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Small molecule discoidin domain receptor kinase inhibitors and potential medical applications.
Journal of medicinal chemistry 20150423
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Defining a role for acid sphingomyelinase in the p38/interleukin-6 pathway.
The Journal of biological chemistry 20140808
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Gene expression profiles in engineered cardiac tissues respond to mechanical loading and inhibition of tyrosine kinases.
Physiological reports 20131001
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Identification of potent Yes1 kinase inhibitors using a library screening approach.
Bioorganic & medicinal chemistry letters 20130801
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Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor.
Journal of medicinal chemistry 20120913
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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]pyrimidine inhibitors using a focused library and structure-based optimization approach.
Journal of medicinal chemistry 20120809
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Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety.
Bioorganic & medicinal chemistry letters 20120801
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p38 MAPK inhibition suppresses the TLR-hypersensitive phenotype in FANCC- and FANCA-deficient mononuclear phagocytes.
Blood 20120301
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Rational approaches to improving selectivity in drug design.
Journal of medicinal chemistry 20120223
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Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α.
European journal of medicinal chemistry 20120201
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Discovery of novel orally active anti-inflammatory N-phenylpyrazolyl-N-glycinyl-hydrazone derivatives that inhibit TNF-α production.
PloS one 20120101
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Molecular dynamics simulation and free energy calculation studies of the binding mechanism of allosteric inhibitors with p38α MAP kinase.
Journal of chemical information and modeling 20111227
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Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor.
Nature chemical biology 20111225
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Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Bioorganic & medicinal chemistry letters 20111201
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Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.
Journal of medicinal chemistry 20111124
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1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
Journal of medicinal chemistry 20111124
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Indolin-2-one p38α inhibitors III: bioisosteric amide replacement.
Bioorganic & medicinal chemistry letters 20111101
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Comprehensive analysis of kinase inhibitor selectivity.
Nature biotechnology 20111030
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A possible mechanism for hepatotoxicity induced by BIRB-796, an orally active p38 mitogen-activated protein kinase inhibitor.
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Design, synthesis, and biological activity of urea derivatives as anaplastic lymphoma kinase inhibitors.
ChemMedChem 20110905
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Synergistic effects of p38 mitogen-activated protein kinase inhibition with a corticosteroid in alveolar macrophages from patients with chronic obstructive pulmonary disease.
The Journal of pharmacology and experimental therapeutics 20110901
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Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
European journal of medicinal chemistry 20110601
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Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
Chemistry & biology 20101124
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Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α.
Bioorganic & medicinal chemistry letters 20101001
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X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.
Bioorganic & medicinal chemistry letters 20100901
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The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.
Bioorganic & medicinal chemistry 20100801
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Analysis of imatinib and sorafenib binding to p38alpha compared with c-Abl and b-Raf provides structural insights for understanding the selectivity of inhibitors targeting the DFG-out form of protein kinases.
Biochemistry 20100504
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Mitogen-activated protein kinase phosphatase-1 negatively regulates the expression of interleukin-6, interleukin-8, and cyclooxygenase-2 in A549 human lung epithelial cells.
The Journal of pharmacology and experimental therapeutics 20100401
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Displacement assay for the detection of stabilizers of inactive kinase conformations.
Journal of medicinal chemistry 20100114
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Role of protein haptenation in triggering maturation events in the dendritic cell surrogate cell line THP-1.
Toxicology and applied pharmacology 20090715
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A new screening assay for allosteric inhibitors of cSrc.
Nature chemical biology 20090601
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Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design.
The Journal of biological chemistry 20090508
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Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.
Bioorganic & medicinal chemistry letters 20090501
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Phosphorylation of Ewing's sarcoma protein (EWS) and EWS-Fli1 in response to DNA damage.
The Biochemical journal 20090315
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Inhibition of p38: has the fat lady sung?
Arthritis and rheumatism 20090201
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Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Bioorganic & medicinal chemistry letters 20080801
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Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.
Journal of medicinal chemistry 20080724
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Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.
Bioorganic & medicinal chemistry letters 20080701
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Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase.
Bioorganic & medicinal chemistry letters 20080601
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The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
Bioorganic & medicinal chemistry letters 20080315
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A quantitative analysis of kinase inhibitor selectivity.
Nature biotechnology 20080101
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The selectivity of protein kinase inhibitors: a further update.
The Biochemical journal 20071215
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New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.
Bioorganic & medicinal chemistry letters 20070801
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Targeted therapy and the T315I mutation in Philadelphia-positive leukemias.
Haematologica 20070401
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p38 mitogen-activated protein kinase inhibition ameliorates angiotensin II-induced target organ damage.
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BIRB 796 enhances cytotoxicity triggered by bortezomib, heat shock protein (Hsp) 90 inhibitor, and dexamethasone via inhibition of p38 mitogen-activated protein kinase/Hsp27 pathway in multiple myeloma cell lines and inhibits paracrine tumour growth.
British journal of haematology 20070201
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The role of IFN-gamma in regulation of IFN-gamma-inducible protein 10 (IP-10) expression in lung epithelial cell and peripheral blood mononuclear cell co-cultures.
Respiratory research 20070101
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Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors.
Journal of medicinal chemistry 20061228
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Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.
Bioorganic & medicinal chemistry letters 20061215
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Microwave-assisted synthesis of N-pyrazole ureas and the p38alpha inhibitor BIRB 796 for study into accelerated cell ageing.
Organic & biomolecular chemistry 20061121
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Homogeneous time-resolved fluorescence and its applications for kinase assays in drug discovery.
Analytical biochemistry 20060915
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Enzyme fragment complementation binding assay for p38alpha mitogen-activated protein kinase to study the binding kinetics of enzyme inhibitors.
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Nature chemical biology 20060701
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Nature biotechnology 20051001
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Chemistry & biology 20050601
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BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo.
The Journal of biological chemistry 20050520
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HierS: hierarchical scaffold clustering using topological chemical graphs.
Journal of medicinal chemistry 20050505
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A small molecule-kinase interaction map for clinical kinase inhibitors.
Nature biotechnology 20050301
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P38 mitogen activated protein kinase is involved in the downregulation of granulocyte CXC chemokine receptors 1 and 2 during human endotoxemia.
Journal of clinical immunology 20040101
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Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.
Journal of medicinal chemistry 20031023
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Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).
Journal of medicinal chemistry 20031023
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The kinetics of binding to p38MAP kinase by analogues of BIRB 796.
Bioorganic & medicinal chemistry letters 20030915
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Anti-arthritic agents--SMi conference: trapping cytokines. 28-29 April 2003, London, UK.
IDrugs : the investigational drugs journal 20030601
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Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
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Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site.
Nature structural biology 20020401