DRUGS BY DESIGN
DRUGS BY DESIGN
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DOI：
10.1038/scientificamerican1293-92
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发表时间：
1993-12-01
影响因子：
3
通讯作者：
MONTGOMERY, JA
中科院分区：
文献类型：
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作者：
BUGG, CE;CARSON, WM;MONTGOMERY, JA
Charles E.威廉·巴格卡森和John A.蒙哥马利在阿拉巴马州伯明翰合作进行药物设计。布格是伯明翰亚拉巴马大学高分子晶体学中心主任、综合癌症中心副主任和生物化学教授。卡森是高分子晶体学中心计算机图形核心设施的主任。蒙哥马利是BioCryst公司的执行副总裁兼研究总监，该公司致力于基于结构的药物设计，也是南方研究所的杰出科学家。定制药物，中心的多色结构，是嘌呤核苷磷酸化酶（PNP）的高效抑制剂，由蓝色球体表示。这种抑制剂是使用基于结构的药物设计方法开发的，专门用于不紧贴酶的活性位点。它现在正在动物身上进行治疗关节炎的试验，一种密切相关的化合物正在临床试验中作为牛皮癣和一种癌症的治疗方法。
CHARLES E. BUGG, WILLIAM M. CARSON and JOHN A. MONTGOMERY collaborate on drug design in Birmingham, Ala. Bugg is director of the Center for Macromolecular Crystallography, associate director of the Comprehensive Cancer Center and professor of biochemistry at the University of Alabama at Birmingham. Carson is director of the Computer Graphics Core Facility at the Center for Macromolecular Crystallography. Montgomery is executive vice president and director of research at BioCryst, a company devoted to structure-based drug design, and distinguished scientist at the Southern Research Institute.CUSTOM-MADE DRUG, the multicolored structure at the center, is a highly potent inhibitor of the enzyme purine nucleoside phosphorylase (PNP), represented by blue spheres. The inhibitor, developed using the structure-based drug design method, was created specifically to ‘t snugly in the enzymeÃs active site. It is now being tested in animals for the treatment of arthritis, and a closely related compound is in clinical trials as a therapy for psoriasis and for one form of cancer.