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Nanomolar E-Selectin Antagonists with Prolonged Half-Lives by a Fragment-Based Approach

Autor: Oliver Schwardt, Brian Cutting, Beat Ernst, Katrin Lemme, Said Rabbani, Céline Weckerle, Jonas Egger

Publikováno v: JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Selectins, a family of C-type lectins, play a key role in inflammatory diseases (e.g., asthma and arthritis). However, the only millimolar affinity of sialyl Lewis(x) (sLe(x)), which is the common tetrasaccharide epitope of all physiological selectin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e5b9b5cf9d3f858df90fca3b64ef7a6

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Mapping the fluorophilicity of a hydrophobic pocket: synthesis and biological evaluation of tricyclic thrombin inhibitors directing fluorinated alkyl groups into the p pocket

Autor: Paul Seiler, Eliane Schweizer, Anja Hoffmann-Röder, Jonas Egger, Ulrike Obst-Sander, Björn Wagner, David Banner, François Diederich, Manfred Kansy

Publikováno v: ChemMedChem. 1(11)

In the completion of our fluorine scan of tricyclic inhibitors to map the fluorophilicity/fluorophobicity of the thrombin active site, a series of 11 new ligands featuring alkyl, alkenyl, and fluoroalkyl groups was prepared to explore fluorine effect

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c54750632d903f9fb4a93a067033a54
https://pubmed.ncbi.nlm.nih.gov/17001711

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