- Chemoenzymatic synthesis of triazole-linked glycopeptides
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Triazole-linked glycopeptides are prepared by C-terminal elongation of glycoamino acids with proteinogenic amino acids following a chemical or enzymatic coupling protocol. Two orthogonal routes for a chemoenzymatic strategy were explored, involving a click-reaction before amide bond formation or in reverse order. It was found that enzymatic peptide coupling under the influence of alcalase proceeds cleanly and in high yields, while the resulting dipeptides can be efficiently clicked to acetylene- or azide-containing sugars. Georg Thieme Verlag Stuttgart.
- Groothuys, Stan,Kuijpers, Brian H. M.,Quaedflieg, Peter J. L. M.,Roelen, Harlof C. P. F.,Wiertz, Roel W.,Blaauw, Richard H.,Van Delft, Floris L.,Rutjes, Floris P. J. T.
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- Cu-catalyzed formation of triazole-linked glycoamino acids and application in chemoenzymatic peptide synthesis
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Novel stable triazole-linked glycoamino acids have been prepared, with the heterocyclic moiety being established by efficient Cumediated cycloaddition between the corresponding azido and acetylene moieties. Selected reactions were scaled up and successful
- Kuijpers, Brian H. M.,Groothuys, Stan,Hawner, Christine,Dam, Jeroen Ten,Quaedflieg, Peter J. L. M.,Sehoemaker, Hans E.,Van Delft, Floris L.,Rutjes, Floris P. J. T.
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- Structure-based design and synthesis of triazole-based macrocyclic inhibitors of norovirus protease: Structural, biochemical, spectroscopic, and antiviral studies
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Outbreaks of acute gastroenteritis caused by noroviruses constitute a public health concern worldwide. To date, there are no approved drugs or vaccines for the management and prophylaxis of norovirus infections. A potentially effective strategy for the development of norovirus therapeutics entails the discovery of inhibitors of norovirus 3CL protease, an enzyme essential for noroviral replication. We describe herein the structure-based design of the first class of permeable, triazole-based macrocyclic inhibitors of norovirus 3C-like protease, as well as pertinent X-ray crystallographic, biochemical, spectroscopic, and antiviral studies.
- Weerawarna, Pathum M.,Kim, Yunjeong,Kankanamalage, Anushka C. Galasiti,Damalanka, Vishnu C.,Lushington, Gerald H.,Alliston, Kevin R.,Mehzabeen, Nurjahan,Battaile, Kevin P.,Lovell, Scott,Chang, Kyeong-Ok,Groutas, William C.
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p. 300 - 318
(2016/07/06)
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- Compounds and Compositions as Channel Activating Protease Inhibitors
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The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
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Page/Page column 17-18
(2008/06/13)
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