Výsledky vyhledávání - "Daniel B. Stein"

Discovery of Novel UDP-N-Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against Pseudomonas aeruginosa

Publikováno v: Journal of Medicinal Chemistry. 64:14377-14425

This study describes a novel series of UDP-N-acetylglucosamine acyltransferase (LpxA) inhibitors that was identified through affinity-mediated selection from a DNA-encoded compound library. The original hit was a selective inhibitor of Pseudomonas ae

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::561a3ec469b1a8704e6a0431f9d286c1
https://doi.org/10.1021/acs.jmedchem.1c00888

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Discovery of Novel UDP

Publikováno v: Journal of medicinal chemistry. 64(19)

This study describes a novel series of UDP

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::a1d1f373433e8f065b03c7c212d95e83
https://pubmed.ncbi.nlm.nih.gov/34569791

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Characterization ofHelicobacter pyloriα1,2-Fucosyltransferase for Enzymatic Synthesis of Tumor-Associated Antigens

Autor: Chun-Hung Lin, Daniel B. Stein, Yu-Nong Lin

Publikováno v: Advanced Synthesis & Catalysis. 350:2313-2321

The a1,2-fucosyltransferase (a1,2-FucT) from Helicobacter pylori catalyzes the fucosylation of acceptor oligosaccharides at the C2-OH of termi- nal Galb units. The enzyme from strain NCTC11639 was evaluated for its ability to synthesize cancer-as- so

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d8f2cdfb36625ee9f91b2ed10355c8ee
https://doi.org/10.1002/adsc.200800435

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Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo

Publikováno v: Journal of medicinal chemistry. 58(9)

The medicinal chemistry community has directed considerable efforts toward the discovery of selective inhibitors of interleukin-2 inducible T-cell kinase (ITK), given its role in T-cell signaling downstream of the T-cell receptor (TCR) and the implic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af042a664b1539fc20b020da84768b01
https://pubmed.ncbi.nlm.nih.gov/25844760

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Impact of Epimerization Domains on the Intermodular Transfer of Enzyme-Bound Intermediates in Nonribosomal Peptide Synthesis

Autor: Daniel B. Stein, Uwe Linne, Mohamed A. Marahiel, Martin Hahn

Publikováno v: ChemBioChem. 7:1807-1814

Assembly of bioactive natural compounds through the action of nonribosomal peptide synthetases (NRPSs) relies on the specific interplay of modules and domains along these multiple mega-enzymes. As the C termini of several bacterial NRPSs often harbor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a62ba57762fea73998020f5f580b7f4
https://doi.org/10.1002/cbic.200600192

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Systematic and Quantitative Analysis of Protein−Protein Recognition between Nonribosomal Peptide Synthetases Investigated in the Tyrocidine Biosynthetic Template

Autor: Daniel B. Stein, Henning D. Mootz, Mohamed A. Marahiel, Uwe Linne

Publikováno v: Biochemistry. 42:5114-5124

We present a systematic and quantitative study of the protein-protein recognition between the three tyrocidine synthetases TycA, TycB, and TycC investigated with two artificial in trans assay systems, which had been previously developed: the "DKP ass

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::507bab72e0f6f50879af07463d954f21
https://doi.org/10.1021/bi034223o

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Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors

Publikováno v: Journal of medicinal chemistry. 57(13)

Interleukin-2 inducible T-cell kinase (ITK), a member of the Tec family of tyrosine kinases, plays a major role in T-cell signaling downstream of the T-cell receptor (TCR), and considerable efforts have been directed toward discovery of ITK-selective

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a977380e3e3a29fa5a4d154bf43b1fe0
https://pubmed.ncbi.nlm.nih.gov/24918870

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Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK)

Publikováno v: Bioorganicmedicinal chemistry letters. 23(23)

Inhibition of the non-receptor tyrosine kinase ITK, a component of the T-cell receptor signalling cascade, may represent a novel treatment for allergic asthma. Here we report the structure-based optimization of a series of benzothiazole amides that d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3ce5fa1fa07a46ec7e74d4dcbfb227a0
https://pubmed.ncbi.nlm.nih.gov/24138940

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Utility of epimerization domains for the redesign of nonribosomal peptide synthetases

Autor: Uwe Linne, Mohamed A. Marahiel, Daniel B. Stein

Publikováno v: The FEBS journal. 272(17)

Many pharmacologically important agents are assembled on multimodular nonribosomal peptide synthetases (NRPSs) whose modules comprise a set of core domains with all essential catalytic functions necessary for the incorporation and modification of one

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfd242f82a60e9d8fef9eb1c0d09e051
https://pubmed.ncbi.nlm.nih.gov/16128819

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