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  • combinatorial chemistry  (2)
  • Kinase  (1)
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  • 1
    Digitale Medien
    Digitale Medien
    Springer
    Molecular diversity 4 (1998), S. 233-256 
    ISSN: 1573-501X
    Schlagwort(e): combinatorial chemistry ; heterocycle ; scaffold ; solid-phase synthesis ; solution-phase synthesis
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie
    Materialart: Digitale Medien
    Standort Signatur Erwartet Verfügbarkeit
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  • 2
    ISSN: 1573-501X
    Schlagwort(e): agonist ; antagonist ; antiinfective ; combinatorial chemistry ; enzyme ; inhibitor ; kinase ; protease ; receptor
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie
    Notizen: Abstract This review is a historical accounting of chemical libraries from which biologically active agents have been obtained. The comprehensive tabulation includes citations as early as 1992, when the first descriptions of biologically active libraries were disclosed, and continues through 1997. Four tables are provided listing libraries screened against (1) proteolytic enzymes, (2) non-proteolytic enzymes, (3) G-protein coupled receptors (GPCRs), and (4) other targets not classified in the first three tables (e.g., non-GPCRs, integrins, antiinfectives). A name, generic structure, and size is provided for each library citation, accompanied by the molecular screen and the structure and potency of the most active library member. In total, 86 libraries are presented with 60% of the contributions reported from pharmaceutical and biotechnology companies. Approximately 70% of the libraries have used α-amino acid synthons in their construction and 85% of the libraries include one or more amide bonds.
    Materialart: Digitale Medien
    Standort Signatur Erwartet Verfügbarkeit
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  • 3
    Digitale Medien
    Digitale Medien
    Springer
    Molecular diversity 2 (1997), S. 223-236 
    ISSN: 1573-501X
    Schlagwort(e): Combinatorial chemistry ; Enzyme ; Inhibitor ; Protease ; Kinase
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie
    Notizen: Summary This review serves to highlight the recent examples of combinatoric methodology as applied to the discovery and optimization of enzyme inhibitors. Early research efforts focused on the identification of polypeptides from libraries as inhibitors of proteases. As solution- and solid-phase chemistries gain in sophistication, libraries containing less peptidic structural motifs have been created. A recurring design stratagem relies on the synthesis of libraries incorporating pharmacophores with known affinity for the target enzyme. Screening of these structure-based libraries has led to the discovery of small-molecule inhibitors of both proteolytic and non-proteolytic enzymes alike. Two tables are provided listing the enzyme targeted libraries through 1996. A name, generic structure and size is given for each library citation, accompanied by the enzyme screen and the structure and potency of the most active library member.
    Materialart: Digitale Medien
    Standort Signatur Erwartet Verfügbarkeit
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