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International journal of cancer, ISSN 0020-7136, 07/2019
Galunisertib (LY2157299), a promising small-molecule inhibitor of the transforming growth factor-beta (TGF-β) receptor, is currently in mono- and combination... 
Index Medicus
Journal Article
Journal of Investigative Dermatology, ISSN 0022-202X, 02/2007, Volume 127, Issue 2, pp. 331 - 341
Keratinocytes are continuously in contact with external stimuli and have the capacity to produce several soluble mediators. Pathogen-associated molecular... 
TOLL-LIKE-RECEPTORS | DOUBLE-STRANDED-RNA | DENDRITIC CELLS | SKIN-ASSOCIATED CHEMOKINE | MONOCYTE CHEMOATTRACTANT PROTEIN-1 | INNATE IMMUNE-RESPONSE | INFLAMMATORY PROTEIN 3-ALPHA | NECROSIS-FACTOR-ALPHA | FACTOR-KAPPA-B | HUMAN EPIDERMAL-KERATINOCYTES | DERMATOLOGY | Oligonucleotides - genetics | Phosphorylation | Toll-Like Receptor 5 - genetics | Humans | Toll-Like Receptor 9 - genetics | I-kappa B Proteins - metabolism | RNA, Messenger - metabolism | Flagellin - pharmacology | Tissue Distribution | Cell Nucleus - metabolism | Protein Isoforms - metabolism | Biological Transport | Oligonucleotides - pharmacology | Toll-Like Receptor 3 - genetics | Toll-Like Receptors - metabolism | Chemokine CXCL9 | Toll-Like Receptor 5 - metabolism | Poly I-C - pharmacology | Cytokines - metabolism | Cells, Cultured | Toll-Like Receptor 4 - genetics | Toll-Like Receptor 3 - metabolism | Toll-Like Receptor 4 - metabolism | Chemokine CXCL10 | Transcription Factor RelA - metabolism | Keratinocytes - metabolism | Toll-Like Receptors - genetics | Chemokines, CXC - metabolism | Lipopolysaccharides - pharmacology | CpG Islands | Ligands | Chemokines - metabolism | Toll-Like Receptor 9 - metabolism | CD40 antigen | Oligonucleotides | Flagellin | mRNA | intercellular adhesion molecule 1 | Immunity | Lipopolysaccharides | CXC chemokines | CCL20 protein | Toll-like receptors | CpG islands | TLR7 protein | Dermatology | Keratinocytes | Nuclear transport | Stress | TLR3 protein | TLR9 protein | TLR1 protein | External stimuli | CXCL10 protein | Histocompatibility antigen HLA | Interferon | Internet | Monocyte chemoattractant protein 1 | Tumor necrosis factor- alpha
Journal Article
International Journal of Cancer, ISSN 0020-7136, 10/2018, Volume 143, Issue 8, pp. 2029 - 2038
Lorlatinib (PF‐06463922) is a promising oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor currently in Phase III clinical trials for treatment of... 
brain accumulation | P‐glycoprotein | cytochrome P450‐3A | oral availability | lorlatinib | P-glycoprotein | cytochrome P450-3A | RESISTANCE PROTEIN | ALK INHIBITORS | TRANSPORTERS | METASTASES | CLINICAL-EXPERIENCE | PF-06463922 | CELL LUNG-CANCER | LIQUID-CHROMATOGRAPHY | ONCOLOGY | CERITINIB | CRIZOTINIB | Cell Line | Lung Neoplasms - drug therapy | Administration, Oral | Lactams, Macrocyclic - metabolism | Humans | Lung Neoplasms - metabolism | Carcinoma, Non-Small-Cell Lung - metabolism | Cytochrome P-450 Enzyme System - metabolism | Biological Availability | Male | Lactams, Macrocyclic - pharmacology | Mice, Knockout | Brain - metabolism | ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism | Pilot Projects | Animals | Dogs | Madin Darby Canine Kidney Cells | Female | Mice | Carcinoma, Non-Small-Cell Lung - drug therapy | Anaplastic Lymphoma Kinase - antagonists & inhibitors | Protein-Tyrosine Kinases - antagonists & inhibitors | Plasma physics | Genetically modified organisms | Cytochrome P-450 | Lymphomas | Genetic engineering | Permeability | Lung cancer, Non-small cell | Cytochrome | Brain | Liver | Lung cancer | Membrane permeability | Clinical trials | Transgenic | Blood | Accumulation | Metastases | MDR1 protein | Intestine | Protein-tyrosine kinase | Genetic modification | Cytochromes P450 | Medical research | Efflux | Cytochrome P450 | Glycoprotein | Non-small cell lung carcinoma | Data processing | Pharmacology | Exposure | Lymphoma | Inhibitors | Plasma levels | Pharmacokinetics | Cancer
Journal Article
PLoS ONE, ISSN 1932-6203, 2013, Volume 8, Issue 2, p. e57802
Chemerin is a specific chemoattractant for macrophages and dendritic cells (DC). In addition, it can rapidly stimulate macrophage adhesion to extracellular... 
METABOLIC SYNDROME | JOINT DAMAGE | MULTIDISCIPLINARY SCIENCES | ATHEROSCLEROSIS | MARKERS | CHEMR23 | RECEPTOR | Tumor Necrosis Factor-alpha - metabolism | Atherosclerosis - pathology | Chemokines - blood | Antibodies, Monoclonal, Humanized - therapeutic use | Smoking - blood | Arthritis, Rheumatoid - blood | Humans | Intercellular Signaling Peptides and Proteins | Middle Aged | Risk Factors | Male | Inflammation - blood | Atherosclerosis - blood | Arthritis, Rheumatoid - drug therapy | Inflammation - drug therapy | Interleukin-6 - blood | Antibodies, Monoclonal, Humanized - pharmacology | Female | Macrophage Migration-Inhibitory Factors - blood | Adalimumab | Tumor Necrosis Factor-alpha - antagonists & inhibitors | Rheumatoid factor | Care and treatment | Tumor necrosis factor | Atherosclerosis | Antigen presenting cells | Arthritis | Inflammation | Research | Risk factors | Endothelium | Therapy | Leukocyte migration | Pathogenesis | Lipids | Family medical history | Metabolic syndrome | Macrophages | Synovium | Interleukin 6 | Proteins | Reduction | Immunology | Tumor necrosis factor-TNF | Extracellular matrix | Enzyme-linked immunosorbent assay | Psoriasis | Dendritic cells | Rheumatology | Health risks | Risk analysis | Joint diseases | Patients | Synoviocytes | Adhesion | Morbidity | Endothelial cells | Macrophage migration inhibitory factor | Serum levels | Weight control | Rheumatoid arthritis | Arteriosclerosis | Migration inhibitory factor | Monoclonal antibodies | Gastrointestinal surgery | Cardiovascular diseases | Chemokines | Smoking
Journal Article
Journal of Leukocyte Biology, ISSN 0741-5400, 03/2017, Volume 101, Issue 3, pp. 775 - 783
Synovial IL‐21 + TNF + CD4 + T cells induce matrix metalloproteinase production by fibroblast‐like synoviocytes in RA patients. Bone and cartilage destruction... 
peripheral blood | autoimmune | inflammation | synovial fluid | Synovial fluid | Autoimmune | Inflammation | Peripheral blood | CRITERIA | ACTIVATION | RECEPTOR | CLASSIFICATION | INTERLEUKIN-21 | IMMUNOLOGY | IL-21 | CELL BIOLOGY | IL-17 | DIFFERENTIATION | HEMATOLOGY | EXPRESSION | TH17 | Tumor Necrosis Factor-alpha - metabolism | Cell Proliferation | RANK Ligand - metabolism | Humans | Synovial Fluid - metabolism | Interferon-gamma - metabolism | Interleukins - metabolism | Peptides, Cyclic - metabolism | CD4-Positive T-Lymphocytes - immunology | Immunoglobulin M - metabolism | Synoviocytes - metabolism | Psoriasis - pathology | T-Lymphocytes, Helper-Inducer - immunology | Proto-Oncogene Proteins c-bcl-6 - metabolism | Interleukin-6 - metabolism | Psoriasis - immunology | Rheumatoid Factor - metabolism | Joints - pathology | Matrix Metalloproteinase 3 - metabolism | Fibroblasts - pathology | T-Box Domain Proteins - metabolism | Arthritis, Rheumatoid - pathology | Interleukin-17 - metabolism | Biopsy | Arthritis, Rheumatoid - immunology | Matrix Metalloproteinase 1 - metabolism | Immunoglobulin M | Destruction | Antibodies | Lymphocytes T | Arthritis | Matrix metalloproteinase | Cartilage | Lymphocytes | Interleukin 21 | Fibroblasts | Metalloproteinase | Interstitial collagenase | Stromelysin 1 | Secretion | Citrulline | Patients | Synoviocytes | CD4 antigen | Rheumatoid factor | Tumor necrosis factor | Rheumatoid arthritis | Health risk assessment | Neutralization
Journal Article
PLoS ONE, ISSN 1932-6203, 2011, Volume 6, Issue 7, p. e21772
The aim of this study was to provide more insight into the question as to why blockade of CCR1, CCR2, and CCR5 may have failed in clinical trials in rheumatoid... 
CHEMOKINE RECEPTOR EXPRESSION | CONTROLLED CLINICAL-TRIAL | COLLAGEN-INDUCED ARTHRITIS | ANTAGONIST | SYNOVIAL TISSUE | MACROPHAGES | BIOLOGY | DOUBLE-BLIND | INFLAMMATORY DISEASE | PERIPHERAL-BLOOD | PROOF-OF-CONCEPT | Monocytes - cytology | Receptors, CCR2 - immunology | Humans | Middle Aged | Synovial Fluid - metabolism | Male | Monocytes - immunology | Case-Control Studies | Receptors, CCR5 - immunology | Dose-Response Relationship, Drug | Arthritis, Rheumatoid - metabolism | Antibodies, Neutralizing - immunology | Piperidines - pharmacology | Arthritis, Rheumatoid - drug therapy | Antibodies, Neutralizing - therapeutic use | Monocytes - pathology | Aged, 80 and over | Adult | Female | Chemokine CCL2 - metabolism | Chemokine CCL5 - metabolism | Receptors, CCR1 - immunology | Phenylurea Compounds - therapeutic use | Antibodies, Neutralizing - pharmacology | Chemotaxis - drug effects | Monocytes - drug effects | Receptors, CCR - immunology | Piperidines - therapeutic use | Receptors, CCR - antagonists & inhibitors | Aged | Phenylurea Compounds - pharmacology | Arthritis, Rheumatoid - immunology | Receptors, CCR1 - antagonists & inhibitors | Rheumatoid factor | High-definition television | Arthritis | Analysis | CC chemokine receptors | Leukocyte migration | RANTES | Migration | Blocking antibodies | Clinical trials | Antibodies | Inflammatory diseases | Recruitment | CCR1 protein | Receptors | Immunology | CCR2 protein | Peripheral blood | Drug dosages | Medical research | CCR5 protein | Immunoglobulins | Cytokines | Computational fluid dynamics | Fluid | Rheumatology | Inflammation | Chemotaxis | Patients | Human subjects | Monocytes | Rheumatoid arthritis | Ligands | Autoimmune diseases | Chemokines | Monocyte chemoattractant protein 1 | Cell migration | Pharmaceuticals
Journal Article
European Journal of Pharmaceutics and Biopharmaceutics, ISSN 0939-6411, 03/2019, Volume 136, pp. 120 - 130
Lorlatinib, a novel generation oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor with high membrane and blood-brain barrier permeability, recently... 
P-glycoprotein | Oral bioavailability | Oatp1a/1b | Lorlatinib | Cytochrome P450-3A | Ritonavir | ALK INHIBITORS | TRANSPORTERS | PF-06463922 | CELL LUNG-CANCER | PHARMACOKINETICS | METABOLISM | MODELS | RESISTANCE | CRIZOTINIB | PHARMACOLOGY & PHARMACY | ROS1 | Lactams, Macrocyclic - metabolism | Biological Availability | Brain - metabolism | Acridines - administration & dosage | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Anaplastic Lymphoma Kinase - metabolism | Lactams, Macrocyclic - administration & dosage | Proto-Oncogene Proteins - metabolism | Proto-Oncogene Proteins - antagonists & inhibitors | Cytochrome P-450 CYP3A Inhibitors - administration & dosage | Ritonavir - administration & dosage | Acridines - metabolism | Administration, Oral | Tetrahydroisoquinolines - administration & dosage | Receptor Protein-Tyrosine Kinases - metabolism | Mice, Knockout | Brain - drug effects | Drug Synergism | Administration, Intravenous | Animals | Cytochrome P-450 CYP3A Inhibitors - metabolism | Ritonavir - metabolism | Tetrahydroisoquinolines - metabolism | Drug Interactions - physiology | Mice | Anaplastic Lymphoma Kinase - antagonists & inhibitors | Antiviral agents | Analysis | Genetically modified organisms | Cytochrome P-450 | Lymphomas | Liquid chromatography | Permeability | Lung cancer, Non-small cell | Mass spectrometry | Index Medicus
Journal Article
Journal Article
Pharmacological Research, ISSN 1043-6618, 11/2018, Volume 137, pp. 47 - 55
Brigatinib is an FDA-approved oral anaplastic lymphoma kinase (ALK) inhibitor for treatment of metastatic non-small cell lung cancer (NSCLC). Using genetically... 
Brigatinib | P-glycoprotein | Oral availability | Cytochrome P450-3A | Brain accumulation | Brigatinib (CID: 68165256) | Elacridar HCl (CID: 170320) | Ko143 (CID: 10322450) | Zosuquidar trihydrochloride (CID: 153997) | ALK INHIBITORS | TRANSPORTERS | METASTASES | MECHANISMS | P-GP/ABCB1 | CELL LUNG-CANCER | AP26113 | POTENT | CERITINIB | CRIZOTINIB | PHARMACOLOGY & PHARMACY | Testis - metabolism | ATP Binding Cassette Transporter, Subfamily G, Member 2 - metabolism | Pyrimidines - blood | Humans | Biological Availability | Male | Neoplasm Proteins - metabolism | Brain - metabolism | Madin Darby Canine Kidney Cells | Organophosphorus Compounds - pharmacology | ATP Binding Cassette Transporter, Subfamily B - genetics | Neoplasm Proteins - genetics | Tetrahydroisoquinolines - pharmacology | Administration, Oral | ATP Binding Cassette Transporter, Subfamily G, Member 2 - genetics | Mice, Transgenic | Pyrimidines - pharmacology | ATP Binding Cassette Transporter, Subfamily B - metabolism | Protein Kinase Inhibitors - blood | Animals | Cytochrome P-450 CYP3A - metabolism | Acridines - pharmacology | Dogs | Organophosphorus Compounds - blood | Protein Kinase Inhibitors - pharmacology | Brain | Plasma physics | Liver | Cytochrome P-450 | Breast cancer | Liquid chromatography | Lung cancer, Non-small cell | Drug approval | Analysis | Genetically modified organisms | Lymphomas | Genetic engineering | Mice | Drug therapy, Combination | Mass spectrometry
Journal Article
International Journal of Pharmaceutics, ISSN 0378-5173, 02/2019, Volume 556, pp. 172 - 180
Journal Article
Molecular pharmaceutics, ISSN 1543-8384, 09/2019, Volume 16, Issue 9, pp. 3842 - 3852
Ribociclib is a CDK4/6 inhibitor recently approved for the treatment of some types of breast cancer in combination with an aromatase inhibitor. It is currently... 
BCRP | DRUG | MEDICINE, RESEARCH & EXPERIMENTAL | P-gp | PERMEABILITY | brain penetration | METASTASES | PENETRATION | CYP3A4 | BLOOD-TUMOR BARRIER | CDK4/6 inhibitor | PHARMACOLOGY & PHARMACY | KNOCKOUT | ABC TRANSPORTERS | INHIBITOR | PHASE-I | ribociclib | CANCER RESISTANCE PROTEIN | Index Medicus
Journal Article
Arthritis research & therapy, ISSN 1478-6354, 2013, Volume 15, Issue 6, pp. R209 - R209
The FMS-related tyrosine ki