Mechanisms and functions of p38 MAPK signalling
A Cuadrado, AR Nebreda - Biochemical journal, 2010 - portlandpress.com
The p38 MAPK (mitogen-activated protein kinase) signalling pathway allows cells to
interpret a wide range of external signals and respond appropriately by generating a …
interpret a wide range of external signals and respond appropriately by generating a …
Approaches to discover non-ATP site kinase inhibitors
LK Gavrin, E Saiah - MedChemComm, 2013 - pubs.rsc.org
The catalytic domain of kinases shows a high degree of sequence homology, especially for
kinases that belong to the same family. They share a common ATP binding site with a …
kinases that belong to the same family. They share a common ATP binding site with a …
Druggability assessment of allosteric proteins by dynamics simulations in the presence of probe molecules
Druggability assessment of a target protein has emerged in recent years as an important
concept in hit-to-lead optimization. A reliable and physically relevant measure of druggability …
concept in hit-to-lead optimization. A reliable and physically relevant measure of druggability …
Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases
SW Cowan-Jacob, W Jahnke… - Future medicinal …, 2014 - Taylor & Francis
Protein kinases are involved in many essential cellular processes and their deregulation can
lead to a variety of diseases, including cancer. The pharmaceutical industry has invested …
lead to a variety of diseases, including cancer. The pharmaceutical industry has invested …
Oxyresveratrol drives caspase-independent apoptosis-like cell death in MDA-MB-231 breast cancer cells through the induction of ROS
Earlier studies from our laboratory have demonstrated that Oxyresveratrol (OXY), a hydroxyl-
substituted stilbene, exhibits potent inhibition of human melanoma cell proliferation. The …
substituted stilbene, exhibits potent inhibition of human melanoma cell proliferation. The …
Proline hydroxylation primes protein kinases for autophosphorylation and activation
Activation of dual-specificity tyrosine-phosphorylation-regulated kinases 1A and 1B
(DYRK1A and DYRK1B) requires prolyl hydroxylation by PHD1 prolyl hydroxylase. Prolyl …
(DYRK1A and DYRK1B) requires prolyl hydroxylation by PHD1 prolyl hydroxylase. Prolyl …
Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase
AHE Hassan, YI Oh, CH Lee, YJ Kim… - Journal of Enzyme …, 2023 - Taylor & Francis
Phenethyl-based edelfosine-analogs with saturated, monounsaturated, or polyunsaturated
alkoxy substituents on phenyl ring were designed as novel antitumor lipids modulating p38 …
alkoxy substituents on phenyl ring were designed as novel antitumor lipids modulating p38 …
Structural basis of p38α regulation by hematopoietic tyrosine phosphatase
MAP kinases regulate essential cellular events, including cell growth, differentiation and
inflammation. The solution structure of a complete MAPK–MAPK-regulatory protein complex …
inflammation. The solution structure of a complete MAPK–MAPK-regulatory protein complex …
Combining structural and coevolution information to unveil allosteric sites
Understanding allosteric regulation in biomolecules is of great interest to pharmaceutical
research and computational methods emerged during the last decades to characterize …
research and computational methods emerged during the last decades to characterize …
Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAP-K2) as an Antiinflammatory Target: Discovery and in Vivo Activity of Selective Pyrazolo[1,5-a] …
T Kosugi, DR Mitchell, A Fujino, M Imai… - Journal of Medicinal …, 2012 - ACS Publications
A novel class of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2)
inhibitors was discovered through screening a kinase-focused library. A homology model of …
inhibitors was discovered through screening a kinase-focused library. A homology model of …