Structure-guided design of a highly selective glycogen synthase kinase-3β inhibitor: a superior neuroprotective pyrazolone showing antimania effects.
作者信息
Chen Wenwen, Gaisina Irina N, Gunosewoyo Hendra, Malekiani Sam A, Hanania Taleen, Kozikowski Alan P
机构信息
Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood St., Chicago, Illinois 60612, USA.
出版信息
ChemMedChem. 2011 Sep 5;6(9):1587-92. doi: 10.1002/cmdc.201100231. Epub 2011 Jul 12.
Abstract
摘要
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本文引用的文献
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Identification of a glycogen synthase kinase-3β inhibitor that attenuates hyperactivity in CLOCK mutant mice.鉴定一种糖原合酶激酶-3β抑制剂，该抑制剂可减轻 CLOCK 突变小鼠的过度活动。
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2
GSK3beta: role in therapeutic landscape and development of modulators.GSK3β：在治疗领域的作用和调节剂的开发。
Br J Pharmacol. 2010 May;160(1):1-19. doi: 10.1111/j.1476-5381.2010.00661.x. Epub 2010 Mar 19.
3
Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3beta inhibitors.运用分子建模、对接和 3D-QSAR 研究，确定苯并呋喃-3-基-（吲哚-3-基）马来酰亚胺作为 GSK-3β抑制剂的结合模式。
J Mol Model. 2009 Dec;15(12):1463-79. doi: 10.1007/s00894-009-0498-x. Epub 2009 May 14.
4
GSK-3 inhibitors: a ray of hope for the treatment of Alzheimer's disease?糖原合成酶激酶-3抑制剂：治疗阿尔茨海默病的一线希望？
J Alzheimers Dis. 2008 Oct;15(2):181-91. doi: 10.3233/jad-2008-15204.
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Highly potent and specific GSK-3beta inhibitors that block tau phosphorylation and decrease alpha-synuclein protein expression in a cellular model of Parkinson's disease.在帕金森病细胞模型中具有高度效力且特异性的糖原合成酶激酶-3β（GSK-3β）抑制剂，其可阻断tau蛋白磷酸化并降低α-突触核蛋白的表达。
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GSK-3alpha regulates production of Alzheimer's disease amyloid-beta peptides.糖原合成酶激酶-3α调节阿尔茨海默病β淀粉样肽的产生。
Nature. 2003 May 22;423(6938):435-9. doi: 10.1038/nature01640.
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