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Tytuł :
Improvement of obesity-associated disorders by a small-molecule drug targeting mitochondria of adipose tissue macrophages.
Autorzy :
Wang Y; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Tang B; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.; Oncology Department, The General Hospital of Western Theater Command, Chengdu, Sichuan, 610083, China.
Long L; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Luo P; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Xiang W; Department of Biochemistry and Molecular Biology, Third Military Medical University, Chongqing, 400038, China.
Li X; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Wang H; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.; Department of Clinical Medicine, Southwest Medical University, Luzhou, Sichuan, 646000, China.
Jiang Q; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.; Department of Clinical Medicine, Southwest Medical University, Luzhou, Sichuan, 646000, China.
Tan X; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Luo S; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Li H; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Wang Z; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Chen Z; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Leng Y; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Jiang Z; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Wang Y; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Ma L; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Wang R; Department of Cardiology, Daping Hospital, Third Military Medical University, Chongqing, 400042, China.
Zeng C; Department of Cardiology, Daping Hospital, Third Military Medical University, Chongqing, 400042, China.
Liu Z; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China.
Wang Y; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China. .
Miao H; Department of Biochemistry and Molecular Biology, Third Military Medical University, Chongqing, 400038, China. .
Shi C; Institute of Rocket Force Medicine, State Key Laboratory of Trauma, Burns and Combined Injury, Third Military Medical University, Chongqing, 400038, China. .
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Źródło :
Nature communications [Nat Commun] 2021 Jan 04; Vol. 12 (1), pp. 102. Date of Electronic Publication: 2021 Jan 04.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Delivery Systems*
Adipose Tissue/*metabolism
Macrophages/*metabolism
Mitochondria/*metabolism
Obesity/*drug therapy
Small Molecule Libraries/*therapeutic use
Animals ; Body Weight/drug effects ; Fatty Liver/genetics ; Fatty Liver/pathology ; Inflammation/genetics ; Inflammation/pathology ; Insulin Resistance ; Liver/metabolism ; Liver/pathology ; Macrophage Activation/drug effects ; Macrophages/drug effects ; Macrophages/pathology ; Male ; Mice ; Mice, Inbred C57BL ; Mitochondria/drug effects ; Obesity/genetics ; Obesity/pathology ; Proto-Oncogene Proteins c-akt/metabolism ; RAW 264.7 Cells ; RNA, Messenger/genetics ; RNA, Messenger/metabolism ; Reactive Oxygen Species/metabolism ; Signal Transduction/drug effects ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/pharmacology ; Weight Loss/drug effects
Czasopismo naukowe
Tytuł :
Site mapping and small molecule blind docking reveal a possible target site on the SARS-CoV-2 main protease dimer interface.
Autorzy :
Liang J; Epigenomic Medicine, Department of Diabetes, Central Clinical School, Monash University, Melbourne, VIC 3004, Australia; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Karagiannis C; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia; School of Agriculture and Food, Faculty of Veterinary and Agricultural Sciences, University of Melbourne, Parkville, VIC 3052, Australia.
Pitsillou E; Epigenomic Medicine, Department of Diabetes, Central Clinical School, Monash University, Melbourne, VIC 3004, Australia; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Darmawan KK; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Ng K; School of Agriculture and Food, Faculty of Veterinary and Agricultural Sciences, University of Melbourne, Parkville, VIC 3052, Australia.
Hung A; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Karagiannis TC; Epigenomic Medicine, Department of Diabetes, Central Clinical School, Monash University, Melbourne, VIC 3004, Australia; Department of Clinical Pathology, The University of Melbourne, Parkville, VIC 3052, Australia. Electronic address: .
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Źródło :
Computational biology and chemistry [Comput Biol Chem] 2020 Dec; Vol. 89, pp. 107372. Date of Electronic Publication: 2020 Sep 05.
Typ publikacji :
Journal Article
MeSH Terms :
Antiviral Agents/*pharmacology
Coronavirus 3C Proteases/*antagonists & inhibitors
Coronavirus 3C Proteases/*chemistry
Coronavirus Protease Inhibitors/*pharmacology
Protein Multimerization/*drug effects
SARS-CoV-2/*drug effects
SARS-CoV-2/*enzymology
Small Molecule Libraries/*pharmacology
Amides/chemical synthesis ; Amides/chemistry ; Amides/pharmacology ; Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Azoles/chemical synthesis ; Azoles/chemistry ; Azoles/pharmacology ; Coronavirus 3C Proteases/metabolism ; Coronavirus Protease Inhibitors/chemical synthesis ; Coronavirus Protease Inhibitors/chemistry ; Humans ; Ligands ; Lopinavir/chemical synthesis ; Lopinavir/chemistry ; Lopinavir/pharmacology ; Microbial Sensitivity Tests ; Models, Molecular ; Molecular Structure ; Organoselenium Compounds/chemical synthesis ; Organoselenium Compounds/chemistry ; Organoselenium Compounds/pharmacology ; Ritonavir/chemical synthesis ; Ritonavir/chemistry ; Ritonavir/pharmacology ; SARS-CoV-2/metabolism ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Discovery of small molecule inhibitors of Leishmania braziliensis Hsp90 chaperone.
Autorzy :
Batista FAH; São Carlos Institute of Chemistry (IQSC), University of São Paulo (USP), São Carlos, Brazil.
Ramos SL Jr; São Carlos Institute of Chemistry (IQSC), University of São Paulo (USP), São Carlos, Brazil.
Tassone G; Department of Biotechnology, Chemistry and Pharmacy - Department of Excellence 2018-2022, University of Siena, Siena, Italy.
Leitão A; Medicinal Chemistry Group (NEQUIMED), IQSC-USP, University of São Paulo, São Carlos, Brazil.
Montanari CA; Medicinal Chemistry Group (NEQUIMED), IQSC-USP, University of São Paulo, São Carlos, Brazil.
Botta M; Department of Biotechnology, Chemistry and Pharmacy - Department of Excellence 2018-2022, University of Siena, Siena, Italy.; Lead Discovery Siena S.r., Siena, Italy.; Sbarro Institute for Cancer Research and Molecular Medicine, Center for Biotechnology, College of Science and Technology, Temple University, Philadelphia, PA, USA.
Mori M; Department of Biotechnology, Chemistry and Pharmacy - Department of Excellence 2018-2022, University of Siena, Siena, Italy.
Borges JC; São Carlos Institute of Chemistry (IQSC), University of São Paulo (USP), São Carlos, Brazil.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 639-649.
Typ publikacji :
Journal Article
MeSH Terms :
Antiprotozoal Agents/*pharmacology
Enzyme Inhibitors/*pharmacology
HSP90 Heat-Shock Proteins/*antagonists & inhibitors
Leishmania braziliensis/*drug effects
Molecular Chaperones/*pharmacology
Small Molecule Libraries/*pharmacology
Adenosine Triphosphatases/antagonists & inhibitors ; Adenosine Triphosphatases/metabolism ; Antiprotozoal Agents/chemical synthesis ; Antiprotozoal Agents/chemistry ; Dose-Response Relationship, Drug ; Drug Discovery ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; HSP90 Heat-Shock Proteins/metabolism ; Leishmania braziliensis/chemistry ; Models, Molecular ; Molecular Chaperones/chemical synthesis ; Molecular Chaperones/chemistry ; Molecular Structure ; Parasitic Sensitivity Tests ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
Autorzy :
Miller RR; Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., 126 E. Lincoln Avenue, Rahway, New Jersey 07065, United States.
Madeira M; Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., 126 E. Lincoln Avenue, Rahway, New Jersey 07065, United States.
Wood HB; Chemistry, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Geissler WM; Business Development & Licensing, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Raab CE; Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States.
Martin IJ; Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12156-12170. Date of Electronic Publication: 2020 Jul 07.
Typ publikacji :
Journal Article
MeSH Terms :
Pharmaceutical Preparations/*metabolism
Small Molecule Libraries/*chemistry
Area Under Curve ; Blood Proteins/chemistry ; Blood Proteins/metabolism ; Drug Design ; Half-Life ; Humans ; Hydrophobic and Hydrophilic Interactions ; Pharmaceutical Preparations/chemistry ; Protein Binding ; ROC Curve ; Small Molecule Libraries/metabolism ; Small Molecule Libraries/pharmacokinetics
Czasopismo naukowe
Tytuł :
Small-Molecule Fms-like Tyrosine Kinase 3 Inhibitors: An Attractive and Efficient Method for the Treatment of Acute Myeloid Leukemia.
Autorzy :
Zhong Y; National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Qiu RZ; National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Sun SL; National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Zhao C; National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Fan TY; National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Chen M; National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Li NG; National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Shi ZH; Department of Organic Chemistry, China Pharmaceutical University, Nanjing 211198, China.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12403-12428. Date of Electronic Publication: 2020 Jul 21.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Review
MeSH Terms :
Protein Kinase Inhibitors/*chemistry
Small Molecule Libraries/*chemistry
fms-Like Tyrosine Kinase 3/*antagonists & inhibitors
Humans ; Indoles/chemistry ; Indoles/pharmacology ; Indoles/therapeutic use ; Leukemia, Myeloid, Acute/drug therapy ; Leukemia, Myeloid, Acute/pathology ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Pyrazoles/therapeutic use ; Pyrimidines/chemistry ; Pyrimidines/pharmacology ; Pyrimidines/therapeutic use ; Signal Transduction/drug effects ; Small Molecule Libraries/pharmacology ; Small Molecule Libraries/therapeutic use ; Urea/analogs & derivatives ; Urea/pharmacology ; Urea/therapeutic use ; fms-Like Tyrosine Kinase 3/metabolism
Czasopismo naukowe
Tytuł :
Reviews on Biological Activity, Clinical Trial and Synthesis Progress of Small Molecules for the Treatment of COVID-19.
Autorzy :
Li D; State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China.
Hu J; State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China. .
Li D; Department of Modern Economy and Trade, Hunan Vocational College of Engineering, Changsha, 410151, People's Republic of China.
Yang W; State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China. .
Yin SF; State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China.
Qiu R; State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China. .
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Źródło :
Topics in current chemistry (Cham) [Top Curr Chem (Cham)] 2021 Jan 11; Vol. 379 (1), pp. 4. Date of Electronic Publication: 2021 Jan 11.
Typ publikacji :
Journal Article; Review
MeSH Terms :
Small Molecule Libraries*
Antiviral Agents/*chemical synthesis
Antiviral Agents/*pharmacology
COVID-19/*drug therapy
Antimalarials/therapeutic use ; Antiviral Agents/therapeutic use ; Clinical Trials as Topic ; Drug Repositioning ; Humans ; Janus Kinase Inhibitors/therapeutic use
Czasopismo naukowe
Tytuł :
Structural Basis of SARS-CoV-2- and SARS-CoV-Receptor Binding and Small-Molecule Blockers as Potential Therapeutics.
Autorzy :
Sivaraman H; Department of Biological Sciences, National University of Singapore, Singapore 117543; email: .
Er SY; Department of Biological Sciences, National University of Singapore, Singapore 117543; email: .
Choong YK; Department of Biological Sciences, National University of Singapore, Singapore 117543; email: .
Gavor E; Department of Biological Sciences, National University of Singapore, Singapore 117543; email: .
Sivaraman J; Department of Biological Sciences, National University of Singapore, Singapore 117543; email: .
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Źródło :
Annual review of pharmacology and toxicology [Annu Rev Pharmacol Toxicol] 2021 Jan 06; Vol. 61, pp. 465-493. Date of Electronic Publication: 2020 Aug 21.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Review
MeSH Terms :
Small Molecule Libraries*
Angiotensin-Converting Enzyme 2/*drug effects
Antiviral Agents/*pharmacology
Antiviral Agents/*therapeutic use
COVID-19/*drug therapy
Receptors, Virus/*drug effects
Humans ; Protease Inhibitors/therapeutic use
Czasopismo naukowe
Tytuł :
Allosteric Inhibition of the SARS-CoV-2 Main Protease: Insights from Mass Spectrometry Based Assays*.
Autorzy :
El-Baba TJ; Physical and Theoretical Chemistry Laboratory, University of Oxford, South Parks Rd., OX1 3QZ, Oxford, UK.
Lutomski CA; Physical and Theoretical Chemistry Laboratory, University of Oxford, South Parks Rd., OX1 3QZ, Oxford, UK.
Kantsadi AL; Department of Biochemistry, University of Oxford, South Parks Rd., OX1 3QU, Oxford, UK.
Malla TR; Chemistry Research Laboratory, University of Oxford, 12 Mansfield Rd, OX1 3TA, Oxford, UK.
John T; Chemistry Research Laboratory, University of Oxford, 12 Mansfield Rd, OX1 3TA, Oxford, UK.
Mikhailov V; Chemistry Research Laboratory, University of Oxford, 12 Mansfield Rd, OX1 3TA, Oxford, UK.
Bolla JR; Physical and Theoretical Chemistry Laboratory, University of Oxford, South Parks Rd., OX1 3QZ, Oxford, UK.
Schofield CJ; Chemistry Research Laboratory, University of Oxford, 12 Mansfield Rd, OX1 3TA, Oxford, UK.
Zitzmann N; Department of Biochemistry, University of Oxford, South Parks Rd., OX1 3QU, Oxford, UK.
Vakonakis I; Department of Biochemistry, University of Oxford, South Parks Rd., OX1 3QU, Oxford, UK.
Robinson CV; Physical and Theoretical Chemistry Laboratory, University of Oxford, South Parks Rd., OX1 3QZ, Oxford, UK.
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Źródło :
Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2020 Dec 21; Vol. 59 (52), pp. 23544-23548. Date of Electronic Publication: 2020 Oct 15.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Models, Molecular*
Coronavirus 3C Proteases/*chemistry
Coronavirus Protease Inhibitors/*chemistry
SARS-CoV-2/*enzymology
Small Molecule Libraries/*chemistry
Allosteric Regulation ; Binding Sites ; Biological Assay ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus Protease Inhibitors/pharmacology ; Crystallography, X-Ray ; Mass Spectrometry ; Protein Binding ; Protein Conformation ; Protein Multimerization ; SARS-CoV-2/physiology ; Small Molecule Libraries/pharmacology ; Substrate Specificity ; Virus Replication
Czasopismo naukowe
Tytuł :
Can scholarly pirate libraries bridge the knowledge access gap? An empirical study on the structural conditions of book piracy in global and European academia.
Autorzy :
Bodó B; Institute for Information Law, University of Amsterdam, Amsterdam, The Netherlands.
Antal D; Independent researcher, The Netherlands.
Puha Z; Department of Methodology and Statistics, Jheronimus Academy of Data Science, Tilburg University, Tilburg, The Netherlands.
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Źródło :
PloS one [PLoS One] 2020 Dec 03; Vol. 15 (12), pp. e0242509. Date of Electronic Publication: 2020 Dec 03 (Print Publication: 2020).
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Access to Information*
Books*
Empirical Research*
Internationality*
Knowledge*
Libraries*
Scholarly Communication*
Europe ; Gross Domestic Product ; Models, Theoretical ; Statistics as Topic
Czasopismo naukowe
Tytuł :
Repurposing strategies on pyridazinone-based series by pharmacophore- and structure-driven screening.
Autorzy :
Floresta G; Institute of Pharmaceutical Science, King's College London, London, UK.
Crocetti L; NEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino (Fi), Italy.
Giovannoni MP; NEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino (Fi), Italy.
Biagini P; NEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino (Fi), Italy.
Cilibrizzi A; Institute of Pharmaceutical Science, King's College London, London, UK.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 1137-1144.
Typ publikacji :
Journal Article
MeSH Terms :
Aspartate Aminotransferases/*antagonists & inhibitors
Enzyme Inhibitors/*pharmacology
Pyridazines/*pharmacology
Small Molecule Libraries/*pharmacology
Aspartate Aminotransferases/metabolism ; Chemistry, Pharmaceutical ; Drug Evaluation, Preclinical ; Enzyme Inhibitors/chemistry ; Ligands ; Models, Molecular ; Molecular Structure ; Pyridazines/chemistry ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Human MYC G-quadruplex: From discovery to a cancer therapeutic target.
Autorzy :
Wang W; Key Laboratory of Saline-alkali Vegetation Ecology Restoration, Ministry of Education, College of Life Science, Northeast Forestry University, Harbin 150040, China.
Hu S; Key Laboratory of Saline-alkali Vegetation Ecology Restoration, Ministry of Education, College of Life Science, Northeast Forestry University, Harbin 150040, China.
Gu Y; Key Laboratory of Saline-alkali Vegetation Ecology Restoration, Ministry of Education, College of Life Science, Northeast Forestry University, Harbin 150040, China.
Yan Y; Key Laboratory of Saline-alkali Vegetation Ecology Restoration, Ministry of Education, College of Life Science, Northeast Forestry University, Harbin 150040, China.
Stovall DB; College of Arts and Sciences, Winthrop University, Rock Hill, SC 29733, United States.
Li D; Key Laboratory of Saline-alkali Vegetation Ecology Restoration, Ministry of Education, College of Life Science, Northeast Forestry University, Harbin 150040, China. Electronic address: .
Sui G; Key Laboratory of Saline-alkali Vegetation Ecology Restoration, Ministry of Education, College of Life Science, Northeast Forestry University, Harbin 150040, China. Electronic address: .
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Źródło :
Biochimica et biophysica acta. Reviews on cancer [Biochim Biophys Acta Rev Cancer] 2020 Dec; Vol. 1874 (2), pp. 188410. Date of Electronic Publication: 2020 Aug 19.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Review
MeSH Terms :
Neoplasms/*genetics
Proto-Oncogene Proteins c-myc/*chemistry
Proto-Oncogene Proteins c-myc/*genetics
Small Molecule Libraries/*pharmacology
Binding Sites ; G-Quadruplexes/drug effects ; Gene Expression Regulation, Neoplastic ; Humans ; Ligands ; Neoplasms/drug therapy ; Promoter Regions, Genetic/drug effects ; Proto-Oncogene Proteins c-myc/metabolism ; Small Molecule Libraries/therapeutic use ; Up-Regulation
Czasopismo naukowe
Tytuł :
Interaction of small molecules with the SARS-CoV-2 main protease in silico and in vitro validation of potential lead compounds using an enzyme-linked immunosorbent assay.
Autorzy :
Pitsillou E; Epigenomic Medicine, Department of Diabetes, Central Clinical School, Monash University, Melbourne, VIC 3004, Australia; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Liang J; Epigenomic Medicine, Department of Diabetes, Central Clinical School, Monash University, Melbourne, VIC 3004, Australia; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Karagiannis C; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia; Food Chemistry, Faculty of Veterinary and Agricultural Sciences, University of Melbourne, Parkville, VIC 3052, Australia.
Ververis K; Epigenomic Medicine, Department of Diabetes, Central Clinical School, Monash University, Melbourne, VIC 3004, Australia.
Darmawan KK; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Ng K; Food Chemistry, Faculty of Veterinary and Agricultural Sciences, University of Melbourne, Parkville, VIC 3052, Australia.
Hung A; School of Science, College of Science, Engineering & Health, RMIT University, VIC 3001, Australia.
Karagiannis TC; Epigenomic Medicine, Department of Diabetes, Central Clinical School, Monash University, Melbourne, VIC 3004, Australia; Department of Clinical Pathology, The University of Melbourne, Parkville, VIC 3052, Australia. Electronic address: .
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Źródło :
Computational biology and chemistry [Comput Biol Chem] 2020 Dec; Vol. 89, pp. 107408. Date of Electronic Publication: 2020 Oct 23.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme-Linked Immunosorbent Assay*
Antiviral Agents/*pharmacology
Coronavirus 3C Proteases/*metabolism
Coronavirus Protease Inhibitors/*pharmacology
SARS-CoV-2/*drug effects
Small Molecule Libraries/*pharmacology
Antiviral Agents/chemistry ; Coronavirus Protease Inhibitors/chemistry ; Fatty Acids/chemistry ; Fatty Acids/pharmacology ; Humans ; Ligands ; Microbial Sensitivity Tests ; Models, Molecular ; Phenols/chemistry ; Phenols/pharmacology ; SARS-CoV-2/metabolism ; Small Molecule Libraries/chemistry
Czasopismo naukowe

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