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1. 发明授权

US5104858A Sensitizing multidrug resistant cells to antitumor agents 失效
标题翻译：敏感细胞耐药细胞
公开(公告)号：US5104858A
公开(公告)日：1992-04-14
申请号：US250891
申请日：1988-09-29
申请人： William N. Hait , James M. Ford
发明人： William N. Hait , James M. Ford
IPC分类号： C07D335/20 , A61K31/00 , A61K31/38 , A61K31/445 , A61K31/495 , A61P31/04
CPC分类号： A61K31/38 , A61K31/445 , A61K31/495
摘要： A method for sensitizing multidrug resistant cells to antitumor agents comprosing contacting multidrug resistant cells, with an effective amount of a compound of the formula ##STR1## wherein n is 1, 2 or 3, X is CF.sub.3, --O--CH.sub.3, Br, I, Cl, H, W and S--CH.sub.3 and R.sup.1 and R.sup.2, independently of each other are --CH.sub.3 --CH.sub.2 --CH.sub.3, CH.sub.2 CH.sub.2 OHCH.sub.2 OH, or NR.sup.1 R.sup.2 form a ring ##STR2## wherein R.sup.3 is --CH.sub.3, CH.sub.2 --CH.sub.3, --H, CH.sub.2 OH and CH.sub.2 CH.sub.2 OH.

2. 发明授权

US5386019A Synthesis of inhibitors of calmodulin-mediated enzymes including KS-501, KS-502 and their enantiomers 失效
标题翻译：钙调蛋白介导的酶抑制剂的合成，包括KS-501，KS-502及其对映异构体
公开(公告)号：US5386019A
公开(公告)日：1995-01-31
申请号：US821719
申请日：1992-01-15
申请人： Samuel J. Danishefsky , Russell Dushin , William N. Hait
发明人： Samuel J. Danishefsky , Russell Dushin , William N. Hait
IPC分类号： C07H15/203 , C07H1/00 , C07H13/02
CPC分类号： C07H15/203
摘要： The total synthesis of a group of compounds with inhibitory effects on calmodulin-mediated enzyme activities has been accomplished. Among these synthesized compounds are KS-501 and KS-502. Other compounds that have been synthesized by the described scheme are ent-KS-501 and ent-KS-502 which are enantiomers of KS-501 and KS-502 and which also have inhibitory effects on calmodulin-mediated enzyme activities.
摘要翻译：已经完成了对钙调蛋白介导的酶活性具有抑制作用的一组化合物的总合成。其中合成的化合物有KS-501和KS-502。通过所述方案合成的其它化合物是KS-501和KS-502的对映体的ent-KS-501和ent-KS-502，其也对钙调蛋白介导的酶活性具有抑制作用。

3. 发明授权

US06346406B1 Elongation factor-2 kinase (EF-2 kinase), and methods of use therefor 失效
标题翻译：伸长因子-2激酶（EF-2激酶）及其使用方法
公开(公告)号：US06346406B1
公开(公告)日：2002-02-12
申请号：US08914999
申请日：1997-08-20
申请人： Alexey G. Ryazanov , William N. Hait , Karen S. Pavur
发明人： Alexey G. Ryazanov , William N. Hait , Karen S. Pavur
IPC分类号： C12N912
CPC分类号： C12N9/1205 , A61K38/00
摘要： A new superfamily of protein kinases has been discovered that centers around eukaryotic elongation factor-2 kinase (eEF-2 kinase). The protein kinases of this new superfamily have the following characteristics: 1) sequence similarity to eEF-2 kinase; 2) no sequence similarity to the protein kinases of either the serine/threonine/tyrosine kinase or histidine kinase superfamily; and, 3) specifically phosphorylates &agr;-helical regions of proteins as opposed to &bgr;-turns, as seen in all other protein kinases. Assays have been developed utilizing eEF-2 kinase and a phosphorylation target consisting of a novel &agr;-helical 16-amino acid peptide sequence to facilitate high-throughput screening for compounds that can specifically inhibit this protein kinase that has been implicated tumor growth and other hyperproliferitive disorders. Additionally, the disclosed invention includes assessing eEF-2 kinase levels for diagnostic purposes, and therapeutic formulations to inhibit eEF-2 kinase activity.
摘要翻译：已经发现了一种新的超家族蛋白激酶，其以真核延伸因子2激酶（eEF-2激酶）为中心。该新型超家族的蛋白激酶具有以下特征：1）与eEF-2激酶的序列相似性; 2）与丝氨酸/苏氨酸/酪氨酸激酶或组氨酸激酶超家族的蛋白激酶没有序列相似性; 和3）特异性地磷酸化与β-匝相反的蛋白质的α-螺旋区域，如在所有其它蛋白激酶中所见。已经开发了使用eEF-2激酶和由新型α-螺旋16-氨基酸肽序列组成的磷酸化靶标的测定，以促进可以特异性抑制该蛋白激酶的化合物的高通量筛选，所述化合物已经涉及肿瘤生长和其它过度增生疾病另外，所公开的发明包括评估用于诊断目的的eEF-2激酶水平和抑制eEF-2激酶活性的治疗制剂。

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