公开(公告)号：US20140155420A1

公开(公告)日：2014-06-05

申请号：US13978820

申请日：2012-01-10

Applicant: Rui Zhao ,  Heide L. Ford ,  Noel Southall ,  Erika Englund ,  Samarjit Patnaik ,  Marc Ferrer ,  Wei Zheng ,  Seameen Dehdashti ,  Juan Marugan

Inventor： Rui Zhao ,  Heide L. Ford ,  Noel Southall ,  Erika Englund ,  Samarjit Patnaik ,  Marc Ferrer ,  Wei Zheng ,  Seameen Dehdashti ,  Juan Marugan

IPC: A61K31/443 ,  A61K31/4174 ,  A61K31/277 ,  A61K31/4709 ,  A61K31/255 ,  A61K31/155

CPC classification number: A61K31/443 ,  A61K31/15 ,  A61K31/155 ,  A61K31/255 ,  A61K31/277 ,  A61K31/4174 ,  A61K31/4709

Abstract: The invention provides small molecule inhibitors of EYA2 phosphatase activity and EYA2 binding to Six1. These inhibitors are proposed for use in methods of treating cancer in a subject, such as those involving Six1 and/or EYA2 disregulation. In some embodiments, the invention further provides for the administration of a second cancer therapy to the subject.

Abstract translation: 本发明提供EYA2磷酸酶活性的小分子抑制剂和与Six1结合的EYA2。 这些抑制剂被提出用于治疗受试者的癌症的方法，例如涉及Six1和/或EYA2失调的那些。 在一些实施方案中，本发明进一步提供对受试者施用第二次癌症治疗。

公开(公告)号：US20210040074A1

公开(公告)日：2021-02-11

申请号：US16977897

申请日：2019-03-06

Applicant: David R. Sibley ,  Kathryn D. Luderman ,  Jennie L. Conroy ,  R. Benjamin Free ,  Prashi Jain ,  Noel T. Southall ,  Marc Ferrer ,  Jeffrey Aubé ,  Kevin Frankowski ,  The United States of America,as represented by the Secretary,Department of Health and Human Service ,  University of Kansas ,  The University of North Carolina at Chapel Hill

Inventor： David R. Sibley ,  Kathryn D. Luderman ,  Jennie L. Conroy ,  R. Benjamin Free ,  Prashi Jain ,  Noel T. Southall ,  Marc Ferrer ,  Jeffrey Aubé ,  Kevin Frankowski

IPC: C07D409/12 ,  C07D471/04

Abstract: Disclosed are compounds of formulas (I) and (III) for treating or preventing a disease or disorder responsive to activation of a D1 dopamine receptor agonist in a mammal in need thereof, wherein m, n, R1-R6, and R11-R13 are as defined herein. Examples of such disease or disorder include Alzheimer's Disease, schizophrenia, Parkinson's disease, a dyskinesia, and Huntington's disease.

公开(公告)号：US20060270841A1

公开(公告)日：2006-11-30

申请号：US10504446

申请日：2003-02-25

Applicant: Amy Espeseth ,  Marc Ferrer ,  Osvaldo Flores ,  Daria Hazuda ,  James Inglese ,  Michael Miller ,  Bruce Register ,  Xiao-Ping Shi ,  Adam Simon ,  Paul Zuck

Inventor： Amy Espeseth ,  Marc Ferrer ,  Osvaldo Flores ,  Daria Hazuda ,  James Inglese ,  Michael Miller ,  Bruce Register ,  Xiao-Ping Shi ,  Adam Simon ,  Paul Zuck

IPC: C12Q1/68 ,  C07H21/04 ,  C12P21/06 ,  C12N9/64

CPC classification number: C07K14/47 ,  C07K14/4702 ,  C07K14/4711 ,  C07K2319/00 ,  C07K2319/50 ,  G01N2500/10

Abstract: The present invention provides DNA constructs, genetically engineered host cells, and methods for identifying inhibitors of amyloid precursor protein (APP) processing. The methods provide for the convenient identification, in a single assay, of inhibitors of β-secretase and γ-secretase as well as other forms of APP processing. The methods rely on fusion proteins of APP and transcription factors in which APP processing releases the transcription factors, allowing the transcription factors to activate transcription of a reporter gene. Inhibitors are identified as substances that block or diminish transcription factor release from the fusion protein, thereby causing a diminution of reporter gene readout.

Abstract translation: 本发明提供了DNA构建体，遗传工程化宿主细胞和用于鉴定淀粉样前体蛋白（APP）处理抑制剂的方法。 该方法提供了在单次测定中方便地鉴定β-分泌酶和γ-分泌酶抑制剂以及其它形式的APP处理。 该方法依赖于APP和转录因子的融合蛋白，其中APP处理释放转录因子，允许转录因子激活报告基因的转录。 抑制剂被鉴定为阻断或减少转录因子从融合蛋白释放的物质，从​​而导致报告基因读出的减少。

公开(公告)号：US20050164311A1

公开(公告)日：2005-07-28

申请号：US10484859

申请日：2002-08-02

Applicant: James Inglese ,  Marc Ferrer ,  Aaron Hamilton

Inventor： James Inglese ,  Marc Ferrer ,  Aaron Hamilton

IPC: G01N33/531 ,  C07K5/10 ,  C07K7/06 ,  C07K7/08 ,  C12Q1/34 ,  C12Q1/37 ,  C12Q1/42 ,  C12Q1/48 ,  C12Q1/527 ,  G01N33/53 ,  G01N33/542 ,  G01N33/573

CPC classification number: G01N33/573 ,  G01N33/542

Abstract: The invention is a method for detecting a reaction product which signals the presence of a reaction product inducer such as an enzyme. The method enables the recognition of epitopes that form the basis of a detection strategy without the need for specific antibodies to the epitope. In the method, a directly or indirectly labeled modular domain and a biotinylated form of the cognate peptide ligand are used as the basis for a measurable interaction. The peptide ligand can be masked by modifications through, for example, phosphorylation of the Ser or Thr residue, or extension of the amino acid sequence beyond the C-terminal Val. Because the masked residues are critical to binding of the labeled modular domain, masking of at least one of the residues prevents binding. Upon treatment of the masked residue by the appropriate enzyme, (e.g., treatment of the phosphorylated residue with a phosphatase enzyme, or treatment of the extended residue with a protease enzyme, the peptide is converted to the original unmasked ligand that is capable of binding to the labeled modular domain and forming a measurable complex.

Abstract translation: 本发明是检测反应产物诱导剂如酶的信号的反应产物的方法。 该方法能够识别构成检测策略基础的表位，而不需要针对表位的特异性抗体。 在该方法中，使用直接或间接标记的模块结构域和生物素化形式的同源肽配体作为可测量相互作用的基础。 可以通过例如Ser或Thr残基的磷酸化或氨基酸序列延伸超过C末端Val的修饰来掩蔽肽配体。 因为掩蔽的残基对于标记的模块结构域的结合至关重要，所以至少一个残基的掩蔽防止结合。 在通过适当的酶处理掩蔽的残留物（例如用磷酸酶处理磷酸化残基或用蛋白酶处理延长的残基时），将肽转化为能够结合到 标记的模块化领域并形成可衡量的复杂。