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1. 发明专利

AU2020206884A1 Modulators of Pin1 activity and uses thereof 未知
公开(公告)号：AU2020206884A1
公开(公告)日：2021-08-05
申请号：AU2020206884
申请日：2020-01-09
申请人： BETH ISRAEL DEACONESS MEDICAL CT INC , DANA FARBER CANCER INST INC , YEDA RES & DEV
发明人： LONDON NIR , ZAIDMAN DANIEL , DUBIELLA CHRISTIAN , GRAY NATHANAEL S , PINCH BENIKA JOAN , LU KUN PING , LOOK ALFRED THOMAS , HE SHUNING , ZHOU XIAO ZHEN , LIAN XIAOLAN
IPC分类号： A61K31/122 , A61K31/381 , A61K31/4178 , A61K31/4192 , A61P35/00 , C07D333/48 , C12Q1/37
摘要： Disclosed herein are compounds comprising an electrophilic moiety and rigid moiety for use in modulating an activity of Pin1. The rigid moiety comprises at least one functional group that is capable of forming hydrogen bonds with hydrogen atoms, wherein the electrophilic moiety and the rigid moiety are arranged such that the electrophilic moiety is capable of covalently binding to the Cys 113 residue of Pin1, and the rigid moiety is capable of forming hydrogen bonds with the Gin 131 and His 157 residues of Pin1. Further disclosed are novel compounds having Formula Id: Wherein the dashed line, W, X, Y, Z, Ra-Rc, R

2. 发明专利

CA3124951A1 MODULATORS OF PIN1 ACTIVITY AND USES THEREOF 未知
公开(公告)号：CA3124951A1
公开(公告)日：2020-07-16
申请号：CA3124951
申请日：2020-01-09
申请人： YEDA RES & DEV , DANA FARBER CANCER INST INC , BETH ISRAEL DEACONESS MEDICAL CT INC
发明人： LONDON NIR , ZAIDMAN DANIEL , DUBIELLA CHRISTIAN , GRAY NATHANAEL S , PINCH BENIKA JOAN , LU KUN PING , LOOK ALFRED THOMAS , HE SHUNING , ZHOU XIAO ZHEN , LIAN XIAOLAN
IPC分类号： A61K31/122 , A61K31/381 , A61K31/4178 , A61K31/4192 , A61P35/00 , C07D333/48 , C12Q1/37
摘要： Disclosed herein are compounds comprising an electrophilic moiety and rigid moiety for use in modulating an activity of Pin1. The rigid moiety comprises at least one functional group that is capable of forming hydrogen bonds with hydrogen atoms, wherein the electrophilic moiety and the rigid moiety are arranged such that the electrophilic moiety is capable of covalently binding to the Cys 113 residue of Pin1, and the rigid moiety is capable of forming hydrogen bonds with the Gin 131 and His 157 residues of Pin1. Further disclosed are novel compounds having Formula Id: Wherein the dashed line, W, X, Y, Z, Ra-Rc, R1, R2, L1, L2 and n are as defined herein, and libraries comprising such compounds. Further disclosed are methods of identifying a compound capable of modulating an activity of Pin1, by screening a library of compounds.

3. 发明专利

AU2005209659A1 Pin1 as a marker for abnormal cell growth 未知
公开(公告)号：AU2005209659A1
公开(公告)日：2005-10-06
申请号：AU2005209659
申请日：2005-09-12
申请人： BETH ISRAEL DEACONESS MEDICAL CT INC
发明人： ZHOU XIAO ZHEN , LU KUN PING , WULF GERBURG
IPC分类号： G01N33/574

4. 发明专利

HK1214165A1 特定構象抗體生成和使用的方法和組合物未知
公开(公告)号：HK1214165A1
公开(公告)日：2016-07-22
申请号：HK16102295
申请日：2016-02-26
申请人： BETH ISRAEL DEACONESS MEDICAL CT INC
发明人： LU KUN PING , ZHOU XIAO ZHEN
IPC分类号： A61K20060101

5. 发明专利

AU3600400A Methods and compositions for regulating protein-protein interactions 未知
公开(公告)号：AU3600400A
公开(公告)日：2000-09-04
申请号：AU3600400
申请日：2000-02-18
申请人： BETH ISRAEL DEACONESS MEDICAL CT INC
发明人： LU KUN PING , ZHOU XIAO ZHEN
IPC分类号： G01N33/50 , A61K38/08 , A61K38/10 , A61K38/17 , A61K38/52 , A61K45/00 , A61K47/48 , A61P25/28 , A61P35/00 , C07K14/47 , C12N5/06 , C12N9/90 , C12N9/99 , G01N33/15 , G01N33/566 , A61K38/00 , A61K38/53 , A61K31/00 , A61K33/00
摘要： The invention relates to methods and compositions of WW-domains as phosphoserine and phosphothrenonine binding modules. The WW-domain containing polypeptides of the invention can be used, for example, to regulate cell growth; to treat neurodegenerative diseases; to screen for substances that modulated interactions between WW-domain containing polypeptides and phosphorylated ligands; as drug targeting vehicles; to direct protein degradation; and in the treatment of certain diseases or conditions characterized by aberrant WW-domain containing polypeptides or their ligands.

6. 发明申请

WO2016011265A3 BIOMARKERS FOR PIN1-ASSOCIATED DISORDERS 审中-公开
标题翻译： PIN1相关疾病的生物标志物
公开(公告)号：WO2016011265A3
公开(公告)日：2016-11-17
申请号：PCT/US2015040771
申请日：2015-07-16
申请人： BETH ISRAEL DEACONESS MEDICAL CT INC
发明人： LU KUN PING , ZHOU XIAO ZHEN , WEI SHUO
IPC分类号： C12Q1/68 , G01N33/53 , G01N33/68
CPC分类号： C12Q1/6886 , A61K9/0019 , A61K9/06 , A61K31/203 , C12Q1/6883 , C12Q2600/156 , C12Q2600/158
摘要： Biomarkers and driver mutations for diagnosis and prognosis of Pin 1 -associated diseases are disclosed. In one embodiment, the methods for diagnosis of Pin 1 -associated diseases may include detecting the level of Pin1 to stage abnormal cell growth, such as breast or prostate cancer. In another embodiment, the methods include evaluating the efficacy of a treatment of abnormal cell growth, such as cancer, by monitoring the levels of Pin1. In another embodiment, the methods include using driver mutations to determine the pharmacogenetics of abnormal cell growth, such as cancer. In the present disclosure, elevated active monomeric Pin1 levels may be detected by Pin1 biomarkers, which may include Pin1 Q33K or E100D driver mutations, Pin1 protein or transcript overexpression, dephosphorylation of Pin1 on Ser71, dephosphorylation of S16, phosphorylation of S65, phosphorylation of S138, deacetylation of Pin1 on K13 and deacetylation of K46, and/or desumoylation of Pin1 on K6 and desumolation of K63, among others.
摘要翻译：公开了针1相关疾病的诊断和预后的生物标志物和驱动突变。在一个实施方案中，用于诊断针1相关疾病的方法可以包括检测Pin1的水平以进行异常细胞生长，例如乳腺癌或前列腺癌。在另一个实施方案中，所述方法包括通过监测Pin1的水平评价治疗异常细胞生长（例如癌症）的功效。在另一个实施方案中，所述方法包括使用驱动突变来确定异常细胞生长的药物遗传学，例如癌症。在本公开中，可以通过Pin1生物标志物检测到活性单体Pin1水平的升高，其可以包括Pin1Q33K或E100D驱动突变，Pin1蛋白或转录本过表达，Ser71上Pin1的去磷酸化，S16的去磷酸化，S65的磷酸化，S138的磷酸化，K13上Pin1的脱乙酰化和K46的脱乙酰化，和/或K6上Pin1的去脂化作用以及K63的脱除等。

7. 发明专利

AU2014240063B2 Methods and compositions for the generation and use of conformation-specific antibodies 未知
公开(公告)号：AU2014240063B2
公开(公告)日：2019-04-11
申请号：AU2014240063
申请日：2014-03-14
申请人： BETH ISRAEL DEACONESS MEDICAL CT INC
发明人： LU KUN PING , ZHOU XIAO ZHEN
IPC分类号： A61K38/10
摘要： The present invention features methods and compositions for the generation and use of conformation-specific antibodies or fragments thereof.

8. 发明专利

AU2013271378A1 Methods and compositions for the inhibition of Pin1 未知
公开(公告)号：AU2013271378A1
公开(公告)日：2014-12-18
申请号：AU2013271378
申请日：2013-06-07
申请人： BETH ISRAEL DEACONESS MEDICAL CT INC , THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： LU KUN PING , BOXER MATTHEW BRIAN , DAVIS MINDY IRENE EMILY , PRAGANI RAJAN , SHEN MIN , SIMEONOV ANTON MOMTCHILOV , WEI SHUO , ZHOU XIAO ZHEN
IPC分类号： A61K31/473 , C12N9/90
摘要： The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.

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