Free-Wilson and Structural Approaches to Co-optimising Human and Rodent Isoform Potency for 11b-Hydroxysteroid Dehydrogenase Type 1 11b-HSD1 Inhibitors

Free-Wilson and Structural Approaches to Co-optimising Human and Rodent Isoform Potency for 11b-Hydroxysteroid Dehydrogenase Type 1 11b-HSD1 Inhibitors Descriptor: 4-cyclopentyl-N-[(1S,3R)-5-oxidanyl-2-adamantyl]-2-[[(3S)-oxolan-3-yl]amino]pyrimidine-5-carboxamide, CORTICOSTEROID 11-BETA-DEHYDROGENASE ISOZYME 1, NADP NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE Authors: Goldberg, F.W, Leach, A.G, Scott, J.S, Snelson, W.L, Groombridge, S.D, Donald, C.S, Bennett, S.N.L, Bodin, C, Morentin Gutierrez, P, Gyte, A.C. Deposit date: 2012-09-20 Release date: 2012-11-28 Last modified: 2024-05-08 Method: X-RAY DIFFRACTION (2.2 Å) Cite: Free-Wilson and Structural Approaches to Co-Optimising Human and Rodent Isoform Potency for 11Beta-Hydroxysteroid Dehydrogenase Type 1 (11Beta-Hsd1) Inhibitors J.Med.Chem., 55, 2012

针对11β-羟类固醇脱氢酶1型（11β-HSD1, 11b-Hydroxysteroid Dehydrogenase Type 1）抑制剂的人源与啮齿类同工酶效力协同优化的Free-Wilson法与结构生物学方法
描述符：4-环戊基-N-[(1S,3R)-5-羟基-2-金刚烷基]-2-[[(3S)-四氢呋喃-3-基]氨基]嘧啶-5-甲酰胺、皮质类固醇11β-脱氢酶同工酶1、烟酰胺腺嘌呤二核苷酸磷酸（NADP, Nicotinamide-Adenine-Dinucleotide Phosphate）
作者：Goldberg, F.W、Leach, A.G、Scott, J.S、Snelson, W.L、Groombridge, S.D、Donald, C.S、Bennett, S.N.L、Bodin, C、Morentin Gutierrez, P、Gyte, A.C.
存入日期：2012年9月20日
发布日期：2012年11月28日
最后修改日期：2024年5月8日
测试方法：X射线衍射（分辨率2.2 Å）
引用文献：《Free-Wilson and Structural Approaches to Co-Optimising Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors》，发表于《药物化学杂志》（Journal of Medicinal Chemistry，缩写：J.Med.Chem.），2012年，第55卷。