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1. 发明申请

WO2005084317A3 DIMERIC SMALL MOLECULE POTENTIATORS OF APOPTOSIS 审中-公开
标题翻译：二聚体小分子拮抗剂
公开(公告)号：WO2005084317A3
公开(公告)日：2006-01-12
申请号：PCT/US2005006650
申请日：2005-03-01
申请人： UNIV TEXAS
发明人： HARRAN PATRICK G , WANG XIAODONG , DE BRABANDER JEF K , LI LIN , THOMAS RANNY MATHEW , SUZUKI HIDETAKA
IPC分类号： A61K31/165 , C07D249/04 , A61K31/41 , A61K31/42 , C07D257/04 , C07D263/08
CPC分类号： C07D413/14 , A61K31/41 , A61K31/422 , C07D207/08 , C07D401/10 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14 , C07D495/04 , C07K5/06026 , C07K5/06034
摘要： Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
摘要翻译：使用通式M1-L-M2的活性二聚体Smac肽模拟物促进胱天蛋白酶活性和凋亡，其中部分M1和M2是单体Smac模拟物，L是共价连接体。靶向癌性或炎性细胞与有效量的活性二聚体Smac模拟物接触，并且检测到靶细胞凋亡的最终增加。接触步骤可以通过给包含治疗有效量的二聚模拟物的药物组合物施用，其中个体可以同时或先前放射或化学治疗用于治疗新生血管病变。

2. 发明申请

WO2012065139A3 ENTPD5 INHIBITORS 审中-公开
标题翻译： ENTPD5抑制剂
公开(公告)号：WO2012065139A3
公开(公告)日：2013-02-21
申请号：PCT/US2011060487
申请日：2011-11-11
申请人： UNIV TEXAS , WANG XIAODONG , MACMILLAN JOHN B , HUANG SONG , FANG MIN
发明人： WANG XIAODONG , MACMILLAN JOHN B , HUANG SONG , FANG MIN
IPC分类号： C07D487/04 , A61K31/4162 , A61K31/519 , A61P35/00 , C07D311/04 , C07D495/04
CPC分类号： A61K31/498 , A61K9/4866 , A61K31/00 , A61K31/404 , A61K31/4168 , A61K31/515
摘要： The invention provides methods and pharmaceutical compositions for treating cancer or promoting apoptosis of cancer cells, or reducing the resistance of cancer cells to chemotherapy or apoptosis-promoting therapies by contacting the cancer cells with an ENTPD5-specific inhibitor.
摘要翻译：本发明提供了通过使癌细胞与ENTPD5特异性抑制剂接触来治疗癌症或促进癌细胞凋亡的方法和药物组合物，或降低癌细胞对化学疗法或细胞凋亡促进疗法的抗性。

3. 发明申请

WO0216402A3 APOPTOTIC COMPOUNDS 审中-公开
标题翻译：凋亡化合物
公开(公告)号：WO0216402A3
公开(公告)日：2002-06-13
申请号：PCT/US0141869
申请日：2001-08-23
申请人： UNIV TEXAS
发明人： WANG XIAODONG , DU CHUNYING
IPC分类号： C07K14/47 , A61K38/02 , A61K38/05 , A61K38/06 , C07K2/00 , C07K5/06 , C07K5/083 , G01N33/53
CPC分类号： A61K38/07 , A61K38/08 , C07K14/4747
摘要： The invention provides methods and compositions for apoptosis of pathogenic cells. The general method comprises the of contacting the cells with an effective amount of an AV peptoid, wherein the AV peptoid is a peptide comprising AX1, wherein X1 is V, I or L, or a peptide mimetic thereof, which interacts with an Inhibitor of Apoptosis protein (IAP) as measured by IAP binding, procaspase-3 activation or promotion of apoptosis, wherein apoptosis of the pathogenic cells is enhanced. The subject compositions encompass pharmaceutical compositions comprising a therapeutically effective amount of a subject AV peptoid in dosage form and a pharmaceutically acceptable carrier, wherein the AV peptoid is a peptide comprising AX1, wherein X1 is V, I or L, or a peptide mimetic thereof, which inhibits the activity of an Inhibitor of Apoptosis protein (IAP) as measured by IAP binding, procaspase-3 activation or promotion of apoptosis. The invention also provides assays for identifying agents which modulates the interaction of an AV peptoid with an IAP, active compounds identified in such screens and their use in the foregoing compositions and therapeutic methods.
摘要翻译：本发明提供了用于致病细胞凋亡的方法和组合物。一般方法包括使细胞与有效量的AV类肽接触，其中AV类肽是包含AX1的肽，其中X1是V，I或L或其肽模拟物，其与细胞凋亡抑制剂相互作用通过IAP结合，procaspase-3活化或促进细胞凋亡测量的蛋白质（IAP），其中致病细胞的凋亡增强。本主题组合物涵盖药物组合物，其包含剂型中的治疗有效量的受试者AV类肽和药学上可接受的载体，其中所述AV类肽是包含AX1的肽，其中X1是V，I或L或其肽模拟物，其抑制凋亡蛋白抑制剂（IAP）的活性，如通过IAP结合，procaspase-3活化或细胞凋亡促进所测量的。本发明还提供了用于鉴定调节AV类肽与IAP相互作用的试剂，在这样的筛选中鉴定的活性化合物以及它们在前述组合物和治疗方法中的用途的测定。

4. 发明申请

WO2012065139A2 ENTPD5 INHIBITORS 审中-公开
标题翻译： ENTPD5抑制剂
公开(公告)号：WO2012065139A2
公开(公告)日：2012-05-18
申请号：PCT/US2011060487
申请日：2011-11-11
申请人： UNIV TEXAS , WANG XIAODONG , MACMILLAN JOHN B , HUANG SONG , FANG MIN
发明人： WANG XIAODONG , MACMILLAN JOHN B , HUANG SONG , FANG MIN
IPC分类号： C07D487/04 , A61K31/4162 , A61K31/519 , A61P35/00 , C07D311/04 , C07D495/04
CPC分类号： A61K31/498 , A61K9/4866 , A61K31/00 , A61K31/404 , A61K31/4168 , A61K31/515
摘要： The invention provides methods and pharmaceutical compositions for treating cancer or promoting apoptosis of cancer cells, or reducing the resistance of cancer cells to chemotherapy or apoptosis-promoting therapies by contacting the cancer cells with an ENTPD5-specific inhibitor.
摘要翻译：本发明提供了通过使癌细胞与ENTPD5特异性抑制剂接触来治疗癌症或促进癌细胞凋亡或降低癌细胞对化疗或凋亡促进疗法的抗性的方法和药物组合物。

5. 发明申请

WO9855615A9 APAF-1, THE CED-4 HUMAN HOMOLOG, AN ACTIVATOR OF CASPASE-3 审中-公开
标题翻译： APAF-1，CED-4人类HOMOLOG，CASPASE-3的激活剂
公开(公告)号：WO9855615A9
公开(公告)日：1999-04-01
申请号：PCT/US9811773
申请日：1998-06-05
申请人： GENENTECH INC , UNIV TEXAS
发明人： ZOU HUA , HENZEL WILLIAM J , WANG XIAODONG
IPC分类号： A01K67/027 , A61K38/00 , A61K39/395 , A61K45/00 , A61P25/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07K14/47 , C07K16/18 , C07K19/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , G01N33/15 , G01N33/50 , A61K38/17 , C12N15/62 , G01N33/68
CPC分类号： C07K14/4747 , A01K2217/075 , A61K38/00 , C07K2319/00
摘要： Novel polypeptides, designated Apaf-1, which are capable of modulating apoptosis are provided. Compositions including Apaf-1 chimeras, nucleic acid encoding Apaf-1, and antibodies to Apaf-1 are also provided.
摘要翻译：提供了能够调节凋亡的新型多肽，称为Apaf-1。还提供了包括Apaf-1嵌合体，编码Apaf-1的核酸和Apaf-1的抗体的组合物。

6. 发明申请

WO9426922A3 METHODS AND COMPOSITIONS RELATING TO STEROL REGULATORY ELEMENT BINDING PROTEINS 审中-公开
标题翻译：与甾体调节元件结合蛋白相关的方法和组合物
公开(公告)号：WO9426922A3
公开(公告)日：1995-01-05
申请号：PCT/US9405300
申请日：1994-05-13
申请人： UNIV TEXAS
发明人： GOLDSTEIN JOSEPH L , BROWN MICHAEL S , BRIGGS MICHAEL R , WANG XIAODONG
IPC分类号： C07K14/47 , C07K14/525 , C07K14/61 , C12N1/21 , C12N9/72 , C12N15/12 , C12N15/67 , C12N15/85 , C12P21/08 , C12Q1/68 , C12P21/02 , C07K13/00 , C12N5/10 , C12N15/11 , G01N33/68
CPC分类号： C07K14/525 , C07K14/4702 , C07K14/61 , C12N9/6459 , C12N15/67 , C12N15/85 , C12N2830/002 , C12N2830/008 , C12N2830/15 , C12N2830/85 , C12Y304/21069
摘要： A sterol regulatory element (SRE) binding protein (SREBP) which activates transcription from SREs, such as SRE-1 of the low density lipoprotein (LDL) receptor gene, is disclosed, as are DNA segments encoding SREBPs such as an SREBP-1 or SREBP-2. Also described are methods for using SREBP to promote SRE-mediated transcription and LDL receptor production in the presence of sterols, and screening assay for the identification of further agents with such properties. The SREBP and other agents may be used to reduce plasma cholesterol levels and to treat various medical problems associated with hypercholesterolemia.

7. 发明申请

WO0149719A3 ACTIVATORS OF CASPASES 审中-公开
标题翻译： CASPASES的激活者
公开(公告)号：WO0149719A3
公开(公告)日：2002-02-07
申请号：PCT/US0100321
申请日：2001-01-05
申请人： UNIV TEXAS
发明人： WANG XIAODONG , DU CHUNYING
IPC分类号： G01N33/50 , C07K14/47 , C12N15/09 , C12Q1/68 , G01N33/15 , C12N15/12
CPC分类号： C07K14/4747
摘要： The invention provides methods and compositions relating to polypeptide activators of caspases such as polypeptide and polynucleotide sequences diagnostic of caspase activators. These sequences and polypeptides and polynucleotides embodying these sequences find a wide variety of diagnostic and therapeutic applications involving detecting and/or modulating expression and/or function of activators or caspases or genes or transcripts encoding such activators and generating genetic and immuno probes specific to activators of caspases.
摘要翻译：本发明提供了与胱天蛋白酶的多肽激活剂相关的方法和组合物，例如胱天蛋白酶激活剂诊断的多肽和多核苷酸序列。体现这些序列的这些序列和多肽和多核苷酸发现了多种诊断和治疗应用，涉及检测和/或调节激活剂或胱天蛋白酶或编码这种激活剂的基因或转录物的表达和/或功能，并产生对于活化剂的活化剂特异性的遗传和免疫探针半胱氨酸蛋白酶。

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