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公开(公告)号：US07378432B2
公开(公告)日：2008-05-27
申请号：US11280209
申请日：2005-11-17
Applicant: Hagit Eldar-Finkelman , Moshe Portnoy
Inventor： Hagit Eldar-Finkelman , Moshe Portnoy
IPC: A01N43/64 , C07D249/04
CPC classification number: C07F9/094 , A61K38/00 , C07F9/6518 , C07K7/06 , C07K14/4703 , C07K14/4705 , C07K2299/00 , C12N9/1205
Abstract: Novel compounds designed to allow interactions with binding sites of GSK-3 and hence are capable of inhibiting GSK-3 activity, via inhibition of substrate binding are disclosed. Further disclosed are pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions.
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公开(公告)号：US06780625B2
公开(公告)日：2004-08-24
申请号：US09951902
申请日：2001-09-14
Applicant: Hagit Eldar-Finkelman
Inventor： Hagit Eldar-Finkelman
IPC: C07K706
CPC classification number: C07K7/06 , A61K38/55 , C07K14/4703 , C07K14/4705 , C07K2299/00 , C12N9/1205
Abstract: Peptide inhibitors of glycogen synthase kinase-3 (GSK-3) have an amino acid sequence motif of XZXXXS(p)X, wherein S(p)=phosphorylated serine or phosphorylated threonine, X=any amino acid, and Z=any amino acid except serine or threonine. These inhibitors, which are about 7 to 50 amino acids long, are specific for GSK-3 and strongly inhibit the enzyme with an IC50 of about 150 &mgr;M. Also provided are methods of treating biological conditions mediated by GSK-3 activity, such as potentiating insulin signaling in a subject, treating or preventing type 2 diabetes in a patient, and treating Alzheimer's Disease by administering peptide inhibitors. Compositions of these peptide inhibitors and pharmaceutically acceptable carriers are also provided, as is a method for identifying inhibitors of GSK-3. The invention further relates to a computer-assisted method of structure based drug design of GSK-3 inhibitors using a three-dimensional structure of a peptide substrate of GSK-3.
Abstract translation: 糖原合成酶激酶-3（GSK-3）的肽抑制剂具有XZXXXS（p）X的氨基酸序列基序，其中S（p）=磷酸化丝氨酸或磷酸化苏氨酸，X =任何氨基酸，Z =任何氨基酸 丝氨酸或苏氨酸除外。 大约7至50个氨基酸长度的这些抑制剂对GSK-3是特异性的，并以约150μM的IC 50强烈抑制酶。 还提供了治疗由GSK-3活性介导的生物学条件的方法，例如在受试者中增强胰岛素信号，治疗或预防患者中的2型糖尿病，并通过施用肽抑制剂治疗阿尔茨海默氏病。 还提供了这些肽抑制剂和药学上可接受的载体的组合物，以及鉴定GSK-3抑制剂的方法。 本发明还涉及使用GSK-3的肽底物的三维结构的GSK-3抑制剂的基于结构的药物设计的计算机辅助方法。
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公开(公告)号：US09688719B2
公开(公告)日：2017-06-27
申请号：US13982300
申请日：2012-01-26
Applicant: Hagit Eldar-Finkelman , Miriam Eisenstein
Inventor： Hagit Eldar-Finkelman , Miriam Eisenstein
CPC classification number: C07K2/00 , A61K38/00 , C07K7/06 , C07K7/08 , C12N9/1205 , C12Y207/01037 , Y02A50/414
Abstract: Novel peptide inhibitors of GSK-3, compositions containing same and uses thereof are disclosed. The novel peptide inhibitors are substrate-competitive inhibitors and have an amino acid sequence designed so as to bind to a defined binding site subunit in GSK-3.
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公开(公告)号：US20090062180A1
公开(公告)日：2009-03-05
申请号：US12155087
申请日：2008-05-29
Applicant: Hagit Eldar-Finkelman
Inventor： Hagit Eldar-Finkelman
IPC: A61K38/28 , C07K7/06 , C07K7/08 , C12N5/00 , A61K38/10 , A61P3/10 , A61P25/00 , A61P3/04 , C07K1/107 , C12N9/99 , A61K38/08
Abstract: Novel conjugates that are capable of inhibiting GSK-3 activity, a process of producing same, pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions are disclosed. Methods of treating affective disorders using GSK-3 inhibitors are further disclosed.
Abstract translation: 公开了能够抑制GSK-3活性的新型缀合物，其制备方法，包含其的药物组合物和其在治疗GSK-3介导的病症中的应用方法。 进一步公开了使用GSK-3抑制剂治疗情感障碍的方法。
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公开(公告)号：US20070072791A1
公开(公告)日：2007-03-29
申请号：US11602406
申请日：2006-11-21
Applicant: Hagit Eldar-Finkelman
Inventor： Hagit Eldar-Finkelman
CPC classification number: C07K7/06 , A61K38/55 , C07K14/4703 , C07K14/4705 , C07K2299/00 , C12N9/1205
Abstract: Peptide inhibitors of glycogen synthase kinase-3 (GSK-3) having an amino acid sequence motif of XZXXXS(p)X, wherein S(p)=phosphorylated serine or phosphorylated threonine, X=any amino acid, and Z=any amino acid except serine or threonine. These inhibitors, which are about 7 to 20 amino acids long, are specific for GSK-3 and strongly inhibit the enzyme with an IC50 of about 150 μM. Also provided are methods of treating biological conditions mediated by GSK-3 activity, such as potentiating insulin signaling in a subject, treating or preventing type 2 diabetes in a patient, and treating Alzheimer's Disease by administering peptide inhibitors. Compositions of these peptide inhibitors and pharmaceutically acceptable carriers are also provided, as is a method for identifying inhibitors of GSK-3. The invention further relates to a computer-assisted method of structure based drug design of GSK-3 inhibitors using a three-dimensional structure of a peptide substrate of GSK-3.
Abstract translation: 具有XZXXXS（p）X的氨基酸序列基序的糖原合成酶激酶-3（GSK-3）的肽抑制剂，其中S（p）=磷酸化丝氨酸或磷酸化苏氨酸，X =任何氨基酸，Z =任何氨基酸 丝氨酸或苏氨酸除外。 大约7至20个氨基酸长度的这些抑制剂对GSK-3是特异性的，并且强烈地抑制具有大约150μM的IC 50的酶。 还提供了治疗由GSK-3活性介导的生物学条件的方法，例如在受试者中增强胰岛素信号，治疗或预防患者中的2型糖尿病，并通过施用肽抑制剂治疗阿尔茨海默氏病。 还提供了这些肽抑制剂和药学上可接受的载体的组合物，以及鉴定GSK-3抑制剂的方法。 本发明还涉及使用GSK-3的肽底物的三维结构的GSK-3抑制剂的基于结构的药物设计的计算机辅助方法。
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Patent Agency Ranking
公开(公告)号：US09243034B2
公开(公告)日：2016-01-26
申请号：US13981668
申请日：2012-01-26
Applicant: Hagit Eldar-Finkelman , Avital Licht-Murava , Batya Plotkin
Inventor： Hagit Eldar-Finkelman , Avital Licht-Murava , Batya Plotkin
CPC classification number: C07K7/08 , A61K38/00 , A61K38/08 , A61K38/10 , C07K7/06 , C12N9/12 , C12N9/1205 , C12Q1/485 , C12Y207/11001 , C40B30/02 , G01N33/573 , G01N2333/912 , G01N2440/14 , G01N2500/04 , G01N2500/10
Abstract: Novel peptide inhibitors of GSK-3, compositions containing same and uses thereof are disclosed. The novel peptide inhibitors are substrate-competitive inhibitors and have an amino acid sequence designed so as to bind to a defined binding site subunit in GSK-3. Also disclosed are GSK-3 substrate competitive inhibitors which bind to the defined binding site subunit in the enzyme. Also disclosed are mutants of GSK-3 and uses thereof for identifying a putative GSK-3 substrate competitive inhibitor.
Abstract translation: 公开了GSK-3的新型肽抑制剂，含有其的组合物及其用途。 新型肽抑制剂是底物竞争性抑制剂，并且具有设计成与GSK-3中规定的结合位点亚基结合的氨基酸序列。 还公开了结合酶中限定的结合位点亚基的GSK-3底物竞争性抑制剂。 还公开了GSK-3的突变体及其用于鉴定推定的GSK-3底物竞争性抑制剂的用途。
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公开(公告)号：US08088941B2
公开(公告)日：2012-01-03
申请号：US12149336
申请日：2008-04-30
Applicant: Hagit Eldar-Finkelman , Moshe Portnoy
Inventor： Hagit Eldar-Finkelman , Moshe Portnoy
IPC: C07F9/02 , A61K31/155
CPC classification number: C07F9/094 , A61K38/00 , C07F9/6518 , C07K7/06 , C07K14/4703 , C07K14/4705 , C07K2299/00 , C12N9/1205
Abstract: Novel compounds designed to allow interactions with binding sites of GSK-3 and hence are capable of inhibiting GSK-3 activity, via inhibition of substrate binding are disclosed. Further disclosed are pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions.
Abstract translation: 公开了旨在允许与GSK-3的结合位点相互作用并因此通过抑制底物结合而抑制GSK-3活性的新型化合物。 进一步公开的是包含其的药物组合物和在治疗GSK-3介导的病症中使用它们的方法。
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公开(公告)号：US07833974B2
公开(公告)日：2010-11-16
申请号：US12155087
申请日：2008-05-29
Applicant: Hagit Eldar-Finkelman
Inventor： Hagit Eldar-Finkelman
Abstract: Novel conjugates that are capable of inhibiting GSK-3 activity, a process of producing same, pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions are disclosed. Methods of treating affective disorders using GSK-3 inhibitors are further disclosed.
Abstract translation: 公开了能够抑制GSK-3活性的新型缀合物，其制备方法，包含其的药物组合物和其在治疗GSK-3介导的病症中的应用方法。 进一步公开了使用GSK-3抑制剂治疗情感障碍的方法。
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公开(公告)号：US20130310303A1
公开(公告)日：2013-11-21
申请号：US13981668
申请日：2012-01-26
Applicant: Hagit Eldar-Finkelman , Avital Licht-Murava , Batya Plotkin
Inventor： Hagit Eldar-Finkelman , Avital Licht-Murava , Batya Plotkin
CPC classification number: C07K7/08 , A61K38/00 , A61K38/08 , A61K38/10 , C07K7/06 , C12N9/12 , C12N9/1205 , C12Q1/485 , C12Y207/11001 , C40B30/02 , G01N33/573 , G01N2333/912 , G01N2440/14 , G01N2500/04 , G01N2500/10
Abstract: Novel peptide inhibitors of GSK-3, compositions containing same and uses thereof are disclosed. The novel peptide inhibitors are substrate-competitive inhibitors and have an amino acid sequence designed so as to bind to a defined binding site subunit in GSK-3. Also disclosed are GSK-3 substrate competitive inhibitors which bind to the defined binding site subunit in the enzyme. Also disclosed are mutants of GSK-3 and uses thereof for identifying a putative GSK-3 substrate competitive inhibitor.
Abstract translation: 公开了GSK-3的新型肽抑制剂，含有其的组合物及其用途。 新型肽抑制剂是底物竞争性抑制剂，并且具有设计成与GSK-3中规定的结合位点亚基结合的氨基酸序列。 还公开了结合酶中限定的结合位点亚基的GSK-3底物竞争性抑制剂。 还公开了GSK-3的突变体及其用于鉴定推定的GSK-3底物竞争性抑制剂的用途。
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公开(公告)号：US20080312188A1
公开(公告)日：2008-12-18
申请号：US12149336
申请日：2008-04-30
Applicant: Hagit Eldar-Finkelman , Moshe Portnoy
Inventor： Hagit Eldar-Finkelman , Moshe Portnoy
IPC: A61K31/675 , C07F9/6503 , A61P3/04 , A61P3/10 , C07F9/58
CPC classification number: C07F9/094 , A61K38/00 , C07F9/6518 , C07K7/06 , C07K14/4703 , C07K14/4705 , C07K2299/00 , C12N9/1205
Abstract: Novel compounds designed to allow interactions with binding sites of GSK-3 and hence are capable of inhibiting GSK-3 activity, via inhibition of substrate binding are disclosed. Further disclosed are pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions.
Abstract translation: 公开了旨在允许与GSK-3的结合位点相互作用并因此通过抑制底物结合而抑制GSK-3活性的新型化合物。 进一步公开的是包含其的药物组合物和在治疗GSK-3介导的病症中使用它们的方法。
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