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公开(公告)号：US20110028753A1
公开(公告)日：2011-02-03
申请号：US12796212
申请日：2010-06-08
IPC分类号： C07C229/00
CPC分类号： C07K1/00 , A61K38/00 , A61K38/02 , C07K1/04 , C07K1/047 , C07K1/10 , C07K1/113 , C07K14/001 , C07K14/4746 , C12N15/1093
摘要： The present invention provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds libraries thereof. The synthesis of these novel stabilized compounds involves (1) synthesizing a peptide from a selected number of natural or non-natural amino acids, wherein said peptide comprises at least two moieties capable of undergoing reaction to promote carbon-carbon bond formation; and (2) contacting said peptide with a reagent to generate at least one crosslinker and to effect stabilization of a secondary structure motif. The present invention, in a preferred embodiment, provides stabilized p53 donor helical peptides. Additionally, the present invention provides methods for disrupting the p53/MDM2 binding interaction comprising (1) providing a crosslinked stabilized α-helical structure; and (2) contacting said crosslinked stabilized α-helical structure with MDM2.
摘要翻译： 本发明提供具有二级结构基序的新型稳定化交联化合物，这些新化合物的文库，以及合成这些化合物文库的方法。 这些新型稳定化合物的合成涉及（1）从选定数量的天然或非天然氨基酸合成肽，其中所述肽包含至少两个能够进行促进碳 - 碳键形成反应的部分; 和（2）使所述肽与试剂接触以产生至少一种交联剂并实现二级结构基序的稳定化。 本发明在优选的实施方案中提供稳定的p53供体螺旋肽。 另外，本发明提供了破坏p53 / MDM2结合相互作用的方法，其包括（1）提供交联的稳定的α-螺旋结构; 和（2）使所述交联的稳定的α-螺旋结构与MDM2接触。
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公开(公告)号：US20100184645A1
公开(公告)日：2010-07-22
申请号：US12593384
申请日：2008-03-28
申请人： Gregory L. Verdine , Young-Woo Kim
发明人： Gregory L. Verdine , Young-Woo Kim
IPC分类号： A61K38/12 , C07K7/08 , C07K1/00 , C07C229/30 , A61P35/02
CPC分类号： C07K1/1075 , C07C229/30 , C07K1/113 , C07K7/06 , C07K7/08 , C07K14/001 , C07K14/005 , C07K14/4705 , C07K14/4746 , C07K14/4747 , C07K14/605 , C07K14/705 , C12N7/00 , C12N9/22 , C12N2740/16322 , C12N2770/24222 , C12Y301/00
摘要： The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.
摘要翻译： 本发明提供了本发明的缝合多肽，其药物组合物，以及制造和使用本发明缝合多肽的方法。
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公开(公告)号：US20090093534A1
公开(公告)日：2009-04-09
申请号：US11807927
申请日：2007-05-29
IPC分类号： A61K31/40 , C07D207/08 , C40B40/04 , A61P25/04
CPC分类号： C07C237/22 , C07C235/34 , C07C237/20 , C07C327/22
摘要： Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.
摘要翻译： 本文描述了包括这些化合物的新型化合物和组合物，以及使用和制备化合物的方法。 该化合物可用于治疗应用，包括对受试者（例如哺乳动物，人，狗，猫，马）中疾病或疾病症状的调节。 通过与该受体的结合亲和力，这些化合物可用作μ阿片受体（MOR）的调节剂。
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公开(公告)号：US06582923B2
公开(公告)日：2003-06-24
申请号：US10104818
申请日：2002-03-22
IPC分类号： C12Q168
CPC分类号： C07H19/10 , C07H19/14 , C07H19/20 , C07H21/00 , C12N9/1252 , C12N15/11 , C12P19/34 , C12Q1/6827 , C12Q1/6872 , C12Q2565/627 , C12Q2525/101 , C12Q2523/107
摘要： The present invention relates to a method of synthesizing a polynucleotide with incorporation of a modified nucleotide.
摘要翻译： 本发明涉及合成多核苷酸并掺入经修饰的核苷酸的方法。
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公开(公告)号：US06500650B1
公开(公告)日：2002-12-31
申请号：US09655104
申请日：2000-09-05
IPC分类号： C12Q168
CPC分类号： C12Q1/6858 , C07H19/10 , C07H19/14 , C07H19/20 , C07H21/00 , C12N9/1252 , C12N15/11 , C12P19/34 , C12Q1/6827 , C12Q1/683 , C12Q1/6872 , C12Q2525/117 , C12Q2523/107 , C12Q2527/107 , C12Q2565/627 , C12Q2525/101
摘要： The present invention relates to methods for the detection of polymorphism in polynucleotides by using hybridization of fragments of segments of a polynucleotide suspected of containing a polymorphism with an oligonucleotide having a sequence complementary to a fragment identifying the polymorphism and subsequent detection of incorporated labels in the oligonucleotide-fragment duplex.
摘要翻译： 本发明涉及通过使用疑似含有多态性的多核苷酸的片段的片段与具有与鉴定多态性的片段互补的序列的寡核苷酸杂交并随后检测寡核苷酸中的并入标记的方法来检测多核苷酸中的多态性的方法 碎片双工。
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公开(公告)号：US06440705B1
公开(公告)日：2002-08-27
申请号：US09394457
申请日：1999-09-10
IPC分类号： C12P1934
CPC分类号： C07H19/10 , C07H19/14 , C07H19/20 , C07H21/00 , C12N9/1252 , C12N15/11 , C12P19/34 , C12Q1/6827 , C12Q1/6872 , C12Q2565/627 , C12Q2525/101 , C12Q2523/107
摘要： The present invention relates to methods for the analysis of polynucleotides including detection of variance in nucleotide sequence without the need for full sequence determination, full sequence determination of a polynucleotide, genotyping of DNA and labeling a polynucleotide fragment during the process of cleaving it into fragments.
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公开(公告)号：US20180216108A1
公开(公告)日：2018-08-02
申请号：US15746220
申请日：2016-07-22
申请人： Chandra Vargeese , Meena , Nenad Svrzikapa , Susovan Mohapatra , Christopher J. Francis , Gregory L. Verdine , Anna Sokolovska
发明人： Chandra Vargeese , Meena , Nenad Svrzikapa , Susovan Mohapatra , Christopher J. Francis , Gregory L. Verdine , Anna Sokolovska
IPC分类号： C12N15/113 , A61P25/28
摘要： Among other things, the present disclosure relates to chirally controlled oligonucleotides of select designs, chirally controlled oligonucleotide compositions, and methods of making and using the same. In some embodiments, a provided chirally controlled oligonucleotide composition provides different cleavage patterns of a nucleic acid polymer than a reference oligonucleotide composition. In some embodiments, a provided chirally controlled oligonucleotide composition provides single site cleavage within a complementary sequence of a nucleic acid polymer. In some embodiments, a chirally controlled oligonucleotide composition has any sequence of bases, and/or pattern or base modifications, sugar modifications, backbone modifications and/or stereochemistry, or combination of these elements, described herein.
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公开(公告)号：US09744183B2
公开(公告)日：2017-08-29
申请号：US13381323
申请日：2010-07-06
申请人： Gregory L. Verdine , Meena . , Naoki Iwamoto
发明人： Gregory L. Verdine , Meena . , Naoki Iwamoto
CPC分类号： A61K31/70 , C07F9/65515 , C07H21/00
摘要： Described herein are nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties. Also described herein are methods of making and using nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties.
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公开(公告)号：US08957026B2
公开(公告)日：2015-02-17
申请号：US13825709
申请日：2011-09-22
CPC分类号： C07K14/4705 , A61K38/00 , C07K1/113 , C07K7/08 , C07K14/47 , C07K14/4702 , C07K14/4703
摘要： The invention relates to β-catenin targeting peptides comprising an α-helical segment that are optionally stapled or stitched, and pharmaceutical compositions thereof. Uses of the inventive β-catenin targeting polypeptides including methods for treatment of disease, such as diseases associated with aberrant Wnt signaling, including cancer, are also provided.
摘要翻译： 本发明涉及包含可选择性地缝合或缝合的α-螺旋区段的β-连环蛋白靶向肽及其药物组合物。 还提供了本发明的β-连环蛋白靶向多肽的用途，包括治疗疾病的方法，例如与异常Wnt信号传导相关的疾病，包括癌症。
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公开(公告)号：US20140235549A1
公开(公告)日：2014-08-21
申请号：US14126642
申请日：2012-06-15
IPC分类号： C07K14/00
CPC分类号： C07K14/001 , A61K38/00 , C07K14/4702
摘要： The present invention provides inventive polypeptides comprising a C terminal RAB binding domain (RabBD) of RAB family interacting proteins (FIPs) stabilized by peptide stapling, and pharmaceutical compositions thereof. Also provided are methods for modulating RAB function comprising contacting an inventive stapled polypeptide with a RAB protein, and methods of treatment associated with modulation of RAB activity. The present invention also provides methods of making the inventive stapled polypeptides by ring closing metathesis of unstapled polypeptide precursors.
摘要翻译： 本发明提供了包含通过肽缝合稳定的RAB家族相互作用蛋白（FIPs）的C末端RAB结合结构域（RabBD）的本发明多肽及其药物组合物。 还提供了用于调节RAB功能的方法，包括使本发明的缝合多肽与RAB蛋白质接触，以及与调节RAB活性相关的治疗方法。 本发明还提供了通过闭合未经取代的多肽前体的复分解制备本发明的缝合多肽的方法。
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