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公开(公告)号：US08680047B2
公开(公告)日：2014-03-25
申请号：US13210117
申请日：2011-08-15
IPC分类号： A61K38/00
CPC分类号： C07K14/70578 , A61K38/00
摘要： Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.
摘要翻译： 开发了禁用Fas的外来肽模拟物。 构建了Fas受体 - 配体复合物的三维模型，并且结构上预测与结合配体相关的受体区域用于产生约束肽模拟物。 鉴定了外环抗Fas肽模拟物阻断Fas受体 - 配体相互作用，并在体外和体内调节Fas生物活性。 模拟物可用于例如治疗Fas相关病理学。
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公开(公告)号：US07288519B2
公开(公告)日：2007-10-30
申请号：US10445399
申请日：2003-05-23
CPC分类号： C07K14/70578 , A61K38/00
摘要： Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.
摘要翻译： 开发了禁用Fas的外来肽模拟物。 构建了Fas受体 - 配体复合物的三维模型，并且结构上预测与结合配体相关的受体区域用于产生约束肽模拟物。 鉴定了外环抗Fas肽模拟物阻断Fas受体 - 配体相互作用，并在体外和体内调节Fas生物活性。 模拟物可用于例如治疗Fas相关病理学。
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公开(公告)号：US20120245081A1
公开(公告)日：2012-09-27
申请号：US13210117
申请日：2011-08-15
IPC分类号： A61K38/08 , A61P31/18 , A61P27/02 , A61P1/16 , A61P13/12 , A61P29/00 , A61P37/06 , A61P19/02 , A61K38/12
CPC分类号： C07K14/70578 , A61K38/00
摘要： Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.
摘要翻译： 开发了禁用Fas的外来肽模拟物。 构建了Fas受体 - 配体复合物的三维模型，并且结构上预测与结合配体相关的受体区域用于产生约束肽模拟物。 鉴定了外环抗Fas肽模拟物阻断Fas受体 - 配体相互作用，并在体外和体内调节Fas生物活性。 模拟物可用于例如治疗Fas相关病理学。
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公开(公告)号：US08022176B2
公开(公告)日：2011-09-20
申请号：US11869556
申请日：2007-10-09
IPC分类号： A61K38/12
CPC分类号： C07K14/70578 , A61K38/00
摘要： Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.
摘要翻译： 开发了禁用Fas的外来肽模拟物。 构建了Fas受体 - 配体复合物的三维模型，并且结构上预测与结合配体相关的受体区域用于产生约束肽模拟物。 鉴定了外环抗Fas肽模拟物阻断Fas受体 - 配体相互作用，并在体外和体内调节Fas生物活性。 模拟物可用于例如治疗Fas相关病理学。
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公开(公告)号：US20080153742A1
公开(公告)日：2008-06-26
申请号：US11869556
申请日：2007-10-09
CPC分类号： C07K14/70578 , A61K38/00
摘要： Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.
摘要翻译： 开发了禁用Fas的外来肽模拟物。 构建了Fas受体 - 配体复合物的三维模型，并且结构上预测与结合配体相关的受体区域用于产生约束肽模拟物。 鉴定了外环抗Fas肽模拟物阻断Fas受体 - 配体相互作用，并在体外和体内调节Fas生物活性。 模拟物可用于例如治疗Fas相关病理学。
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公开(公告)号：US20150010551A1
公开(公告)日：2015-01-08
申请号：US14485525
申请日：2014-09-12
IPC分类号： C07K16/32 , A61K45/06 , A61N5/10 , A61K39/395
CPC分类号： C07K16/32 , A61K38/1709 , A61K39/39558 , A61K45/06 , A61K48/00 , A61K2039/505 , A61K2039/507 , A61K2039/572 , A61N5/10 , C07K14/71 , C07K2317/24 , C07K2317/73 , A61K2300/00
摘要： Methods of treating an individual who has an erbB protein mediated tumor is disclosed. Methods of preventing erbB protein mediated tumors in an individual are disclosed. The methods comprise administering to the individual a nucleic acid molecule that encodes a protein that dimerizes with an erbB protein and that is deficient in tyrosine kinase activity. Composition that comprise such nucleic acid molecules including pharmaceutical compositions are disclosed.
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7.发明授权Cavity induced allosteric modification of intermolecular interactions and methods of identifying compounds that effect the same 有权分子间相互作用的腔诱导变构修饰和识别影响相同的化合物的方法公开(公告)号：US08785419B2
公开(公告)日：2014-07-22
申请号：US13194832
申请日：2011-07-29
IPC分类号： A01N33/26 , A61K31/655 , A01N43/36 , A61K31/40 , A01N37/28 , A61K31/215 , A01N47/28 , A61K31/17 , A61K8/42
CPC分类号： A61K31/655 , A61K8/42 , A61K31/17 , A61K31/40 , G01N33/573 , G01N33/68 , G01N2500/02
摘要： Method of identifying compounds that modulate intermolecular interactions between a target protein and a modifier are disclosed. Pharmaceutical composition comprising compounds that inhibit intermolecular interactions between a target protein and a modifier are disclosed. Methods of treating individual suffering from inflammatory conditions, undesirable immune responses, immunological conditions and bacterial infections are disclosed.
摘要翻译： 公开了鉴定调节靶蛋白和修饰剂之间的分子间相互作用的化合物的方法。 公开了包含抑制靶蛋白和修饰剂之间的分子间相互作用的化合物的药物组合物。 公开了治疗患有炎性病症，不良免疫应答，免疫学条件和细菌感染的个体的方法。
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公开(公告)号：US20120122910A1
公开(公告)日：2012-05-17
申请号：US13142731
申请日：2010-01-19
申请人： Alan Berezov , Qiang Wang , Ramachandran Murali , Mark I. Greene
发明人： Alan Berezov , Qiang Wang , Ramachandran Murali , Mark I. Greene
IPC分类号： A61K31/4747 , A61K31/352 , A61P35/04 , A61P35/00 , A61P35/02 , A61K31/404 , A61K31/192
CPC分类号： A61K31/404 , A61K31/352 , A61K31/4704
摘要： Disclosed herein are methods of treating cancer by administering to a patient a small molecule inhibitor of Survivin. Also disclosed herein are methods of inhibiting Survivin dimerization in a patient by administering a compound of formula (I), (II), (III), or (IV). Methods of inducing cell cycle arrest in cancer cells, comprising G2/M stage arrest, in a patient by administering a compound of formula (I), (II), (III), or (IV) are also disclosed. Further disclosed herein are methods of inducing apoptosis in cancer cells in a patient by administering a compound of formula (I), (II), (III), or (IV).
摘要翻译： 本文公开了通过向患者施用存活蛋白的小分子抑制剂来治疗癌症的方法。 本文还公开了通过施用式（I），（II），（III）或（IV）的化合物来抑制患者存活蛋白二聚化的方法。 还公开了通过施用式（I），（II），（III）或（IV）的化合物在患者体内诱导细胞周期停滞的方法，包括G2 / M期骤停。 本文进一步公开的是通过施用式（I），（II），（III）或（IV）化合物来诱导患者癌细胞凋亡的方法。
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公开(公告)号：US08057799B2
公开(公告)日：2011-11-15
申请号：US12625706
申请日：2009-11-25
申请人： Mark I. Greene , Ramachandran Murali , Hongtao Zhang , Mark Richter , Alan Berezov , Qingdu Liu , Jinqiu Chen
发明人： Mark I. Greene , Ramachandran Murali , Hongtao Zhang , Mark Richter , Alan Berezov , Qingdu Liu , Jinqiu Chen
IPC分类号： A61K39/00
CPC分类号： C07K14/71 , A61K38/00 , A61K39/00 , A61K39/0011 , A61K47/48238 , A61K47/4833 , A61K47/48384 , A61K47/48407 , A61K47/48507 , A61K47/62 , A61K47/646 , A61K47/6803 , A61K47/6809 , A61K47/6835 , A61K51/10 , C07K7/06 , C07K7/08 , C07K14/7151 , C07K14/82
摘要： Peptides, mimetics and antibodies of erbB, TNF, and IgSF receptors and pharmaceutical compositions comprising the same are described. Methods of using such antibodies, peptides, and mimetics in therapeutic, prophylactic, imaging and diagnostic applications are disclosed.
摘要翻译： 描述了erbB，TNF和IgSF受体的肽，模拟物和抗体以及包含其的药物组合物。 公开了在治疗，预防，成像和诊断应用中使用这些抗体，肽和模拟物的方法。
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公开(公告)号：US20100311669A1
公开(公告)日：2010-12-09
申请号：US12758435
申请日：2010-04-12
CPC分类号： C07K16/32 , A61K2039/505 , C07K2317/565
摘要： Novel peptides and pharmaceutical compositions comprising the same are disclosed. Conjugated compositions peptides linked to detectable agents and/or cytotoxic agents. are disclosed. Method of detecting tumors that have p185 on tumor cell surfaces are disclosed. Methods of preventing transformation of a normal cell into a tumor cell in an individual at risk of developing a tumor having tumor cells which have p185 on their surfaces are disclosed. Methods of treating an individual who has cancer characterized by tumor cells that have a p185 on their cell surfaces are disclosed.
摘要翻译： 公开了包含其的新型肽和药物组合物。 与可检测的试剂和/或细胞毒性剂连接的共轭组合物肽。 被披露。 公开了检测肿瘤细胞表面上具有p185的肿瘤的方法。 公开了防止正常细胞转化成具有在其表面具有p185的肿瘤细胞的肿瘤的风险中的个体的肿瘤细胞的方法。 公开了在细胞表面处理具有p185的肿瘤细胞特征的癌症的个体的方法。
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