Regulation of Tumorigenesis by p38α MAP Kinase

2007 ◽  
pp. 99-128 ◽  
Author(s):  
Ignacio Dolado ◽  
Angel R. Nebreda
Keyword(s):  
Map Kinase ◽  
P38α Map Kinase

Modelling Flexible Protein-Ligand Binding in p38α MAP Kinase using the QUBE Force Field

2019 ◽  
Author(s):  
Joshua Horton ◽  
Alice Allen ◽  
Daniel Cole
Keyword(s):  
Quantum Mechanics ◽  
Force Field ◽  
Map Kinase ◽  
Binding Free Energy ◽  
Quantum Mechanical ◽  
Enhanced Sampling ◽  
Relative Binding ◽  
Stringent Test ◽  
Flexible Protein ◽  
P38α Map Kinase

<div><div><div><p>The quantum mechanical bespoke (QUBE) force field is used to retrospectively calculate the relative binding free energy of a series of 17 flexible inhibitors of p38α MAP kinase. The size and flexibility of the chosen molecules represent a stringent test of the derivation of force field parameters from quantum mechanics, and enhanced sampling is required to reduce the dependence of the results on the starting structure. Competitive accuracy with a widely-used biological force field is achieved, indicating that quantum mechanics derived force fields are approaching the accuracy required to provide guidance in prospective drug discovery campaigns.</p></div></div></div>

N-Phenyl-N-purin-6-yl ureas: The design and synthesis of p38α MAP kinase inhibitors

2003 ◽  
Vol 13 (6) ◽  
pp. 1191-1194 ◽  
Author(s):  
Zehong Wan ◽  
Jeffrey C. Boehm ◽  
Michael J. Bower ◽  
Shouki Kassis ◽  
John C. Lee ◽  
...  
Keyword(s):  
Map Kinase ◽  
Kinase Inhibitors ◽  
Design And Synthesis ◽  
P38α Map Kinase

Design of Potent and Selective 2-Aminobenzimidazole-Based p38α MAP Kinase Inhibitors with Excellent in Vivo Efficacy

2005 ◽  
Vol 48 (7) ◽  
pp. 2270-2273 ◽  
Author(s):  
Alfonso de Dios ◽  
Chuan Shih ◽  
Beatriz López de Uralde ◽  
Concepción Sánchez ◽  
Miriam del Prado ◽  
...  
Keyword(s):  
Map Kinase ◽  
Kinase Inhibitors ◽  
In Vivo Efficacy ◽  
P38α Map Kinase

scholarly journals The role of Pitx2 and Pitx3 in muscle stem cells gives new insights into P38α MAP kinase and redox regulation of muscle regeneration

eLife ◽  
2018 ◽  
Vol 7 ◽  
Author(s):  
Aurore L'honoré ◽  
Pierre-Henri Commère ◽  
Elisa Negroni ◽  
Giorgia Pallafacchina ◽  
Bertrand Friguet ◽  
...  
Keyword(s):  
Stem Cells ◽  
Map Kinase ◽  
Satellite Cells ◽  
Muscle Regeneration ◽  
Redox Regulation ◽  
Primary Cultures ◽  
Rapid Expansion ◽  
Skeletal Muscle Regeneration ◽  
Muscle Stem Cells ◽  
P38α Map Kinase

Skeletal muscle regeneration depends on satellite cells. After injury these muscle stem cells exit quiescence, proliferate and differentiate to regenerate damaged fibres. We show that this progression is accompanied by metabolic changes leading to increased production of reactive oxygen species (ROS). Using Pitx2/3 single and double mutant mice that provide genetic models of deregulated redox states, we demonstrate that moderate overproduction of ROS results in premature differentiation of satellite cells while high levels lead to their senescence and regenerative failure. Using the ROS scavenger, N-Acetyl-Cysteine (NAC), in primary cultures we show that a physiological increase in ROS is required for satellite cells to exit the cell cycle and initiate differentiation through the redox activation of p38α MAP kinase. Subjecting cultured satellite cells to transient inhibition of P38α MAP kinase in conjunction with NAC treatment leads to their rapid expansion, with striking improvement of their regenerative potential in grafting experiments.

Dibenzepinones, dibenzoxepines and benzosuberones based p38α MAP kinase inhibitors: Their pharmacophore modelling, 3D-QSAR and docking studies

2019 ◽  
Vol 110 ◽  
pp. 175-185 ◽  
Author(s):  
Mohemmed Faraz Khan ◽  
Garima Verma ◽  
Perwez Alam ◽  
Mymoona Akhter ◽  
Md Afroz Bakht ◽  
...  
Keyword(s):  
Map Kinase ◽  
Kinase Inhibitors ◽  
3D Qsar ◽  
Docking Studies ◽  
Pharmacophore Modelling ◽  
P38α Map Kinase

Kinetic and mechanistic studies of p38α MAP kinase phosphorylation by MKK 6

FEBS Journal ◽  
2019 ◽  
Vol 286 (5) ◽  
pp. 1030-1052 ◽  
Author(s):  
Yu‐Lu Wang ◽  
Yuan‐Yuan Zhang ◽  
Chang Lu ◽  
Wenhao Zhang ◽  
Haiteng Deng ◽  
...  
Keyword(s):  
Map Kinase ◽  
Mechanistic Studies ◽  
Kinase Phosphorylation ◽  
P38α Map Kinase

Dynamics in the p38α MAP Kinase–SB203580 Complex Observed by Liquid-State NMR Spectroscopy

2008 ◽  
Vol 47 (19) ◽  
pp. 3548-3551 ◽  
Author(s):  
Valerie S. Honndorf ◽  
Nicolas Coudevylle ◽  
Stefan Laufer ◽  
Stefan Becker ◽  
Christian Griesinger
Keyword(s):  
Nmr Spectroscopy ◽  
Map Kinase ◽  
Liquid State ◽  
P38α Map Kinase
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