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Hit and lead generation: beyond high-throughput screening

Alanine, Alexander I ; Bleicher, Konrad H ; Böhm, Hans-Joachim ; Müller, Klaus

Nature reviews. Drug discovery, 2003-05, Vol.2 (5), p.369-378 [Periódico revisado por pares]

England: Nature Publishing Group

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  • Título:
    Hit and lead generation: beyond high-throughput screening
  • Autor: Alanine, Alexander I ; Bleicher, Konrad H ; Böhm, Hans-Joachim ; Müller, Klaus
  • Assuntos: Amino Acid Motifs ; Combinatorial Chemistry Techniques ; Drug Design ; Drug Evaluation, Preclinical ; Drugs ; G proteins ; Genomics ; Physiological aspects ; Portfolio management ; Product development ; Proteomics
  • É parte de: Nature reviews. Drug discovery, 2003-05, Vol.2 (5), p.369-378
  • Notas: ObjectType-Article-2
    SourceType-Scholarly Journals-1
    ObjectType-Feature-3
    content type line 23
    ObjectType-Review-1
  • Descrição: The identification of small-molecule modulators of protein function, and the process of transforming these into high-content lead series, are key activities in modern drug discovery. The decisions taken during this process have far-reaching consequences for success later in lead optimization and even more crucially in clinical development. Recently, there has been an increased focus on these activities due to escalating downstream costs resulting from high clinical failure rates. In addition, the vast emerging opportunities from efforts in functional genomics and proteomics demands a departure from the linear process of identification, evaluation and refinement activities towards a more integrated parallel process. This calls for flexible, fast and cost-effective strategies to meet the demands of producing high-content lead series with improved prospects for clinical success.
  • Editor: England: Nature Publishing Group
  • Idioma: Inglês
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