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Tytuł :
[Digital archives for historians: research during the pandemic].
Autorzy :
Palma P; Investigadora, Departamento de Ciencias Históricas y Geográficas/ Universidad de Tarapacá.Arica - Región de Arica y Parinacota - Chile .
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Transliterated Title :
Archivos digitales para historiadores: investigar en tiempos de pandemia.
Źródło :
Historia, ciencias, saude--Manguinhos [Hist Cienc Saude Manguinhos] 2021 Jan-Mar; Vol. 2828 (1), pp. 293-300.
Typ publikacji :
Directory; Historical Article
MeSH Terms :
Archives*
Libraries, Digital*
COVID-19 ; Chile ; History of Medicine ; Latin America ; Libraries ; Peru
Referencja
Tytuł :
Development of photocontrolled BRD4 PROTACs for tongue squamous cell carcinoma (TSCC).
Autorzy :
Li Z; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China.
Ma S; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China.
Yang X; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China.
Zhang L; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China.
Liang D; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China.
Dong G; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China.
Du L; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China. Electronic address: .
Lv Z; Department of Head and Neck Surgery, Shandong Provincial ENT Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250022, China. Electronic address: .
Li M; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Oct 15; Vol. 222, pp. 113608. Date of Electronic Publication: 2021 Jun 05.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Development*
Antineoplastic Agents/*pharmacology
Carcinoma, Squamous Cell/*drug therapy
Cell Cycle Proteins/*antagonists & inhibitors
Small Molecule Libraries/*pharmacology
Tongue Neoplasms/*drug therapy
Transcription Factors/*antagonists & inhibitors
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Carcinoma, Squamous Cell/metabolism ; Carcinoma, Squamous Cell/pathology ; Cell Cycle Proteins/metabolism ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Cells, Cultured ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Mice ; Mice, Nude ; Molecular Structure ; Neoplasms, Experimental/drug therapy ; Neoplasms, Experimental/metabolism ; Neoplasms, Experimental/pathology ; Photochemical Processes ; Proteolysis ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry ; Structure-Activity Relationship ; Tongue Neoplasms/metabolism ; Tongue Neoplasms/pathology ; Transcription Factors/metabolism ; Zebrafish
Czasopismo naukowe
Tytuł :
Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).
Autorzy :
Huang Q; Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Zhong Y; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Li B; Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Ouyang S; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Deng L; Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Mo J; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Shi S; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Lv N; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Wu R; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Liu P; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Hu W; Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Zhang X; Guangdong Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China. Electronic address: .
Wang Y; Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Oct 05; Vol. 221, pp. 113525. Date of Electronic Publication: 2021 May 07.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Antineoplastic Agents/*pharmacology
Pyridines/*pharmacology
STAT3 Transcription Factor/*antagonists & inhibitors
Small Molecule Libraries/*pharmacology
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Apoptosis/drug effects ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Cells, Cultured ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Female ; Humans ; Mammary Neoplasms, Experimental/drug therapy ; Mammary Neoplasms, Experimental/metabolism ; Mammary Neoplasms, Experimental/pathology ; Mice ; Mice, Inbred NOD ; Mice, SCID ; Molecular Docking Simulation ; Molecular Structure ; Pyridines/chemical synthesis ; Pyridines/chemistry ; STAT3 Transcription Factor/metabolism ; Signal Transduction/drug effects ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
High-Throughput Affinity Selection Mass Spectrometry Using SAMDI-MS to Identify Small-Molecule Binders of the Human Rhinovirus 3C Protease.
Autorzy :
Scholle MD; SAMDI Tech, Inc., Chicago, IL, USA.
McLaughlin D; MoMa Therapeutics, Boston, MA, USA.
Gurard-Levin ZA; SAMDI Tech, Inc., Chicago, IL, USA.
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Źródło :
SLAS discovery : advancing life sciences R & D [SLAS Discov] 2021 Sep; Vol. 26 (8), pp. 974-983. Date of Electronic Publication: 2021 Jun 19.
Typ publikacji :
Journal Article
MeSH Terms :
High-Throughput Screening Assays*
COVID-19/*drug therapy
Rhinovirus/*drug effects
Small Molecule Libraries/*chemistry
3C Viral Proteases/chemistry ; COVID-19/virology ; Drug Discovery ; Humans ; Ligands ; Mass Spectrometry ; SARS-CoV-2/drug effects ; SARS-CoV-2/pathogenicity ; Small Molecule Libraries/isolation & purification ; Small Molecule Libraries/therapeutic use
Czasopismo naukowe
Tytuł :
Targeting a noncanonical, hairpin-containing G-quadruplex structure from the MYCN gene.
Autorzy :
Yang M; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
Carter S; Pediatric Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-1928, USA.
Parmar S; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
Bume DD; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
Calabrese DR; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
Liang X; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
Yazdani K; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
Xu M; Pediatric Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-1928, USA.
Liu Z; Pediatric Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-1928, USA.
Thiele CJ; Pediatric Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-1928, USA.
Schneekloth JS; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702-1201, USA.
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Źródło :
Nucleic acids research [Nucleic Acids Res] 2021 Aug 20; Vol. 49 (14), pp. 7856-7869.
Typ publikacji :
Journal Article; Research Support, N.I.H., Intramural
MeSH Terms :
G-Quadruplexes*
DNA/*chemistry
N-Myc Proto-Oncogene Protein/*genetics
Nucleic Acid Conformation/*drug effects
Small Molecule Libraries/*pharmacology
Base Sequence ; Cell Line, Tumor ; Cell Survival/drug effects ; Cell Survival/genetics ; Circular Dichroism ; DNA/genetics ; DNA/metabolism ; Gene Expression Regulation, Neoplastic/drug effects ; Humans ; Ligands ; Molecular Structure ; N-Myc Proto-Oncogene Protein/metabolism ; Neuroblastoma/genetics ; Neuroblastoma/metabolism ; Neuroblastoma/pathology ; Oligonucleotides/chemistry ; Oligonucleotides/genetics ; Oligonucleotides/metabolism ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/metabolism ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
A Michael Acceptor Analogue, SKSI-0412, Down-Regulates Inflammation and Proliferation Factors through Suppressing Signal Transducer and Activator of Transcription 3 Signaling in IL-17A-Induced Human Keratinocyte.
Autorzy :
Kim AR; Department of Dermatology, School of Medicine, CHA University, 120 Haeryong-ro, Pocheon 11160, Gyeonggi-do, Korea.
Lee S; Department of Pharmacy, College of Pharmacy, CHA University, 120 Haeryong-ro, Pocheon 11160, Gyeonggi-do, Korea.
Shin JU; Department of Dermatology, CHA Bundang Mediacal Center, School of Medicine, CHA University, 59 Yatap-ro, Bundang-gu, Seongnam 13496, Gyeonggi-do, Korea.
Seok SH; Department of Dermatology, CHA Bundang Mediacal Center, School of Medicine, CHA University, 59 Yatap-ro, Bundang-gu, Seongnam 13496, Gyeonggi-do, Korea.
Suh YG; Department of Pharmacy, College of Pharmacy, CHA University, 120 Haeryong-ro, Pocheon 11160, Gyeonggi-do, Korea.
Kim DH; Department of Dermatology, CHA Bundang Mediacal Center, School of Medicine, CHA University, 59 Yatap-ro, Bundang-gu, Seongnam 13496, Gyeonggi-do, Korea.
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Źródło :
International journal of molecular sciences [Int J Mol Sci] 2021 Aug 16; Vol. 22 (16). Date of Electronic Publication: 2021 Aug 16.
Typ publikacji :
Journal Article
MeSH Terms :
Anti-Inflammatory Agents/*pharmacology
Interleukin-17/*adverse effects
Keratinocytes/*cytology
STAT3 Transcription Factor/*metabolism
Small Molecule Libraries/*pharmacology
Anti-Inflammatory Agents/chemical synthesis ; Anti-Inflammatory Agents/chemistry ; Cell Proliferation/drug effects ; Cells, Cultured ; Down-Regulation ; Humans ; Keratinocytes/drug effects ; Keratinocytes/metabolism ; Phosphorylation/drug effects ; Primary Cell Culture ; STAT3 Transcription Factor/chemistry ; Signal Transduction/drug effects ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Tailor-made amino acids in the design of small-molecule blockbuster drugs.
Autorzy :
Han J; Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing, 210037, Jiangsu, China.
Konno H; Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata, 992-8510, Japan.
Sato T; Hamari Chemicals Ltd., 1-19-40, Nankokita, Suminoe-ku, Osaka, 559-0034, Japan.
Soloshonok VA; Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, 20018, San Sebastián, Spain; IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, Plaza Bizkaia, 48013, Bilbao, Spain. Electronic address: .
Izawa K; Hamari Chemicals Ltd., 1-19-40, Nankokita, Suminoe-ku, Osaka, 559-0034, Japan. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Aug 05; Vol. 220, pp. 113448. Date of Electronic Publication: 2021 Apr 16.
Typ publikacji :
Journal Article; Review
MeSH Terms :
Drug Design*
Amino Acids/*pharmacology
Small Molecule Libraries/*pharmacology
Amino Acids/chemistry ; Chemistry, Pharmaceutical ; Humans ; Molecular Structure ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Understanding the brain uptake and permeability of small molecules through the BBB: A technical overview.
Autorzy :
Chowdhury EA; Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, Amarillo, USA.
Noorani B; Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, Amarillo, USA.
Alqahtani F; Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Bhalerao A; Department of Foundational Medical Studies, Oakland University William Beaumont School of Medicine, Rochester, USA.
Raut S; Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, Amarillo, USA.
Sivandzade F; Department of Foundational Medical Studies, Oakland University William Beaumont School of Medicine, Rochester, USA.
Cucullo L; Department of Foundational Medical Studies, Oakland University William Beaumont School of Medicine, Rochester, USA.
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Źródło :
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism [J Cereb Blood Flow Metab] 2021 Aug; Vol. 41 (8), pp. 1797-1820. Date of Electronic Publication: 2021 Jan 14.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Review
MeSH Terms :
Blood-Brain Barrier/*metabolism
Brain/*metabolism
Permeability/*drug effects
Small Molecule Libraries/*pharmacology
Animals ; Blood-Brain Barrier/drug effects ; Humans ; Kinetics ; Nervous System Diseases/metabolism ; Nervous System Diseases/pathology ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/metabolism ; Sucrose/chemistry ; Sucrose/metabolism
Czasopismo naukowe
Tytuł :
Cellular model system to dissect the isoform-selectivity of Akt inhibitors.
Autorzy :
Quambusch L; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Depta L; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Landel I; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Lubeck M; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Kirschner T; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Nabert J; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Uhlenbrock N; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Weisner J; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Kostka M; Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Dortmund, Germany.
Levy LM; Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Dortmund, Germany.
Schultz-Fademrecht C; Lead Discovery Center GmbH, Dortmund, Germany.
Glanemann F; Bridge Institute of Experimental Tumor Therapy, West German Cancer Center, University Medicine Essen, Essen, Germany.; Division of Solid Tumor Translational Oncology, German Cancer Research Center (DKFZ) and German Cancer Consortium (DKTK), partner site Essen, Heidelberg, Germany.
Althoff K; Bridge Institute of Experimental Tumor Therapy, West German Cancer Center, University Medicine Essen, Essen, Germany.; Division of Solid Tumor Translational Oncology, German Cancer Research Center (DKFZ) and German Cancer Consortium (DKTK), partner site Essen, Heidelberg, Germany.
Müller MP; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany.
Siveke JT; Bridge Institute of Experimental Tumor Therapy, West German Cancer Center, University Medicine Essen, Essen, Germany.; Division of Solid Tumor Translational Oncology, German Cancer Research Center (DKFZ) and German Cancer Consortium (DKTK), partner site Essen, Heidelberg, Germany.
Rauh D; Faculty of Chemistry and Chemical Biology, TU Dortmund University and Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Dortmund, Germany. .
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Źródło :
Nature communications [Nat Commun] 2021 Sep 06; Vol. 12 (1), pp. 5297. Date of Electronic Publication: 2021 Sep 06.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Antineoplastic Agents/*pharmacology
Lymphocytes/*drug effects
Protein Kinase Inhibitors/*pharmacology
Proto-Oncogene Proteins c-akt/*antagonists & inhibitors
Small Molecule Libraries/*pharmacology
Adaptor Proteins, Signal Transducing/genetics ; Adaptor Proteins, Signal Transducing/metabolism ; Allosteric Regulation ; Allosteric Site ; Animals ; Antineoplastic Agents/chemical synthesis ; Cell Line ; Drug Design ; Gene Expression ; HEK293 Cells ; Humans ; Inhibitory Concentration 50 ; Lymphocytes/cytology ; Lymphocytes/enzymology ; Mice ; Mitogen-Activated Protein Kinase 1/genetics ; Mitogen-Activated Protein Kinase 1/metabolism ; Mitogen-Activated Protein Kinase 3/genetics ; Mitogen-Activated Protein Kinase 3/metabolism ; Protein Kinase Inhibitors/chemical synthesis ; Proto-Oncogene Proteins c-akt/chemistry ; Proto-Oncogene Proteins c-akt/genetics ; Proto-Oncogene Proteins c-akt/metabolism ; Recombinant Proteins/chemistry ; Recombinant Proteins/genetics ; Recombinant Proteins/metabolism ; Sf9 Cells ; Small Molecule Libraries/chemical synthesis ; Spodoptera ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Bifunctional small molecules that mediate the degradation of extracellular proteins.
Autorzy :
Caianiello DF; Department of Chemistry, Yale University, New Haven, CT, USA.
Zhang M; Department of Chemistry, Yale University, New Haven, CT, USA.; Department of Molecular Biophysics and Biochemistry, Yale University, New Haven, CT, USA.
Ray JD; Department of Chemistry, Yale University, New Haven, CT, USA.
Howell RA; Department of Chemistry, Yale University, New Haven, CT, USA.
Swartzel JC; Department of Chemistry, Yale University, New Haven, CT, USA.; Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, CT, USA.
Branham EMJ; Department of Chemistry, Yale University, New Haven, CT, USA.
Chirkin E; Department of Chemistry, Yale University, New Haven, CT, USA.
Sabbasani VR; Department of Chemistry, Yale University, New Haven, CT, USA.
Gong AZ; Department of Chemistry, Yale University, New Haven, CT, USA.
McDonald DM; Department of Chemistry, Yale University, New Haven, CT, USA.
Muthusamy V; Yale Center for Precision Cancer Modeling, Yale University School of Medicine, New Haven, CT, USA.
Spiegel DA; Department of Chemistry, Yale University, New Haven, CT, USA. .
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Źródło :
Nature chemical biology [Nat Chem Biol] 2021 Sep; Vol. 17 (9), pp. 947-953. Date of Electronic Publication: 2021 Aug 19.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Asialoglycoprotein Receptor/*metabolism
Small Molecule Libraries/*pharmacology
Animals ; Dinitrophenols/chemistry ; Dinitrophenols/metabolism ; Hep G2 Cells ; Humans ; Male ; Mice ; Mice, Inbred C57BL ; Molecular Structure ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Exploring the Druggability of Conserved RNA Regulatory Elements in the SARS-CoV-2 Genome.
Autorzy :
Sreeramulu S; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Richter C; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Berg H; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Wirtz Martin MA; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Ceylan B; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Matzel T; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Adam J; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Altincekic N; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Azzaoui K; Saverna Therapeutics, Pumpmattenweg 3, 4105, Biel-Benken, Switzerland.
Bains JK; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Blommers MJJ; Saverna Therapeutics, Pumpmattenweg 3, 4105, Biel-Benken, Switzerland.
Ferner J; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Fürtig B; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Göbel M; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Grün JT; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Hengesbach M; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Hohmann KF; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Hymon D; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Knezic B; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Martins JN; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Mertinkus KR; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Niesteruk A; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Peter SA; Department of Biology, Technical University of Darmstadt, Schnittspahnstr. 10, 64287, Darmstadt, Germany.
Pyper DJ; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Qureshi NS; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.; Present address: EMBL Heidelberg, Meyerhofstr. 1, 69117, Heidelberg, Germany.
Scheffer U; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Schlundt A; Institute for Molecular Biosciences, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Schnieders R; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Stirnal E; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Sudakov A; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Tröster A; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Vögele J; Institute for Molecular Biosciences, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Wacker A; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Weigand JE; Department of Biology, Technical University of Darmstadt, Schnittspahnstr. 10, 64287, Darmstadt, Germany.
Wirmer-Bartoschek J; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Wöhnert J; Institute for Molecular Biosciences, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
Schwalbe H; Institute for Organic Chemistry and Chemical Biology, Center for Biomolecular Magnetic Resonance (BMRZ), Johann Wolfgang Goethe-University, Max-von-Laue-Str. 7+9, 60438, Frankfurt/M., Germany.
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Źródło :
Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2021 Aug 23; Vol. 60 (35), pp. 19191-19200. Date of Electronic Publication: 2021 Aug 03.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Genome*
RNA, Viral/*metabolism
SARS-CoV-2/*genetics
Small Molecule Libraries/*metabolism
Drug Evaluation, Preclinical ; Ligands ; Molecular Structure ; Nucleic Acid Conformation ; Proton Magnetic Resonance Spectroscopy ; RNA, Viral/chemistry ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Therapeutic Approaches Targeting Proteostasis in Kidney Disease and Fibrosis.
Autorzy :
Chen JH; Graduate Institute of Toxicology, College of Medicine, National Taiwan University, Taipei 100233, Taiwan.
Wu CH; Graduate Institute of Toxicology, College of Medicine, National Taiwan University, Taipei 100233, Taiwan.; Department of Physiology of Visceral Function and Body Fluid, Nagasaki University Graduate School of Biomedical Sciences, Nagasaki 852-8523, Japan.
Chiang CK; Graduate Institute of Toxicology, College of Medicine, National Taiwan University, Taipei 100233, Taiwan.; Department of Integrated Diagnostics & Therapeutics, National Taiwan University Hospital, Taipei 100225, Taiwan.; Center for Biotechnology, National Taiwan University, Taipei 10672, Taiwan.
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Źródło :
International journal of molecular sciences [Int J Mol Sci] 2021 Aug 12; Vol. 22 (16). Date of Electronic Publication: 2021 Aug 12.
Typ publikacji :
Journal Article; Review
MeSH Terms :
Proteostasis/*drug effects
Renal Insufficiency, Chronic/*metabolism
Renal Insufficiency, Chronic/*pathology
Small Molecule Libraries/*pharmacology
Endoplasmic Reticulum/metabolism ; Endoplasmic Reticulum Stress ; Fibrosis ; Humans ; Molecular Targeted Therapy ; Renal Insufficiency, Chronic/drug therapy ; Signal Transduction/drug effects ; Small Molecule Libraries/therapeutic use ; Unfolded Protein Response/drug effects
Czasopismo naukowe
Tytuł :
Bioactive recombinant human oncostatin M for NMR-based screening in drug discovery.
Autorzy :
Mass OA; Biomoleculer Research Center, Boise State University, Boise, ID, 83725, USA.
Tuccinardi J; Department of Chemistry and Biochemistry, Boise State University, 1910 University Dr., Boise, ID, 83725, USA.
Woodbury L; Biomoleculer Research Center, Boise State University, Boise, ID, 83725, USA.
Wolf CL; Biomolecular Sciences Graduate Program, Boise State University, Boise, ID, 83725, USA.; Department of Biological Sciences, Boise State University, Boise, ID, 83725, USA.
Grantham B; Biomoleculer Research Center, Boise State University, Boise, ID, 83725, USA.
Holdaway K; Department of Chemistry and Biochemistry, Boise State University, 1910 University Dr., Boise, ID, 83725, USA.
Pu X; Biomoleculer Research Center, Boise State University, Boise, ID, 83725, USA.; Biomolecular Sciences Graduate Program, Boise State University, Boise, ID, 83725, USA.
King MD; Department of Chemistry and Biochemistry, Boise State University, 1910 University Dr., Boise, ID, 83725, USA.; Biomolecular Sciences Graduate Program, Boise State University, Boise, ID, 83725, USA.
Warner DL; Department of Chemistry and Biochemistry, Boise State University, 1910 University Dr., Boise, ID, 83725, USA.; Biomolecular Sciences Graduate Program, Boise State University, Boise, ID, 83725, USA.
Jorcyk CL; Biomolecular Sciences Graduate Program, Boise State University, Boise, ID, 83725, USA.; Department of Biological Sciences, Boise State University, Boise, ID, 83725, USA.
Warner LR; Biomoleculer Research Center, Boise State University, Boise, ID, 83725, USA. .; Department of Chemistry and Biochemistry, Boise State University, 1910 University Dr., Boise, ID, 83725, USA. .; Biomolecular Sciences Graduate Program, Boise State University, Boise, ID, 83725, USA. .
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Źródło :
Scientific reports [Sci Rep] 2021 Aug 10; Vol. 11 (1), pp. 16174. Date of Electronic Publication: 2021 Aug 10.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Drug Discovery/*methods
Oncostatin M/*antagonists & inhibitors
Small Molecule Libraries/*pharmacology
Binding Sites ; Cell Line, Tumor ; Humans ; Magnetic Resonance Spectroscopy/methods ; Molecular Docking Simulation ; Oncostatin M/chemistry ; Oncostatin M/metabolism ; Phosphorylation ; Protein Binding ; STAT3 Transcription Factor/metabolism ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Combining High-Throughput Synthesis and High-Throughput Protein Crystallography for Accelerated Hit Identification.
Autorzy :
Sutanto F; University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713, AV, Groningen, The Netherlands.
Shaabani S; University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713, AV, Groningen, The Netherlands.
Oerlemans R; University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713, AV, Groningen, The Netherlands.
Eris D; Photon Science Division, Paul Scherrer Institute, Switzerland.
Patil P; University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713, AV, Groningen, The Netherlands.
Hadian M; University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713, AV, Groningen, The Netherlands.
Wang M; Photon Science Division, Paul Scherrer Institute, Switzerland.
Sharpe ME; Photon Science Division, Paul Scherrer Institute, Switzerland.
Groves MR; University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713, AV, Groningen, The Netherlands.
Dömling A; University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713, AV, Groningen, The Netherlands.
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Źródło :
Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2021 Aug 09; Vol. 60 (33), pp. 18231-18239. Date of Electronic Publication: 2021 Jul 09.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms :
Coronavirus 3C Proteases/*metabolism
Cysteine Proteinase Inhibitors/*metabolism
Small Molecule Libraries/*metabolism
Acrylamides/chemical synthesis ; Acrylamides/metabolism ; Acrylates/chemical synthesis ; Acrylates/metabolism ; Catalytic Domain ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus 3C Proteases/chemistry ; Crystallography, X-Ray ; Cysteine Proteinase Inhibitors/chemical synthesis ; Drug Discovery ; High-Throughput Screening Assays ; Protein Binding ; SARS-CoV-2/chemistry ; Small Molecule Libraries/chemical synthesis
Czasopismo naukowe
Tytuł :
An update of new small-molecule anticancer drugs approved from 2015 to 2020.
Autorzy :
Liang X; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China. Electronic address: .
Wu P; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Yang Q; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Xie Y; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
He C; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Yin L; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Yin Z; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Yue G; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Zou Y; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Li L; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Song X; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Lv C; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Zhang W; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
Jing B; Natural Medicine Research Center, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, PR China.
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Aug 05; Vol. 220, pp. 113473. Date of Electronic Publication: 2021 Apr 17.
Typ publikacji :
Journal Article; Review
MeSH Terms :
Drug Approval*
Antineoplastic Agents/*pharmacology
Enzyme Inhibitors/*pharmacology
Neoplasms/*drug therapy
Small Molecule Libraries/*pharmacology
Antineoplastic Agents/chemistry ; Enzyme Inhibitors/chemistry ; Humans ; Neoplasms/enzymology ; Small Molecule Libraries/chemistry
Czasopismo naukowe

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