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1. Full Text Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors
by Romero, F. Anthony and Taylor, Alexander M and Crawford, Terry D and Tsui, Vickie and Côté, Alexandre and Magnuson, Steven
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2016, Volume 59, Issue 4, pp. 1271 - 1298
Bromodomains, small protein modules that recognize acetylated lysine on histones, play a significant role in the epigenome, where they function as "readers"... 
CHEMISTRY, MEDICINAL | SWI/SNF COMPLEXES | SMALL-MOLECULE INHIBITORS | PROSTATE-CANCER | SELECTIVE INHIBITORS | GENE-EXPRESSION | CHEMICAL PROBE | TUMOR-SUPPRESSOR | BET INHIBITORS | HISTONE ACETYLTRANSFERASE | PHD FINGER | Small Molecule Libraries - pharmacology | Antigens, Nuclear - metabolism | Humans | Drug Discovery - methods | CREB-Binding Protein - antagonists & inhibitors | Chromosomal Proteins, Non-Histone - antagonists & inhibitors | DNA-Binding Proteins - metabolism | CREB-Binding Protein - metabolism | Protein Processing, Post-Translational - drug effects | Adaptor Proteins, Signal Transducing - antagonists & inhibitors | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Lysine - metabolism | Protein-Serine-Threonine Kinases - metabolism | RNA-Binding Proteins - antagonists & inhibitors | Nerve Tissue Proteins - antagonists & inhibitors | ATPases Associated with Diverse Cellular Activities | DNA-Binding Proteins - antagonists & inhibitors | Chromosomal Proteins, Non-Histone - metabolism | Carrier Proteins - antagonists & inhibitors | Adenosine Triphosphatases - metabolism | Models, Molecular | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Nerve Tissue Proteins - metabolism | Transcription Factors - metabolism | Adenosine Triphosphatases - antagonists & inhibitors | DNA Helicases - metabolism | Small Molecule Libraries - chemistry | Acetylation - drug effects | Animals | Carrier Proteins - metabolism | Nuclear Proteins - antagonists & inhibitors | DNA Helicases - antagonists & inhibitors | Histones - metabolism | Adaptor Proteins, Signal Transducing - metabolism | RNA-Binding Proteins - metabolism | Index Medicus
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2. Full Text Signal Transducer and Activator of Transcription 3 Is the Dominant Mediator of the Anti-Inflammatory Effects of IL-10 in Human Macrophages
by Williams, Lynn and Bradley, Laura and Smith, Alexandra and Foxwell, Brian
The Journal of Immunology, ISSN 0022-1767, 01/2004, Volume 172, Issue 1, pp. 567 - 576
The signaling mechanism by which the anti-inflammatory cytokine IL-10 mediates suppression of proinflammatory cytokine synthesis remains largely unknown.... 
RHEUMATOID-ARTHRITIS | TUMOR-NECROSIS-FACTOR | DNA-BINDING | HUMAN NEUTROPHILS | TYROSINE PHOSPHORYLATION | INTERLEUKIN-10 RECEPTOR | GENE-EXPRESSION | KAPPA-B-ALPHA | IMMUNOLOGY | HUMAN MONOCYTES | MONONUCLEAR PHAGOCYTES | Protein Binding - genetics | Protein Biosynthesis | Interleukin-6 - antagonists & inhibitors | Humans | Tumor Necrosis Factor-alpha - genetics | Immunoglobulins - genetics | Lipopolysaccharides - antagonists & inhibitors | RNA, Messenger - metabolism | Suppressor of Cytokine Signaling Proteins | Repressor Proteins - antagonists & inhibitors | Antigens, CD - metabolism | Trans-Activators - physiology | Protein Tyrosine Phosphatases - antagonists & inhibitors | RNA, Messenger - biosynthesis | Protein Tyrosine Phosphatases - genetics | Inflammation Mediators - physiology | Glycoproteins - genetics | DNA-Binding Proteins - physiology | Protein Tyrosine Phosphatases - biosynthesis | DNA-Binding Proteins - antagonists & inhibitors | Signal Transduction - genetics | DNA - metabolism | Down-Regulation - genetics | Macrophages - metabolism | Protein Tyrosine Phosphatase, Non-Receptor Type 2 | Repressor Proteins - biosynthesis | Up-Regulation - immunology | Interleukin-10 - antagonists & inhibitors | Lipopolysaccharides - pharmacology | Adenoviruses, Human - genetics | Interleukin-10 - immunology | Tumor Necrosis Factor-alpha - biosynthesis | Phosphorylation | Tissue Inhibitor of Metalloproteinase-1 - biosynthesis | Antigens, CD - biosynthesis | Receptors, Cell Surface | Receptors, IgG - biosynthesis | Receptors, IgG - antagonists & inhibitors | Interleukin-10 - physiology | Signal Transduction - immunology | Tissue Inhibitor of Metalloproteinase-1 - metabolism | Signaling Lymphocytic Activation Molecule Family Member 1 | Receptors, Tumor Necrosis Factor - antagonists & inhibitors | RNA, Messenger - antagonists & inhibitors | Receptors, Tumor Necrosis Factor, Type II | Trans-Activators - genetics | Inflammation Mediators - antagonists & inhibitors | Trans-Activators - biosynthesis | Immunoglobulins - biosynthesis | Macrophages - immunology | Inflammation Mediators - immunology | Receptors, Tumor Necrosis Factor - metabolism | Immune Sera - pharmacology | Proteins - physiology | Cells, Cultured | Glycoproteins - antagonists & inhibitors | Histocompatibility Antigens Class II - biosynthesis | Tissue Inhibitor of Metalloproteinase-1 - antagonists & inhibitors | Transcription Factors - antagonists & inhibitors | Transcription Factors - biosynthesis | Up-Regulation - genetics | DNA-Binding Proteins - genetics | DNA - antagonists & inhibitors | Glycoproteins - biosynthesis | Suppressor of Cytokine Signaling 3 Protein | Down-Regulation - immunology | Interleukin-6 - biosynthesis | Receptors, Tumor Necrosis Factor - biosynthesis | STAT3 Transcription Factor | Trans-Activators - antagonists & inhibitors | Genetic Vectors | DNA-Binding Proteins - biosynthesis | Tumor Necrosis Factor-alpha - antagonists & inhibitors | SOCS-3 protein | Index Medicus | Abridged Index Medicus
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3. Drug concentration monitoring ; Microbial alpha-glucosidase inhibitors ; Plasminogen activators
by Bottorff, M. B
1988, ISBN 3540190023, 148
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4. Full Text Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells
by Remsing Rix, L.L and Rix, U and Colinge, J and Hantschel, O and Bennett, K.L and Stranzl, T and Müller, A and Baumgartner, C and Valent, P and Augustin, M and Till, J.H and Superti-Furga, G
Leukemia, ISSN 0887-6924, 03/2009, Volume 23, Issue 3, pp. 477 - 485
The detailed molecular mechanism of action of second-generation BCR-ABL tyrosine kinase inhibitors, including perturbed targets and pathways, should contribute... 
BCR-ABL INHIBITORS | SRC | TYROSINE KINASE | MECHANISMS | NILOTINIB | BREAST-CANCER CELLS | dasatinib | ONCOLOGY | IMATINIB | kinase profiling | RESISTANCE | chronic myeloid leukemia | chemical proteomics | SKI-606 | HEMATOLOGY | bosutinib | Nitriles - pharmacology | Proto-Oncogene Proteins c-abl - antagonists & inhibitors | Humans | Substrate Specificity | Neoplasm Proteins - antagonists & inhibitors | Gene Expression Profiling | K562 Cells - drug effects | Quinolines - pharmacology | Drug Delivery Systems | Leukemia, Myeloid, Accelerated Phase - pathology | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Dasatinib | Nerve Tissue Proteins - antagonists & inhibitors | Aniline Compounds - pharmacology | Leukocytes, Mononuclear - drug effects | Quinolines - chemistry | src-Family Kinases - antagonists & inhibitors | Pyrimidines - pharmacology | Calcium-Calmodulin-Dependent Protein Kinase Type 2 - antagonists & inhibitors | K562 Cells - enzymology | Leukemia, Myeloid, Accelerated Phase - enzymology | Mitogen-Activated Protein Kinases - antagonists & inhibitors | Signal Transduction - drug effects | Fusion Proteins, bcr-abl - antagonists & inhibitors | Nitriles - chemistry | Leukocytes, Mononuclear - enzymology | Protein Kinase Inhibitors - pharmacology | Thiazoles - pharmacology | Aniline Compounds - chemistry | Drug Screening Assays, Antitumor | Protein-Tyrosine Kinases - antagonists & inhibitors | Enzyme inhibitors | Physiological aspects | Chronic myeloid leukemia | Research | Drug therapy | Health aspects | Protein kinases | Index Medicus
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5. Full Text Converting a broad matrix metalloproteinase family inhibitor into a specific inhibitor of MMP‐9 and MMP‐14
by Shirian, Jason and Arkadash, Valeria and Cohen, Itay and Sapir, Tamila and Radisky, Evette S and Papo, Niv and Shifman, Julia M
FEBS Letters, ISSN 0014-5793, 04/2018, Volume 592, Issue 7, pp. 1122 - 1134
MMP ‐14 and MMP ‐9 are two well‐established cancer targets for which no specific clinically relevant inhibitor is available. Using a powerful combination of... 
protein–protein interactions | binding specificity | protein engineering | matrix metalloproteinase inhibitors | BINDING-SPECIFICITY | TIMP-2 | ACTIVATION | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | ESCHERICHIA-COLI | PROTEIN INTERFACES | CANCER-THERAPY | protein-protein interactions | CELL BIOLOGY | BIOPHYSICS | COMPUTATIONAL DESIGN | HUMAN TISSUE INHIBITOR | YEAST SURFACE DISPLAY | Tissue Inhibitor of Metalloproteinase-2 - chemistry | Humans | Matrix Metalloproteinase 14 - chemistry | Protein Binding | Matrix Metalloproteinase Inhibitors - chemistry | Matrix Metalloproteinase 9 - chemistry | Matrix Metalloproteinase 14 - chemical synthesis | Index Medicus
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6. Full Text Population Pharmacokinetics and Pharmacodynamics of Rivaroxaban an Oral, Direct Factor Xa Inhibitor in Patients Undergoing Major Orthopaedic Surgery
by Mueck, Wolfgang and Eriksson, Bengt I and Bauer, Kenneth A and Borris, Lars and Dahl, Ola E and Fisher, William D and Gent, Michael and Haas, Sylvia and Huisman, Menno V and Kakkar, Ajay K and Kalebo, Peter and Kwong, Louis M and Misselwitz, Frank and Turpie, Alexander G.G
Clinical Pharmacokinetics, ISSN 0312-5963, 2008, Volume 47, Issue 3, pp. 203 - 216
Background: There is a clinical need for novel oral anticoagulants with predictable pharmacokinetics and pharmacodynamics. Rivaroxaban is an oral direct Factor... 
Anticoagulants | Rivaroxaban | Pharmacokinetic pharmacodynamic relationships | Pharmacodynamic modelling | Factor IXA inhibitors | Pharmacokinetic modelling | Research and development | Orthopaedic surgery | Pharmacotherapy | Internal Medicine | Medicine & Public Health | Pharmacology/Toxicology | BAY-59-7939 | VIVO COAGULATION TIME | VENOUS THROMBOEMBOLISM | DABIGATRAN ETEXILATE | HEALTHY-SUBJECTS | SAFETY | TOLERABILITY | PREVENTION | TOTAL HIP-REPLACEMENT | MODEL ANALYSIS | PHARMACOLOGY & PHARMACY | Age Factors | Factor Xa Inhibitors | Humans | Middle Aged | Prothrombin Time | Male | Thiophenes - administration & dosage | Dose-Response Relationship, Drug | Tissue Distribution | Venous Thromboembolism - prevention & control | Time Factors | Aged, 80 and over | Adult | Arthroplasty, Replacement, Knee | Female | Double-Blind Method | Morpholines - administration & dosage | Morpholines - pharmacology | Thiophenes - pharmacology | Arthroplasty, Replacement, Hip | Thiophenes - pharmacokinetics | Models, Biological | Sex Factors | Aged | Morpholines - pharmacokinetics | Nonlinear Dynamics | Index Medicus
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7. Full Text Immune‐related alopecia (areata and universalis) in cancer patients receiving immune checkpoint inhibitors
by Zarbo, A and Belum, V.R and Sibaud, V and Oudard, S and Postow, M.A and Hsieh, J.J and Motzer, R.J and Busam, K.J and Lacouture, M.E
British Journal of Dermatology, ISSN 0007-0963, 06/2017, Volume 176, Issue 6, pp. 1649 - 1652
Cytotoxic T‐lymphocyte‐associated protein‐4, programmed cell death protein and programmed cell death protein ligand 1 monoclonal antibodies (immune checkpoint... 
ANTIBODIES | PD-L1 | THERAPY | TOXICITIES | ANTI-PD-1 | DERMATOLOGY | Antibodies, Monoclonal, Humanized - adverse effects | Skin Neoplasms - drug therapy | Humans | Middle Aged | Male | Immunotherapy - adverse effects | Neoplasm Metastasis | B7-H1 Antigen - antagonists & inhibitors | Melanoma - drug therapy | Adult | Female | Aged | CTLA-4 Antigen - antagonists & inhibitors | Carcinoma, Renal Cell - drug therapy | Drug Therapy, Combination | Kidney Neoplasms - drug therapy | Alopecia Areata - chemically induced | Cancer patients | Care and treatment | Management science | Alopecia | Baldness | Psoriasis | Cell death | Analysis | Immunotherapy | Monoclonal antibodies | Exanthema | Cytotoxicity | Lymphocytes T | Pruritus | Proteins | Literature reviews | Hepatitis | Vitiligo | Eruptions | Rosacea | Hair | Immune response | Quality of life | Pneumonitis | Immune checkpoint | PD-L1 protein | Colitis | Hair loss | Cancer | Apoptosis | CTLA-4 | alopecia areata | PD-1 | VEGF
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8. Full Text Heterogeneous effects of tissue inhibitors of matrix metalloproteinases on cardiac fibroblasts
by Joshua D. Lovelock and Andrew H. Baker and Feng Gao and Jing-Fei Dong and Angela L. Bergeron and Willie McPheat and Natarajan Sivasubramanian and Douglas L. Mann
American Journal of Physiology - Heart and Circulatory Physiology, ISSN 0363-6135, 02/2005, Volume 288, Issue 2, pp. 461 - 468
The balance between matrix metalloproteinases (MMPs) and their natural inhibitors, the tissue inhibitors of metalloproteinases (TIMPs), plays a critical role... 
Matrix metalloproteinase | Proliferation | Apoptosis | Phenotypic differentiation | DEATH DOMAIN | CELLS | phenotypic differentiation | CARDIAC & CARDIOVASCULAR SYSTEMS | PHYSIOLOGY | proliferation | RAT | apoptosis | FAILING HUMAN HEART | GROWTH-FACTOR-BETA | matrix metalloproteinase | RECOMBINANT ADENOVIRUSES | MYOFIBROBLASTS | PERIPHERAL VASCULAR DISEASE | MOLECULAR-CLONING | EXPRESSION | Humans | Actins - metabolism | Culture Media, Conditioned - pharmacology | Tissue Inhibitor of Metalloproteinase-3 - antagonists & inhibitors | Tissue Inhibitor of Metalloproteinase-2 - genetics | Tissue Inhibitor of Metalloproteinases - genetics | Tissue Inhibitor of Metalloproteinase-1 - metabolism | Tissue Inhibitor of Metalloproteinase-2 - metabolism | Myocardium - metabolism | Tissue Inhibitor of Metalloproteinase-3 - metabolism | Adenoviridae - genetics | Fibroblasts - metabolism | Tissue Inhibitor of Metalloproteinase-3 - genetics | Recombinant Proteins - metabolism | Recombinant Proteins - antagonists & inhibitors | Mice, Inbred C57BL | Tissue Inhibitor of Metalloproteinases - antagonists & inhibitors | Cells, Cultured | Tissue Inhibitor of Metalloproteinase-1 - antagonists & inhibitors | Tissue Inhibitor of Metalloproteinases - metabolism | Myocardium - cytology | Cell Division - physiology | Tissue Inhibitor of Metalloproteinase-1 - genetics | Animals | Fibroblasts - cytology | Mice | Apoptosis - physiology | Tissue Inhibitor of Metalloproteinase-2 - antagonists & inhibitors | Index Medicus
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9. Full Text A Small-Molecule Inhibitor of Tgf-β Signaling Replaces Sox2 in Reprogramming by Inducing Nanog
by Ichida, Justin K and Blanchard, Joel and Lam, Kelvin and Son, Esther Y and Chung, Julia E and Egli, Dieter and Loh, Kyle M and Carter, Ava C and Di Giorgio, Francesco P and Koszka, Kathryn and Huangfu, Danwei and Akutsu, Hidenori and Liu, David R and Rubin, Lee L and Eggan, Kevin
Cell Stem Cell, ISSN 1934-5909, 11/2009, Volume 5, Issue 5, pp. 491 - 503
The combined activity of three transcription factors can reprogram adult cells into induced pluripotent stem cells (iPSCs). However, the transgenic methods... 
STEMCELL | PLURIPOTENT STEM-CELLS | OCT4 | POTENT | MOUSE | HUMAN FIBROBLASTS | GENERATION | INDUCTION | DIFFERENTIATION | CELL & TISSUE ENGINEERING | CELL BIOLOGY | Induced Pluripotent Stem Cells - pathology | Transforming Growth Factor beta - immunology | Cell Line | Small Molecule Libraries - pharmacology | Nanog Homeobox Protein | Transduction, Genetic | Signal Transduction | Homeodomain Proteins - metabolism | Antibodies, Monoclonal | Homeodomain Proteins - genetics | SOXB1 Transcription Factors - metabolism | Animals | High-Throughput Screening Assays | Receptors, Transforming Growth Factor beta - antagonists & inhibitors | SOXB1 Transcription Factors - genetics | Dioxoles - pharmacology | Transforming Growth Factor beta - antagonists & inhibitors | Cell Transdifferentiation | Benzamides - pharmacology | Induced Pluripotent Stem Cells - immunology | Mice | Pyridines - pharmacology | Induced Pluripotent Stem Cells - metabolism | Pyrazoles - pharmacology | Index Medicus
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10. Full Text Identification and pharmaceutical evaluation of novel frog skin-derived serine proteinase inhibitor peptide–PE-BBI (Pelophylax esculentus Bowman-Birk inhibitor) for the potential treatment of cancer
by Lyu, Peng and Ge, Lilin and Ma, Rui and Wei, Ran and McCrudden, Cian M and Chen, Tianbao and Shaw, Chris and Kwok, Hang Fai
Scientific Reports, ISSN 2045-2322, 12/2018, Volume 8, Issue 1, pp. 14502 - 10
Amphibian venom-derived peptides have high potential in the field of anticancer drug discovery. We have isolated a novel Bowman-Birk proteinase inhibitor... 
PROTEASE-ACTIVATED RECEPTORS | ODOROUS FROG | MESSENGER-RNA EXPRESSION | COLORECTAL-CANCER | MULTIDISCIPLINARY SCIENCES | AMPHIBIAN SKIN | HUMAN TISSUE KALLIKREINS | ANTIMICROBIAL PEPTIDES | HUMAN POLYMORPHONUCLEAR LEUKOCYTES | TRYPSIN-INHIBITOR | CLINICAL-SIGNIFICANCE | Peptidase | Epithelial cells | Secretion | Therapeutic applications | Serine | Colorectal carcinoma | Proteinase | Serine proteinase inhibitors | Amino acid sequence | Kallikrein | Cytotoxicity | Smooth muscle | mRNA | Proteinase inhibitors | Secretions | Polymerase chain reaction | Trypsin | Venom | Serine proteinase | Skin | Cancer
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11. Full Text Serotonin Transporter Occupancy of Five Selective Serotonin Reuptake Inhibitors at Different Doses: An [11C]DASB Positron Emission Tomography Study
by Meyer, Jeffrey H and Wilson, Alan A and Sagrati, Sandra and Hussey, Doug and Carella, Anna and Potter, William Z and Ginovart, Nathalie and Spencer, Edgar P and Cheok, Andy and Houle, Sylvain
American Journal of Psychiatry, ISSN 0002-953X, 05/2004, Volume 161, Issue 5, pp. 826 - 835
OBJECTIVE: Minimum therapeutic doses of paroxetine and citalopram produce 80% occupancy for the serotonin (5-HT) transporter (5-HTT). The authors used... 
H-3 PAROXETINE BINDING | ANTIDEPRESSANTS | DASB | 5-HT2 RECEPTORS | PSYCHIATRY | IN-VIVO | HIGH-AFFINITY | HUMAN-BRAIN | MAJOR DEPRESSION | UPTAKE SITES | PET | Paroxetine - pharmacokinetics | Serotonin Uptake Inhibitors - pharmacokinetics | Cyclohexanols - pharmacokinetics | Fluoxetine - pharmacokinetics | Membrane Glycoproteins - metabolism | Humans | Middle Aged | Male | Paroxetine - therapeutic use | Serotonin Plasma Membrane Transport Proteins | Carrier Proteins - drug effects | Corpus Striatum - metabolism | Dose-Response Relationship, Drug | Sertraline - pharmacokinetics | Sertraline - therapeutic use | Adult | Female | Fluoxetine - therapeutic use | Serotonin Uptake Inhibitors - therapeutic use | Nerve Tissue Proteins | Venlafaxine Hydrochloride | Carrier Proteins - metabolism | Membrane Transport Proteins | Serotonin - metabolism | Benzylamines | Corpus Striatum - drug effects | Cyclohexanols - therapeutic use | Membrane Glycoproteins - drug effects | Citalopram - pharmacokinetics | Citalopram - therapeutic use | Tomography, Emission-Computed | Corpus Striatum - diagnostic imaging | Delayed-Action Preparations | Carbon Radioisotopes | Dosage and administration | Serotonin agents | Drug therapy | Mental illness | Tomography | Mental disorders | Antidepressants | Psychiatry | Clinical outcomes | Index Medicus | Abridged Index Medicus
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12. Full Text Tissue kallikrein inhibitors based on the sunflower trypsin inhibitor scaffold - A potential therapeutic intervention for skin diseases
by Chen, Wenjie and Kinsler, Veronica A and Macmillan, Derek and Di, Wei-Li
PLoS ONE, ISSN 1932-6203, 11/2016, Volume 11, Issue 11, pp. e0166268 - e0166268
Tissue kallikreins (KLKs), in particular KLK5, 7 and 14 are the major serine proteases in the skin responsible for skin shedding and activation of inflammatory... 
PROTEINASE-ACTIVATED RECEPTOR-2 | AMINO-ACID-SEQUENCE | MECHANISM | MULTIDISCIPLINARY SCIENCES | ALPHA-CHYMOTRYPSIN | STRATUM-CORNEUM | ACYL TRANSFER | SERINE-PROTEASE | GENE-THERAPY | NETHERTON-SYNDROME | SFTI-1 | Cell Line | Netherton Syndrome - metabolism | Skin Diseases - metabolism | Skin - metabolism | Helianthus - metabolism | Humans | Receptor, PAR-2 - metabolism | Trypsin Inhibitors - pharmacology | Skin Diseases - drug therapy | Peptides, Cyclic - metabolism | Proteinase Inhibitory Proteins, Secretory - pharmacology | Peptides, Cyclic - antagonists & inhibitors | Tissue Kallikreins - antagonists & inhibitors | Interleukin-8 - metabolism | Skin - drug effects | Netherton Syndrome - drug therapy | Trypsin | Protease inhibitors | Interleukins | Kallikrein | Amino acids | Skin diseases | Skin | Health aspects | Cell culture | Shedding | Soybeans | Peptides | Calcium | Pathogenesis | Interleukin | Childrens health | Proteins | Cell activation | Tissue kallikrein | Protease | Inhibition | Resins | Interleukin 8 | Netherton syndrome | Enzymes | Calcium (intracellular) | Analogue | Secretion | Titration calorimetry | Inflammation | Signaling | Inhibitors | Calorimetry | Titration | Mutation | Gene therapy | Index Medicus
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