinase signalling cascades

2. Advances in kinase targeting: current clinical use and clinical trials

3. The p38 MAP kinase pathway as a therapeutic target in inflammatory disease

4. p38 MAP kinases: key signalling molecules as therapeutic targets for inflammatory diseases

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