Zobrazeno 1 - 10 of 16 pro vyhledávání: '"Bodo Scheiper"'
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Akademický článek
High-resolution cryo-EM of the human CDK-activating kinase for structure-based drug design
Autor: Victoria I. Cushing, Adrian F. Koh, Junjie Feng, Kaste Jurgaityte, Alexander Bondke, Sebastian H. B. Kroll, Marion Barbazanges, Bodo Scheiper, Ash K. Bahl, Anthony G. M. Barrett, Simak Ali, Abhay Kotecha, Basil J. Greber
Publikováno v: Nature Communications, Vol 15, Iss 1, Pp 1-17 (2024)
Abstract Rational design of next-generation therapeutics can be facilitated by high-resolution structures of drug targets bound to small-molecule inhibitors. However, application of structure-based methods to macromolecules refractory to crystallizat
Externí odkaz: https://doaj.org/article/a393bf7c13c14f7a93881e19f56dabfa
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5
Nanomolar inhibitors of Mycobacterium tuberculosis glutamine synthetase 1: Synthesis, biological evaluation and X-ray crystallographic studies
Autor: Bodo Scheiper, Bernard Pessegue, Axel Ganzhorn, Christoph Pöverlein, Cédric Couturier, Sandra Silve, Eric Bacqué, Armin Bauer, Anil Nair, Renaud Morales, Sylvie Llopart, Sophie Lagrange
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:1455-1459
A series of imidazo[1,2-a]indeno[1,2-e]pyrazin-4-ones that potently inhibit M. tuberculosis glutamine synthetase (GlnA1) has been identified by high throughput screening. Exploration of this series was performed owing to a short chemistry program. De
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ae9b3cfa07ea339bf3443a7b1877766
https://doi.org/10.1016/j.bmcl.2015.02.035
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Identification and optimization of a new series of anti-tubercular quinazolinones
Autor: Jerome Menegotto, Cédric Couturier, Anna M. Upton, Christine Lair, Eric Bacqué, Sophie Lagrange, Armin Bauer, Takushi Kaneko, Bodo Scheiper, Eric Cogo, Corinne Perron, Alain Pellet
Publikováno v: Bioorganicmedicinal chemistry letters. 26(21)
A high throughput phenotypic screening against Mycobacterium smegmatis led us to the discovery of a new class of bacteriostatic, highly hydrophobic antitubercular quinazolinones that potently inhibited the in vitro growth of either extracellular or i
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3d4519b2b8393fea7d0a03d992486fa
https://pubmed.ncbi.nlm.nih.gov/27671498
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7
Synthesis-driven mapping of the dictyodendrin alkaloids
Autor: Jörg Rust, Mathias M. Domostoj, Bodo Scheiper, Alois Fürstner, Richard Mynott, Philipp Buchgraber, Cornelia Wirtz
Publikováno v: Tetrahedron. 65:6519-6534
The dictyodendrin alkaloids have been described as the first telomerase inhibitors of marine origin. As such they represent interesting lead compounds in the quest for small molecule inhibitors of this tumor-marker enzyme. Described herein is the pre
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::50ee0918ceb4a7c6ec8dd12f88bd45c4
https://doi.org/10.1016/j.tet.2009.06.058
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The Development of a Selective Cyclin-Dependent Kinase Inhibitor That Shows Antitumor Activity
Autor: Anthony G. M. Barrett, R. Charles Coombes, Seshu K. Kanneganti, Ashutosh S. Jogalekar, Jan Brackow, Manikandan Periyasamy, Matthew J. Fuchter, James P. Snyder, Eric O. Aboagye, Dean A. Heathcote, Alekasandra Siwicka, Simak Ali, Hetal Patel, Bodo Scheiper, Robert S. Tolhurst, Dennis C. Liotta, Sebastian H. B. Kroll
Publikováno v: Cancer Research. 69:6208-6215
Normal progression through the cell cycle requires the sequential action of cyclin-dependent kinases CDK1, CDK2, CDK4, and CDK6. Direct or indirect deregulation of CDK activity is a feature of almost all cancers and has led to the development of CDK
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3193fb5fe413189c0e6e9d588fa1fcff
https://doi.org/10.1158/0008-5472.can-09-0301
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9
Total Syntheses of the Telomerase Inhibitors Dictyodendrin B, C, and E
Autor: Bodo Scheiper, Alois Fürstner, Mathias M. Domostoj
Publikováno v: Journal of the American Chemical Society. 128:8087-8094
Concise and flexible total syntheses of the pyrrolo[2,3-c]carbazole alkaloids dictyodendrin B (2), C (3), and E (5) are described. These polycyclic telomerase inhibitors of marine origin derive from the common intermediate 18 which was prepared on a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f5b2e1bbdf32185667ed7b95ad6cc0e
https://doi.org/10.1021/ja0617800
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10
Catalysis-based enantioselective total synthesis of the macrocyclic spermidine alkaloid isooncinotine
Autor: Alois Fürstner, Bodo Scheiper, Frank Glorius, Andreas Leitner
Publikováno v: Proceedings of the National Academy of Sciences. 101:11960-11965
A concise and efficient total synthesis of the spermidine alkaloid (-)-isooncinotine ( 1 ) incorporating a 22-membered lactam ring is outlined. The approach is largely catalysis-based, involving a selective iron-catalyzed alkyl–aryl cross-coupling
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c421f7e174a65ad830c1bd3f470d9eab
https://doi.org/10.1073/pnas.0401322101
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