DFG-in and DFG-out homology models of TrkB kinase receptor: Induced-fit and ensemble docking
Keywords: مهار کننده های کیناز; Kinase inhibitors; DFG-in and DFG-out; TrkB
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Synthesis and structure–activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase
Keywords: مهار کننده های کیناز; Anaplastic lymphoma kinase; Kinase inhibitors
De-regulated FGF receptors as therapeutic targets in cancer
Keywords: مهار کننده های کیناز; Cancer; FGFR; Kinase inhibitors; Signal transduction; TherapeuticsCML, chronic myeloid leukaemia; DAG, diacylglycerol; Der, derivative chromosome; DUSP, dual specificity phosphatase; EGFR, epidermal growth factor receptor; EMS, 8p11 myeloproliferative syn
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds
Keywords: مهار کننده های کیناز; WKFRHTGMVITXBX-UHFFFAOYSA-N; Boc; tert-butoxycarbonyl; BRAF; V-RAF murine sarcoma viral oncogene homolog B1; DCM; dichloromethane; DMF; dimethylformamide; ERK; extracellular regulated kinase; MAPK; mitogen-activated protein kinase; MEK; MAPK/ERK kinase; M
Fragment-based discovery of JAK-2 inhibitors
Keywords: مهار کننده های کیناز; Fragment-based design; JAK-2 inhibitors; Structure-based design; Aminoindazole; Kinase inhibitors
Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2α (HRI) kinase
Keywords: مهار کننده های کیناز; Anemia; Kinase inhibitors; Hemoglobin; HRI kinase; Blood
Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors
Keywords: مهار کننده های کیناز; GSK-3; CDK5; Kinase inhibitors; Alzheimer’s disease; Pyrazolo[3,4-b]pyridines; 3,6-Diamino-1H-pyrazolo[3,4-b]pyridine-5-carbonitriles; Molecular modelling
Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR
Keywords: مهار کننده های کیناز; Mammalian target of rapamycin; mTOR; Kinase inhibitors; Phosphatidylinositol 3-kinase; PI3K
Imidazo[1,2-a]pyrazine diaryl ureas: Inhibitors of the receptor tyrosine kinase EphB4
Keywords: مهار کننده های کیناز; Imidazo[1,2-a]pyrazine; Small molecule drug discovery; EphB4; VEGFR2; Tie2; Receptor tyrosine kinase; Multiplex kinase inhibitors; Anti-angiogenesis; Diaryl ureas; Kinase inhibitors;
Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins
Keywords: مهار کننده های کیناز; Meridianins; Suzuki cross-coupling; Kinase inhibitors; Dyrk1A inhibitors
Induction of macrophage migration by neurotoxic prion protein fragment
Keywords: مهار کننده های کیناز; PrP106-126; Ana-1 macrophages; Chemotaxis assay; Kinase inhibitors; Substance P;
Design, synthesis, screening, and molecular modeling study of a new series of ROS1 receptor tyrosine kinase inhibitors
Keywords: مهار کننده های کیناز; Kinase inhibitors; ROS1; Glioblastoma multiforme; Homology modeling; Pyrazole
Synthesis, kinase inhibitory potencies and in vitro antiproliferative activity of isoindigo and 7′-azaisoindigo derivatives substituted by Sonogashira cross-coupling
Keywords: مهار کننده های کیناز; Indigoids; Isoindigos; Kinase inhibitors; Antitumour agents
Treatment of Advanced and Metastatic Renal Cancer: A Revolution?
Keywords: مهار کننده های کیناز; Cytokines; Immunotherapy; Kidney cancer; Kinase inhibitors; Nephrectomy; Renal cell carcinoma; Targeted therapy
Regioselective halogenation of aminopyrimidinyl-pyrrole carboxylic acid derivatives
Keywords: مهار کننده های کیناز; Pyrimidine; Pyrrole; N-Halosuccinimide; Halogenation; Kinase inhibitors;
Advances in the biology and therapy of patients with chronic myeloid leukaemia
Keywords: مهار کننده های کیناز; Chronic myeloid leukemia; Management; Kinase inhibitors; T315I mutation;
Management of Drug Toxicities in Chronic Myeloid Leukaemia
Keywords: مهار کننده های کیناز; CML; toxicity; kinase inhibitors
Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer
Keywords: مهار کننده های کیناز; CSF-1R; Kinase inhibitors; Bisamide; Thiazole
Identification of novel protein kinase CK1 delta (CK1δ) inhibitors through structure-based virtual screening
Keywords: مهار کننده های کیناز; Protein kinase CK1 delta; Kinase inhibitors; Structure-based virtual screening; Molecular docking
Synthesis and biological evaluation of novel 2,4,5-triaryl-1H-pyrazol-3(2H)-ones as inhibitors of ALK5
Keywords: مهار کننده های کیناز; Activin-like kinases5 (ALK5); Kinase inhibitors; 1H-Pyrazol-3(2H)-ones
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3)
Keywords: مهار کننده های کیناز; Kinase inhibitors; GSK-3; Aurora A; Diabetes; Alzheimer’s; Depression; Bipolar disorder; Molecular modeling
Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors
Keywords: مهار کننده های کیناز; VEGFR-2; Kinase inhibitors; Pyrrolo[2,1-f][1,2,4]triazine;
Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7
Keywords: مهار کننده های کیناز; Malaria; Kinase inhibitors; Imidazopyridazines
Dual binding site inhibitors of B-RAF kinase
Keywords: مهار کننده های کیناز; B-RAF; Kinase inhibitors; Diarylimidazoles
Identification of pharmacological inhibitors of the MEK5/ERK5 pathway
Keywords: مهار کننده های کیناز; MEK5; ERK5; Kinase inhibitors; Pharmacological inhibitors
Fingerprint-based clustering applied to define a QSAR model use radius
Keywords: مهار کننده های کیناز; QSAR validation; GRAS; Kinase inhibitors; Skin permeability
Effects of growth factors and kinase inhibitors on the properties of human adipose-stromal cells in different culture conditions
Keywords: مهار کننده های کیناز; Human adipose tissue-derived stromal cells; Growth factors; Kinase inhibitors; Human serum-contained media; Fetal bovine serum-contained media;
Intervention in growth factor activated signaling pathways by renally targeted kinase inhibitors
Keywords: مهار کننده های کیناز; Drug targeting; Kidney; Linker technology; Kinase inhibitors; Fibrosis
Targeted therapies in gastrointestinal stromal tumors
Keywords: مهار کننده های کیناز; GIST; Targeted therapy; Kinase inhibitors; Imatinib; Sunitinib;
The JAK kinases: Not just another kinase drug discovery target
Keywords: مهار کننده های کیناز; Review; JAK; Kinase inhibitors; Myeloproliferative disorders; Cancer;
Molecular cancer therapy: Can our expectation be MET?
Keywords: مهار کننده های کیناز; Tyrosine kinase receptors; MET/hepatocyte growth factor receptor; Targeted therapy; Kinase inhibitors; Clinical trials
Resorcylic acid lactones: A pluripotent scaffold with therapeutic potential
Keywords: مهار کننده های کیناز; Resorcylic acid lactones (RALs); Kinase inhibitors; HSP90; Total synthesis; Combinatorial synthesis; Solid-phase synthesis; Polymer supported reagentsLactone de l'acide resorcyclique; Inhibiteurs de kinasas; HSP90; Synthèse total; Synthèse combinatoire; P
Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors
Keywords: مهار کننده های کیناز; CDK2; Kinase inhibitors; Pyrazolo[1,5-a]pyrimidine
Discovery of thienopyridines as Src-family selective Lck inhibitors
Keywords: مهار کننده های کیناز; Lck inhibitors; Src-family; Kinase inhibitors; Thienopyridines
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: Development of an expedient and divergent synthetic route and preliminary SAR
Keywords: مهار کننده های کیناز; Lymphocyte specific kinase (Lck); Anti-inflammatory; Kinase inhibitors; Furopyrimidine
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors
Keywords: مهار کننده های کیناز; KDR kinase; VEGFR-2 kinase; Kinase inhibitors; 1,2,3-Thiadiazole-pyrazolones
Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk
Keywords: مهار کننده های کیناز; Pfmrk; CDK7; Protein kinase A; Malaria; Plasmodium falciparum; Kinase inhibitors; Cyclin dependent protein kinase; Anti-malarials; Drug target; Parasite
Erythropoietin protects cardiac myocytes against anthracycline-induced apoptosis
Keywords: مهار کننده های کیناز; Erythropoietin; Cardiac myocyte; Apoptosis; Anthracycline; Kinase inhibitors;
Effect of the branched-chain α-keto acids accumulating in maple syrup urine disease on S100B release from glial cells
Keywords: مهار کننده های کیناز; Branched-chain α-keto acids; Maple syrup urine disease; S100B; Antioxidants; Creatine; Kinase inhibitors
Synthesis and structure–activity relationship of 3,4′-bispyridinylethylenes: Discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer
Keywords: مهار کننده های کیناز; Inhibitors of Akt; Akt1; Akt2; Akt3; PKA; PKB; protein kinase B; GSK3; FL5.12-Akt1; X-ray; Anticancer; Apoptosis; Antitumor; Pharmacokinetics; Kinase inhibitors; Structure-based design
Synthesis of aminopyrimidylindoles structurally related to meridianins
Keywords: مهار کننده های کیناز; Meridianins; Kinase inhibitors; Pyrimidine; Indole; Antitumor agents;
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors
Keywords: مهار کننده های کیناز; c-src; RET; Kinase inhibitors; 4-Anilinoquinolines
Macrocyclic ureas as potent and selective Chk1 inhibitors: An improved synthesis, kinome profiling, structure–activity relationships, and preliminary pharmacokinetics
Keywords: مهار کننده های کیناز; Checkpoint kinase 1; Chk1; Ureas; Kinase inhibitors; Macrocycles; Ring-closure metathesis; DNA damage
Comparative molecular field analysis of flavonoid inhibitors of the PIM-1 kinase
Keywords: مهار کننده های کیناز; Pim-1; Comparative molecular field analysis (CoMFA); Flavonoids; Kinase inhibitors
Report of the IWGT working group on strategy/interpretation for regulatory in vivo tests: II. Identification of in vivo-only positive compounds in the bone marrow micronucleus test
Keywords: مهار کننده های کیناز; IWGT; Genotoxicity tests; In vivo; Rodent bone marrow; Micronucleus test; In vivo-only positive compounds; ADME; In vitro versus in vivo metabolism; Sex-specific metabolism; Influence of gut flora; Pharmacological mechanisms; Kinase inhibitors; Regulatory
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors
Keywords: مهار کننده های کیناز; Thienopyrazoles; Kinase inhibitors; KDR inhibitors; Targeted libraries; De novo design
Induction of prolactin expression and release in human preadipocytes by cAMP activating ligands
Keywords: مهار کننده های کیناز; Prolactin; Breast preadipocytes; Differentiation; IBMX; Isoproterenol; PACAP; Kinase inhibitors; Superdistal prolactin promoter
BrainâDerived Neurotrophic Factor (BDNF) Acts Primarily via the JAK/STAT Pathway to Promote Neurite Growth in the Major Pelvic Ganglion of the Rat: Part 2
Keywords: مهار کننده های کیناز; BDNF; Neurotrophin Receptors; Major Pelvic Ganglia; JAK/STAT Pathway; Impotence; Kinase Inhibitors;
Feature-similarity protein classifier as a ligand engineering tool
Keywords: مهار کننده های کیناز; Kinase inhibitors; Selectivity
Synthesis of 3-substituted-2-oxoindole analogues and their evaluation as kinase inhibitors, anticancer and antiangiogenic agents
Keywords: مهار کننده های کیناز; Indolinone; Kinase inhibitors