Development of Novel In Vivo Chemical Probes to Address CNS Protein Kinase Involvement in Synaptic Dysfunction

Is the Amyloid Hypothesis of Alzheimer's disease therapeutically relevant?

(2012) Andrew F. Teich et al.   BIOCHEMICAL JOURNAL

New Directions in Targeting Protein Kinases: Focusing Upon True Allosteric and Bivalent Inhibitors

(2012) Vandana Lamba et al.   CURRENT PHARMACEUTICAL DESIGN

Synthesis of quinoline derivatives: Discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease

(2012) Jole Fiorito et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting the Hinge Glycine Flip and the Activation Loop: Novel Approach to Potent p38α Inhibitors

(2012) Kathrin E. Martz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-based 3D-QSAR models and dynamics analysis of novel N-benzyl pyridinone as p38α MAP kinase inhibitors for anticytokine activity

(2012) Zaheer Ul-Haq et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Early Stage Drug Treatment That Normalizes Proinflammatory Cytokine Production Attenuates Synaptic Dysfunction in a Mouse Model That Exhibits Age-Dependent Progression of Alzheimer's Disease-Related Pathology

(2012) A. D. Bachstetter et al.   JOURNAL OF NEUROSCIENCE

Diaminopyridine-Based Potent and Selective Mps1 Kinase Inhibitors Binding to an Unusual Flipped-Peptide Conformation

(2012) Ken-ichi Kusakabe et al.   ACS Medicinal Chemistry Letters

Substituted N -aryl-6-pyrimidinones: A new class of potent, selective, and orally active p38 MAP kinase inhibitors

(2011) Balekudru Devadas et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Indolin-2-one p38α inhibitors I: Design, profiling and crystallographic binding mode

(2011) Paul Eastwood et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition of Wnt/β-Catenin Signaling by p38 MAP Kinase Inhibitors Is Explained by Cross-Reactivity with Casein Kinase Iδ/ɛ

(2011) Folkert Verkaar et al.   CHEMISTRY & BIOLOGY

1,7-Naphthyridine 1-Oxides as Novel Potent and Selective Inhibitors of p38 Mitogen Activated Protein Kinase

(2011) Wenceslao Lumeras et al.   JOURNAL OF MEDICINAL CHEMISTRY

Microglial p38α MAPK is a key regulator of proinflammatory cytokine up-regulation induced by toll-like receptor (TLR) ligands or beta-amyloid (Aβ)

(2011) Adam D Bachstetter et al.   Journal of Neuroinflammation

The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor

(2011) John P. Duffy et al.   ACS Medicinal Chemistry Letters

Review: Disruption of the Postsynaptic Density in Alzheimer’s Disease and Other Neurodegenerative Dementias

(2010) Yuesong Gong et al.   American Journal of Alzheimers Disease and Other Dementias

Non-ATP Competitive Protein Kinase Inhibitors

(2010) L. Garuti et al.   CURRENT MEDICINAL CHEMISTRY

Discovery and Evaluation of 7-Alkyl-1,5-bis-aryl-pyrazolopyridinones as Highly Potent, Selective, and Orally Efficacious Inhibitors of p38α Mitogen-Activated Protein Kinase⊥⊥ Atomic coordinates and structure factors for crystal structure of compound3dwith p38α can be accessed using PDB code 3LHJ.

(2010) Liping H. Pettus et al.   JOURNAL OF MEDICINAL CHEMISTRY

The three-dimensional structure of MAP kinase p38β: different features of the ATP-binding site in p38β compared with p38α

(2009) Sangita B. Patel et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Structural Bioinformatics-Based Prediction of Exceptional Selectivity of p38 MAP Kinase Inhibitor PH-797804

(2009) Li Xing et al.   BIOCHEMISTRY

Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase

(2009) Shaun R. Selness et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition

(2009) Kevin D. Jerome et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular Properties and CYP2D6 Substrates: Central Nervous System Therapeutics Case Study and Pattern Analysis of a Substrate Database

(2009) L. K. Chico et al.   DRUG METABOLISM AND DISPOSITION

Design, Synthesis, and Structure−Activity Relationships of AminopyridineN-Oxides, a Novel Scaffold for the Potent and Selective Inhibition of p38 Mitogen Activated Protein Kinase

(2009) Wenceslao Lumeras et al.   JOURNAL OF MEDICINAL CHEMISTRY

Picomolar Amyloid-  Positively Modulates Synaptic Plasticity and Memory in Hippocampus

(2009) D. Puzzo et al.   JOURNAL OF NEUROSCIENCE

Targeting protein kinases in central nervous system disorders

(2009) Laura K. Chico et al.   NATURE REVIEWS DRUG DISCOVERY

Protection against β-amyloid induced abnormal synaptic function and cell death by Ginkgolide J

(2007) Ottavio Vitolo et al.   NEUROBIOLOGY OF AGING