非肽类亲环蛋白配体的合成与生物学评价
Synthesis and biological evaluation of non-peptidic cyclophilin ligands.
作者信息
Wu Yong-Qian, Belyakov Sergei, Choi Chi, Limburg David, Thomas IV Bert E, Vaal Mark, Wei Ling, Wilkinson Douglas E, Holmes Agnes, Fuller Mike, McCormick Jocelyn, Connolly Maureen, Moeller Tim, Steiner Joseph, Hamilton Gregory S
机构信息
Department of Research, Guilford Pharmaceuticals, Inc., 6611 Tributary Street, Baltimore, Maryland 21224, USA.
出版信息
J Med Chem. 2003 Mar 27;46(7):1112-5. doi: 10.1021/jm020409u.
Peptidylprolyl isomerase cyclophilins play critical roles in a variety of biological processes. Recent findings that cyclophilins are present at high levels in the CNS and that cyclosporin A may possess neuroprotective/neurotrophic effects have prompted us to search for nonimmunosuppressant small molecule cyclophilin ligands. To this end, we report the lead identification through "virtual screening" and the synthesis of our first series of non-peptidic cyclophilin ligands, along with the preliminary biological results.
肽基脯氨酰异构酶亲环蛋白在多种生物学过程中发挥关键作用。最近的研究发现亲环蛋白在中枢神经系统中高水平存在，并且环孢菌素A可能具有神经保护/神经营养作用，这促使我们寻找非免疫抑制性的小分子亲环蛋白配体。为此，我们报告了通过“虚拟筛选”进行的先导物鉴定以及我们的首个非肽类亲环蛋白配体系列的合成，以及初步的生物学结果。
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