肌醇磷脂依赖的细胞信号:药物发现的机会。

Drug design and delivery Pub Date : 1990-05-01
R C Young, C P Downes
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引用次数: 0

摘要

在这篇综述中,对磷酸肌苷代谢进行了讨论,并确定了潜在的治疗干预位点。肌醇化学的几个分支最近取得了快速进展,这极大地提高了我们对识别途径中涉及的各种关键酶和d -肌醇1,4,5-三磷酸生理受体的结构要求的认识。根据现有的线索,药物机会出现在减少极性,利用极性前药,以及开发创新的细胞内递送系统。有可能为未来的探索发现新的药效团。
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Inositol phospholipid-dependent cellular signalling: opportunities for drug discovery.

In this review, phosphoinositide metabolism is discussed and potential sites for therapeutic intervention are identified. The rapid recent progress in several branches of inositol chemistry has greatly improved our knowledge of the structural requirements for recognition by a variety of key enzymes involved in the pathways, and by the physiological receptor for D-myo-inositol 1,4,5-trisphosphate. Based on existing leads, drug opportunities arise in reducing polarity, in the utilisation of apolar pro-drugs, and in the development of innovative intracellular delivery systems. The identification of novel pharmacophores for future exploration is likely.

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