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61. Full Text Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors
by Mougenot, Patrick and Namane, Claudie and Fett, Eykmar and Goumy, Florence and Dadji-FaĆÆhun, Rommel and Langot, Gwladys and Monseau, Catherine and Onofri, BĆ©nĆ©dicte and Pacquet, FranƧois and Pascal, CĆ©cile and Crespin, Olivier and Ben-Hassine, Majdi and Ragot, Jean-Luc and Van-Pham, Thao and Philippo, Christophe and Chatelain-Egger, Florence and PĆ©ron, Philippe and Le Bail, Jean-Christophe and Guillot, Etienne and Chamiot-Clerc, Philippe and Chabanaud, Marie-Aude and Pruniaux, Marie-Pierre and MĆ©negotto, JĆ©rĆ“me and Schmidt, Friedemann and Venier, Olivier and Viviani, Fabrice and Nicolai, Eric
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2016, Volume 26, Issue 1, pp. 25 - 32
Chemical modulation of a formerly disclosed DGAT-1 inhibitor resulted in the identification of a compound with a suitable profile for preclinical development.... 
DGAT-1 inhibitors | Oxadiazole | Diacylglycerol acyltransferase type 1 | Metabolic lability | Thiadiazole | Solubility | CHEMISTRY, MEDICINAL | METABOLISM | 1 DGAT1 | CHEMISTRY, ORGANIC | Oxadiazoles - chemical synthesis | Humans | Enzyme Inhibitors - pharmacology | Models, Molecular | Structure-Activity Relationship | Enzyme Inhibitors - chemical synthesis | Diacylglycerol O-Acyltransferase - antagonists & inhibitors | Dose-Response Relationship, Drug | Thiadiazoles - chemical synthesis | Oxadiazoles - pharmacology | Thiadiazoles - chemistry | Enzyme Inhibitors - chemistry | Molecular Structure | Diacylglycerol O-Acyltransferase - metabolism | Oxadiazoles - chemistry | Thiadiazoles - pharmacology
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62. Full Text Novel group of tyrosyl-DNA-phosphodiesterase 1 inhibitors based on disaccharide nucleosides as drug prototypes for anti-cancer therapy
by Komarova, Anastasia O and Drenichev, Mikhail S and Dyrkheeva, Nadezhda S and Kulikova, Irina V and Oslovsky, Vladimir E and Zakharova, Olga D and Zakharenko, Alexandra L and Mikhailov, Sergey N and Lavrik, Olga I
Journal of Enzyme Inhibition and Medicinal Chemistry, ISSN 1475-6366, 01/2018, Volume 33, Issue 1, pp. 1415 - 1429
A new class of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors based on disaccharide nucleosides was identified. TDP1 plays an essential role in the... 
TDP1 inhibitor | tyrosyl-DNA phosphodiesterase 1 | Disaccharide nucleosides | topotecan | POLY(ADP-RIBOSE) POLYMERASE | CHEMISTRY, MEDICINAL | REPAIR ENZYME | CRYSTAL-STRUCTURE | HUMAN-CELLS | BIOCHEMISTRY & MOLECULAR BIOLOGY | TOPOISOMERASE-I | DAMAGE | SPINOCEREBELLAR ATAXIA | TDP1 | PYRIMIDINE NUCLEOSIDES | DERIVATIVES | Index Medicus
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63. Full Text Synthesis and biological evaluation of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides as pyruvate dehydrogenase kinase 1 (PDK1) inhibitors to reduce the growth of cancer cells
by Zhang, Shao-Lin and Zhang, Wen and Yang, Zheng and Hu, Xiaohui and Tam, Kin Yip
European Journal of Pharmaceutical Sciences, ISSN 0928-0987, 12/2017, Volume 110, pp. 87 - 92
Most cancer cells exhibit a high rate of glycolysis and reduced capacity in mitochondrial oxidative phosphorylation. The expression of pyruvate dehydrogenase... 
Anti-proliferation | Pyruvate dehydrogenase kinase | Binding affinity | Pyruvate dehydrogenase complex | Amides - pharmacology | Propionates - pharmacology | Oxidoreductases - metabolism | Amides - chemical synthesis | Apoptosis - drug effects | Cell Survival | Antineoplastic Agents - chemical synthesis | Humans | Enzyme Inhibitors - pharmacology | Mitochondria - drug effects | Enzyme Inhibitors - chemical synthesis | Drug Discovery | Oxidoreductases - chemistry | Glucose - chemistry | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Cell Line, Tumor | Glucose - metabolism | Glycolysis | Antineoplastic Agents - pharmacology | Propionates - chemical synthesis | Protein-Serine-Threonine Kinases - metabolism | Prevention | Glucose metabolism | Growth | Cell death | Analysis | Cancer cells | Cancer
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64. Full Text Platelets retain high levels of active plasminogen activator inhibitor 1
by Brogren, HelƩn and Wallmark, Karin and Deinum, Johanna and Karlsson, Lena and Jern, Sverker and Sahlgrenska akademin and Institutionen fƶr medicin, avdelningen fƶr akut och kardiovaskulƤr medicin and Institute of Medicine, Department of Emergeny and Cardiovascular Medicine and Gƶteborgs universitet and Gothenburg University and Sahlgrenska Academy
PLoS ONE, ISSN 1932-6203, 11/2011, Volume 6, Issue 11, p. e26762
The vascular fibrinolytic system is crucial for spontaneous lysis of blood clots. Plasminogen activator inhibitor 1 (PAI-1), the principal inhibitor of the key... 
PLASMA | SODIUM DODECYL-SULFATE | HUMAN THROMBI | MULTIDISCIPLINARY SCIENCES | HUMAN-ENDOTHELIAL CELLS | VITRONECTIN | ANTIGEN ASSAYS | PAI-1 | TYPE-1 | PROTEINS | IDENTIFICATION | Iodine Radioisotopes | Platelet Count | Enzyme-Linked Immunosorbent Assay | Plasminogen Activator Inhibitor 1 - metabolism | Tissue Plasminogen Activator - metabolism | Blood Platelets - metabolism | Humans | Platelet Activation - physiology | Octoxynol | Fibrinolysis | Blotting, Western | Physiological aspects | Tissue plasminogen activator | Analysis | Plasma | Sonication | Antigens | Blood coagulation | Enzymes | Complex formation | Laboratories | Polyamide-imides | Thawing | Scintigraphy | Blood | Freezing | t-Plasminogen activator | Proteins | Medicine | Studies | Fibrin | Dilution | Inhibitors | Blood platelets | Lysis | Plasminogen activator inhibitors | Platelets | MEDICIN OCH HƄLSOVETENSKAP | MEDICAL AND HEALTH SCIENCES
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65. Full Text Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1ā€²-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-3,4-dihydrospiro[chromene-2,4ā€²-piperidine] analogs
by Uto, Yoshikazu and Ueno, Yuko and Kiyotsuka, Yohei and Miyazawa, Yuriko and Kurata, Hitoshi and Ogata, Tsuneaki and Yamada, Makiko and Deguchi, Tsuneo and Konishi, Masahiro and Takagi, Toshiyuki and Wakimoto, Satoko and Ohsumi, Jun
European Journal of Medicinal Chemistry, ISSN 0223-5234, 2010, Volume 45, Issue 11, pp. 4788 - 4796
In continuation of our investigation on novel stearoyl-CoA desaturase (SCD) 1 inhibitors, we have already reported on the structural modification of the... 
Oxadiazole | SCD1 inhibitor | Spiropiperidine | CHEMISTRY, MEDICINAL | TRIGLYCERIDES | IDENTIFICATION | POTENT INHIBITORS | DISCOVERY | OBESITY | DISRUPTION | GENE | BIOSYNTHESIS | MICE | SCD INHIBITORS | Magnetic Resonance Spectroscopy | Pyridines - chemistry | Mice, Inbred C57BL | Enzyme Inhibitors - pharmacology | Pyridines - chemical synthesis | Pyridines - pharmacokinetics | Structure-Activity Relationship | Stearoyl-CoA Desaturase - antagonists & inhibitors | Enzyme Inhibitors - chemical synthesis | Animals | Spectrometry, Mass, Electrospray Ionization | Enzyme Inhibitors - pharmacokinetics | Enzyme Inhibitors - chemistry | Mice | Pyridines - pharmacology | Drug Evaluation, Preclinical | Physiological aspects | Enzymes | Heterocyclic compounds | Analysis
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66. Full Text Discovery of potent polyphosphate kinase 1 (PPK1) inhibitors using structureā€based exploration of PPK1Pharmacophoric space coupled with docking analyses
by Bashatwah, Rasha M and Khanfar, Mohammad A and Bardaweel, Sanaa K
Journal of Molecular Recognition, ISSN 0952-3499, 10/2018, Volume 31, Issue 10, pp. e2726 - n/a
Inorganic polyphosphate (polyP) is present in all living forms of life. Studied mainly in prokaryotes, polyP and its associated enzymes are vital in diverse... 
PPK1 inhibitors | structureā€based aided design | bacterial resistance | biofilm | metabolic phenotype | PolyP | structure-based aided design | INORGANIC POLYPHOSPHATE | CELLS | PROTEIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | ESCHERICHIA-COLI | INDUCTION | PSEUDOMONAS-AERUGINOSA PAO1 | BIOPHYSICS | PURIFICATION | DICTYOSTELIUM-DISCOIDEUM | HELICOBACTER-PYLORI | Phosphates | Discovery and exploration | Chemotherapy | Outer space | Escherichia coli | Drug resistance | Cancer | Virulence | Homology | Gene deletion | Kinases | PharmacoPhores | Eukaryotes | Maps | Clonal deletion | E coli | Deletion | Docking | Inhibition | Polyphosphate kinase | Enzymes | Prokaryotes | Exploration | Pharmacology | Metabolism | Organic chemistry | Biofilms | Inhibitors | Metabolic pathways | Gene mapping | Binding sites
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67. Full Text Novel 11Ī²-hydroxysteroid dehydrogenase 1 inhibitors reduce cortisol levels in keratinocytes and improve dermal collagen content in human ex vivo skin after exposure to cortisone and UV
by Boudon, StƩphanie M and Vuorinen, Anna and Geotti-Bianchini, Piero and Wandeler, Eliane and Kratschmar, Denise V and Heidl, Marc and Campiche, Remo and Jackson, Eileen and Odermatt, Alex
PloS one, ISSN 1932-6203, 2017, Volume 12, Issue 2, p. e0171079
Activity and selectivity assessment of new bi-aryl amide 11 beta-hydroxysteroid dehydrogenase 1 (11 beta-HSD1) inhibitors, prepared in a modular manner via... 
GLUCOCORTICOID-RECEPTOR | CYTOKINE PRODUCTION | STIMULATION | MULTIDISCIPLINARY SCIENCES | IN-VIVO | ULTRAVIOLET-RADIATION | AGED SKIN | TYPE-1 | CORTICOSTEROIDS | PITUITARY-ADRENAL AXIS | MOLECULAR-MECHANISMS | Amides - pharmacology | Amides - chemical synthesis | Skin - metabolism | Cortisone - adverse effects | Humans | Skin Aging - drug effects | Enzyme Inhibitors - pharmacology | Hydrocortisone - metabolism | Skin Aging - radiation effects | Enzyme Inhibitors - chemical synthesis | 11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors | Ultraviolet Rays - adverse effects | Collagen - metabolism | Keratinocytes - drug effects | Keratinocytes - metabolism | Skin - radiation effects | Enzyme Inhibitors - chemistry | HEK293 Cells | Amides - chemistry | Skin Aging - physiology | In Vitro Techniques | Skin - drug effects | Enzymes | Cross coupling | Dehydrogenases | Cytokines | Keratinocytes | Hormones | Hydrocortisone | Dehydrogenase | Damage prevention | Cortisone | Coupling (molecular) | Toxicology | Inhibitors | Aromatic compounds | Rodents | Collagen | 11Ī²-Hydroxysteroid dehydrogenase | Fibroblasts | Aging | Skin | Inhibition | Pharmaceutical industry | Pharmaceutical sciences | Recombinant
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68. Full Text Impairment of prostate cancer cell growth by a selective and reversible lysineā€specific demethylase 1 inhibitor
by Willmann, Dominica and Lim, Soyoung and Wetzel, Stefan and Metzger, Eric and Jandausch, Anett and Wilk, Wolfram and Jung, Manfred and Forne, Ignasi and Imhof, Axel and Janzer, Andreas and Kirfel, Jutta and Waldmann, Herbert and SchĆ¼le, Roland and Buettner, Reinhard
International Journal of Cancer, ISSN 0020-7136, 12/2012, Volume 131, Issue 11, pp. 2704 - 2709
Postā€translational modifications of histones by chromatin modifying enzymes regulate chromatin structure and gene expression. As deregulation of histone... 
demethylation | prostate cancer | chromatinā€modifying enzyme | inhibitor | LSD1 | chromatin-modifying enzyme | TRANS-2-PHENYLCYCLOPROPYLAMINE | ONCOLOGY | ANALOGS | REEXPRESSION | HISTONE DEMETHYLATION | SILENCED GENES | Chromatin - metabolism | Prostatic Neoplasms - metabolism | Histone Demethylases - antagonists & inhibitors | Humans | Receptors, Androgen - metabolism | Male | Histone Demethylases - genetics | Pyrones - pharmacology | Prostatic Neoplasms - genetics | Protein Processing, Post-Translational - drug effects | Prostatic Neoplasms - drug therapy | Prostatic Neoplasms - pathology | Cell Growth Processes - drug effects | Enzyme Inhibitors - pharmacology | Xenograft Model Antitumor Assays | Histone Demethylases - metabolism | Animals | Histones - genetics | Methylation - drug effects | Mice, Nude | Cell Line, Tumor | Mice | Histones - metabolism | Androgens - metabolism | Chromatin - genetics | Enzymes | Medical colleges | Chromatin | Growth | Genes | Development and progression | DNA binding proteins | Gene expression | Prevention | Anopheles | Lysine | Physiological aspects | Histones | Prostate cancer | Cancer | Cell growth
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69. Full Text Discovery and Structureā€“Activity Relationship of Novel 2,3-Dihydrobenzofuran-7-carboxamide and 2,3-Dihydrobenzofuran-3(2H)ā€‘one-7-carboxamide Derivatives as Poly(ADP-ribose)polymeraseā€‘1 Inhibitors
by Patel, Maulik R and Bhatt, Aaditya and Steffen, Jamin D and Chergui, Adel and Murai, Junko and Pommier, Yves and Pascal, John M and Trombetta, Louis D and Fronczek, Frank R and Talele, Tanaji T and Brookhaven National Laboratory (BNL)
Journal of Medicinal Chemistry, ISSN 0022-2623, 07/2014, Volume 57, Issue 13, pp. 5579 - 5601
Novel substituted 2,3-dihydrobenzofuran-7-carboxamide (DHBF-7-carboxamide) and 2,3-dihydrobenzofuran-3Ā­(2H)-one-7-carboxamide (DHBF-3-one-7-carboxamide)... 
DESIGN | CHEMISTRY, MEDICINAL | MUTANT-CELLS | DNA-DAMAGE | POLYMERASE INHIBITOR | ABT-888 | ALPHA | OPTIMIZATION | AGENTS | PARP INHIBITORS | FAMILY | Amides - pharmacology | Cell Line | Animals | Amides - chemical synthesis | Chickens | Enzyme Inhibitors - pharmacology | Benzofurans - chemical synthesis | Benzofurans - pharmacology | Structure-Activity Relationship | Enzyme Inhibitors - chemical synthesis | Drug Discovery | Poly(ADP-ribose) Polymerase Inhibitors
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70. Full Text Updates in the clinical development of Epacadostat and other indoleamine 2,3-dioxygenase 1 inhibitors (IDO1) for human cancers
by Komiya, Takefumi and Huang, Chao H
Frontiers in Oncology, ISSN 2234-943X, 10/2018, Volume 8, p. 423
Recent application of immunotherapy in clinical oncology revolutionized ourmanagement of advanced human cancers. Check point inhibitors targeting CTLA4 and... 
IDO (indoleamine 2,3-dioxygenase) | Tryptophan | Clinical trials as topic | Immuno-oncology | PD-1 | IDO1 inhibitor | IDO (indoleamine 2, 3-dioxygenase) | clinical trials as topic | STAGE-III | SUPPRESSION | CHEMOTHERAPY | CELL LUNG-CANCER | TRIAL | MELANOMA | ONCOLOGY | immuno-oncology | NIVOLUMAB | tryptophan | PROGRESSION | IPILIMUMAB | Antimitotic agents | Enzyme inhibitors | Tryptophan metabolism | Immunotherapy | Oncology, Experimental | Research | Antineoplastic agents | Health aspects | Cancer
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71. Full Text Prevention of Obesity and Insulin Resistance in Mice Lacking Plasminogen Activator Inhibitor 1
by Li-Jun Ma and Su-Li Mao and Kevin L. Taylor and Talerngsak Kanjanabuch and YouFei Guan and YaHua Zhang and Nancy J. Brown and Larry L. Swift and Owen P. McGuinness and David H. Wasserman and Douglas E. Vaughan and Agnes B. Fogo
Diabetes, ISSN 0012-1797, 02/2004, Volume 53, Issue 2, pp. 336 - 346
Prevention of Obesity and Insulin Resistance in Mice Lacking Plasminogen Activator Inhibitor 1 Li-Jun Ma 1 , Su-Li Mao 1 , Kevin L. Taylor 1 , Talerngsak... 
SKELETAL-MUSCLE | TYPE-2 DIABETIC-PATIENTS | ENERGY-EXPENDITURE | ENDOCRINOLOGY & METABOLISM | GENE-EXPRESSION | PPAR-GAMMA | DIET-INDUCED OBESITY | CARDIOVASCULAR MORBIDITY | MITOCHONDRIAL UNCOUPLING PROTEINS | ANGIOTENSIN-CONVERTING-ENZYME | ADIPOSE-TISSUE | Ion Channels | Male | Mitochondrial Proteins | Obesity - blood | Obesity - genetics | Plasminogen Activator Inhibitor 1 - physiology | Adiponectin | Insulin Resistance - physiology | Polymerase Chain Reaction | Transcription, Genetic | Plasminogen Activator Inhibitor 1 - deficiency | Plasminogen Activator Inhibitor 1 - genetics | Weight Gain | Hyperinsulinism | Disease Models, Animal | Insulin - pharmacology | Membrane Proteins - genetics | Intercellular Signaling Peptides and Proteins | RNA, Messenger - genetics | Insulin - administration & dosage | Calorimetry, Indirect | Mice, Knockout | Triglycerides - metabolism | Blood Glucose - drug effects | Proteins - genetics | Carrier Proteins - genetics | Animals | Obesity - prevention & control | Insulin Resistance - genetics | Triglycerides - blood | Mice | Glucose Clamp Technique | Uncoupling Protein 1 | Blood Glucose - metabolism | Case studies | Obesity | Insulin resistance | Care and treatment | Thrombolytic drugs | Diabetes
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72. Full Text Lysine-Specific Histone Demethylase 1 Inhibitors Control Breast Cancer Proliferation in ERĪ±-Dependent and -Independent Manners
by Pollock, Julie A and Larrea, Michelle D and Jasper, Jeff S and McDonnell, Donald P and McCafferty, Dewey G
ACS Chemical Biology, ISSN 1554-8929, 07/2012, Volume 7, Issue 7, pp. 1221 - 1231
Lysine specific demethylase 1 (LSD1, also known as KDM1) is a histone modifying enzyme that regulates the expression of many genes important in cancer... 
TRANS-2-PHENYLCYCLOPROPYLAMINE | METHYLATION | ANALOGS | BIOCHEMISTRY & MOLECULAR BIOLOGY | DEACETYLASE INHIBITORS | CLINICAL-TRIALS | LSD1 | TRANSCRIPTION | GENE ACTIVATION | REEXPRESSION | SILENCED GENES | Pargyline - therapeutic use | Histone Demethylases - antagonists & inhibitors | Humans | Enzyme Inhibitors - pharmacology | Breast Neoplasms - drug therapy | Enzyme Inhibitors - therapeutic use | Histone Demethylases - metabolism | Breast Neoplasms - enzymology | Breast Neoplasms - pathology | Cell Line, Tumor | Pargyline - pharmacology | Female | Cell Proliferation - drug effects | Estrogen Receptor alpha - physiology | breast cancer | phenylcyclopropylamines | Lysine demethylase | estrogen receptor
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73. Full Text One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening
by Mpamhanga, Chidochangu P and Spinks, Daniel and Tulloch, Lindsay B and Shanks, Emma J and Robinson, David A and Collie, Iain T and Fairlamb, Alan H and Wyatt, Paul G and Frearson, Julie A and Hunter, William N and Gilbert, Ian H and Brenk, Ruth
Journal of Medicinal Chemistry, ISSN 0022-2623, 07/2009, Volume 52, Issue 14, pp. 4454 - 4465
The enzyme pteridine reductase 1 (PTR1) is a potential target for new compounds to treat human African trypanosomiasis. A virtual screening campaign for... 
LEISHMANIA-MAJOR | CHEMISTRY, MEDICINAL | MOLECULAR-DOCKING | METABOLISM | PROTEIN-LIGAND DOCKING | THYMIDYLATE SYNTHASE | ANTIOPPORTUNISTIC INFECTION AGENTS | RESISTANCE | FORCE-FIELD | ANTITUMOR | PREDICTION | Oxidoreductases - antagonists & inhibitors | Drug Evaluation, Preclinical - methods | Enzyme Inhibitors - metabolism | Oxidoreductases - metabolism | Benzothiazoles - pharmacology | Humans | Molecular Conformation | Enzyme Inhibitors - pharmacology | Models, Molecular | Substrate Specificity | Benzimidazoles - chemistry | Trypanosoma brucei brucei - enzymology | Oxidoreductases - chemistry | Animals |