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      Opportunities and challenges in developing stearoyl-coenzyme A desaturase-1 inhibitors as novel therapeutics for human disease.

      1 , ,
      Journal of medicinal chemistry

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          Abstract

          This review provides an overview of stearoyl-coenzyme A desaturase-1 (SCD1) as a novel therapeutic target for metabolic disorders and other indications. Target validation is reviewed, and limitations due to incomplete knowledge of the relevant biological systems are described. Assay development, particularly for high throughput screening, and characterization of SCD1 inhibition are summarized. The progress and evolution in medicinal chemistry are discussed, specifically focusing on key attributes of the most advanced SCD1 inhibitors described in the primary literature and in patent applications. This work culminated in numerous companies identifying potent selective inhibitors, some of which progressed to early clinical development. The status of current SCD1 drug discovery programs is reviewed. Challenges are discussed, and potential new directions are indicated.

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          Author and article information

          Journal
          J. Med. Chem.
          Journal of medicinal chemistry
          1520-4804
          0022-2623
          Jun 26 2014
          : 57
          : 12
          Affiliations
          [1 ] Signalchem Lifesciences Corp. , 550-5600 Parkwood Way, Richmond, British Columbia, V6V 2M2, Canada.
          Article
          10.1021/jm401516c
          24295027
          696c0759-2328-42b9-b165-4924f1965056
          History

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