Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
about
Activation and function of the MAPKs and their substrates, the MAPK-activated protein kinasesThe selectivity of protein kinase inhibitors: a further updateStructural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor DesignStructure-Activity Relationships and X-ray Structures Describing the Selectivity of Aminopyrazole Inhibitors for c-Jun N-terminal Kinase 3 (JNK3) over p38A consistent description of HYdrogen bond and DEhydration energies in protein-ligand complexes: methods behind the HYDE scoring functionDiscovery of novel orally active anti-inflammatory N-phenylpyrazolyl-N-glycinyl-hydrazone derivatives that inhibit TNF-α productionBIRB796, the inhibitor of p38 mitogen-activated protein kinase, enhances the efficacy of chemotherapeutic agents in ABCB1 overexpression cellsKinetic barriers in the isomerization of substituted ureas: implications for computer-aided drug designAn efficient rapid system for profiling the cellular activities of molecular libraries.Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approachFacile Route to Tetrasubstituted Pyrazoles Utilizing Ceric Ammonium Nitrate.Interaction of diuron and related substituted phenylureas with the Ah receptor pathway.Novel VEGFR-2 kinase inhibitors identified by the back-to-front approach.Protein kinase IKKβ-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells.Tandem mass spectrometry study of p38α kinase inhibitors and related substances.Identification of p38β as a therapeutic target for the treatment of Sézary syndrome.Novel potent imidazo[1,2-a]pyridine-N-Glycinyl-hydrazone inhibitors of TNF-α production: in vitro and in vivo studiesReview article: mitogen-activated protein kinases in chronic intestinal inflammation - targeting ancient pathways to treat modern diseases.Improving MM-GB/SA Scoring through the Application of the Variable Dielectric Model.Trypanosoma brucei S-adenosylmethionine decarboxylase N terminus is essential for allosteric activation by the regulatory subunit prozymeThe p38 MAPK inhibitor BIRB796 enhances the antitumor effects of VX680 in cervical cancer.Use of inhibitors in the study of MAP kinases.Accurate calculation of mutational effects on the thermodynamics of inhibitor binding to p38α MAP kinase: a combined computational and experimental studySD0006: a potent, selective and orally available inhibitor of p38 kinase.Trk kinase inhibitors as new treatments for cancer and pain.Development of extracellular signal-regulated kinase inhibitors.Current status of agents active against the T315I chronic myeloid leukemia phenotype.Molecular mechanisms of drug resistance in tyrosine kinases cAbl and cKit.Critical review of p38 MAP kinase inhibitors: a bioanalytical perspective.In silico fragment-based drug design.Interleukins in glioblastoma pathophysiology: implications for therapy.Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition.Molecular mechanisms involved in the regulation of cytokine production by muramyl dipeptide.Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N'-Diarylurea Derivatives.Evaluation of WO2015042088 A1 - a novel urea-based scaffold for TrkA inhibition.Design, Synthesis and Biological Evaluation of Novel Substituted N,N'-Diaryl ureas as Potent p38 Inhibitors.Use of p38 MAPK Inhibitors for the Treatment of Werner Syndrome.Gram-scale synthesis of the p38α MAPK-inhibitor VX-745 for preclinical studies into Werner syndrome.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 growthSynthetic studies toward aryl-(4-aryl-4H-[1,2,4]triazole-3-yl)-amine from 1,3-diarylthiourea as urea mimetics.
P2860
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P2860
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
description
2002 nî lūn-bûn
@nan
2002年の論文
@ja
2002年論文
@yue
2002年論文
@zh-hant
2002年論文
@zh-hk
2002年論文
@zh-mo
2002年論文
@zh-tw
2002年论文
@wuu
2002年论文
@zh
2002年论文
@zh-cn
name
Pyrazole urea-based inhibitors ...... ompound to clinical candidate.
@en
type
label
Pyrazole urea-based inhibitors ...... ompound to clinical candidate.
@en
prefLabel
Pyrazole urea-based inhibitors ...... ompound to clinical candidate.
@en
P2093
P356
P1476
Pyrazole urea-based inhibitors ...... ompound to clinical candidate.
@en
P2093
Alan Swinamer
Alfred Proto
Anne G Graham
Bernhard Klaus
Carol Torcellini
Chris Pargellis
Eugene Hickey
Jeffrey Madwed
John Regan
Liang Tong
P304
P356
10.1021/JM020057R
P407
P577
2002-07-01T00:00:00Z