Azoline Compound and Azole Compound Library and Method for Producing Same
    1.
    发明申请
    Azoline Compound and Azole Compound Library and Method for Producing Same 审中-公开
    唑啉化合物和唑类化合物库及其制备方法

    公开(公告)号:US20140113830A1

    公开(公告)日:2014-04-24

    申请号:US14003506

    申请日:2012-03-09

    IPC分类号: G01N33/543

    摘要: An object of the present invention is to provide a method of efficiently constructing a library abundant in diversity and also usable for screening of a compound that binds to a target substance having protease activity.The present invention provides a method of constructing an azoline compound library containing two or more azoline compounds having an azoline backbone introduced into at least one of Cys, Ser, Thr, and 2,3-diamino acid, and analogs thereof of Xaa0 of a peptide represented by the following formula (I): A-(Xaa0)n-B  (I) [wherein, m numbers of Xaa0s respectively represent arbitrary amino acids, at least one of which is an amino acid selected from the group consisting of Cys, Ser, Thr, and 2,3-diamino acid, and analogs thereof, m represents an inter selected from 2 to 40, and A and B each independently represent a peptide composed of from 0 to 100 amino acids].

    摘要翻译: 本发明的目的是提供一种有效地构建多样性丰富的文库并且也可用于筛选结合具有蛋白酶活性的目标物质的化合物的方法。 本发明提供一种构建含有两个或更多个具有引入到Cys,Ser,Thr和2,3-二氨基酸中的至少一种的唑啉主链的二环或二唑化合物的唑啉化合物文献的方法,以及肽类似物的Xaa0 由下式(I)表示:A-(Xaa0)nB(I)[其中,Xaa0的m个数分别表示任意氨基酸,其中至少一个是选自Cys,Ser, Thr和2,3-二氨基酸及其类似物,m表示选自2至40个,A和B各自独立地表示由0至100个氨基酸组成的肽]。

    Azoline compound and azole compound library and method for producing same

    公开(公告)号:US10197567B2

    公开(公告)日:2019-02-05

    申请号:US14003506

    申请日:2012-03-09

    摘要: An object of the present invention is to provide a method of efficiently constructing a library abundant in diversity and also usable for screening of a compound that binds to a target substance having protease activity.The present invention provides a method of constructing an azoline compound library containing two or more azoline compounds having an azoline backbone introduced into at least one of Cys, Ser, Thr, and 2,3-diamino acid, and analogs thereof of Xaa0 of a peptide represented by the following formula (I): A-(Xaa0)n-B  (I) [wherein, m numbers of Xaa0s respectively represent arbitrary amino acids, at least one of which is an amino acid selected from the group consisting of Cys, Ser, Thr, and 2,3-diamino acid, and analogs thereof, m represents an inter selected from 2 to 40, and A and B each independently represent a peptide composed of from 0 to 100 amino acids].

    Methods for ribosomal synthesis of polypeptides containing unnatural N-terminal groups and applications thereof
    3.
    发明授权
    Methods for ribosomal synthesis of polypeptides containing unnatural N-terminal groups and applications thereof 有权
    含有非天然N端基的多肽的核糖体合成方法及其应用

    公开(公告)号:US08557542B2

    公开(公告)日:2013-10-15

    申请号:US12515074

    申请日:2007-11-13

    IPC分类号: C12P21/06

    CPC分类号: C12N15/67 C12P21/02

    摘要: The present invention aims to synthesize a polypeptide having an unnatural structure at the N-terminus via a biosynthetic process by translation of amino acid sequence information encoded by a nucleic acid. A polypeptide having any amino acid at the N-terminus is synthesized by using an ARS ribozyme that catalyzes the acylation of tRNA with any amino acid to attach any amino acid to an initiator tRNA, thereby initiating a translation with the initiator tRNA.

    摘要翻译: 本发明旨在通过生物合成方法通过翻译由核酸编码的氨基酸序列信息在N末端合成具有非天然结构的多肽。 通过使用催化tRNA与任何氨基酸酰化以将任何氨基酸连接至引发剂tRNA的ARS核酶合成在N末端具有任何氨基酸的多肽,从而开始与引发剂tRNA的翻译。

    NOVEL ARTIFICIAL TRANSLATION/SYNTHESIS SYSTEM
    4.
    发明申请
    NOVEL ARTIFICIAL TRANSLATION/SYNTHESIS SYSTEM 有权
    新人工翻译/合成系统

    公开(公告)号:US20130217599A1

    公开(公告)日:2013-08-22

    申请号:US13816911

    申请日:2011-08-26

    IPC分类号: C12P21/00

    CPC分类号: C12P21/00 C12N15/67 C12P21/02

    摘要: A new artificial translation-synthesis system of adding tRNAs binding special amino acids to the in vitro translation system and synthesizing peptides with special amino acids incorporated thereto according to a dual genetic code table and an artificial codon box division.

    摘要翻译: 一种新的人工翻译 - 合成系统,其将特异性氨基酸结合到体外翻译系统中并根据双重遗传密码表和人造密码子分组合成具有特异氨基酸的肽。

    METHODS FOR RIBOSOMAL SYNTHESIS OF POLYPEPTIDES CONTAINING UNNATURAL N-TERMINAL GROUPS AND APPLICATIONS THEREOF
    5.
    发明申请
    METHODS FOR RIBOSOMAL SYNTHESIS OF POLYPEPTIDES CONTAINING UNNATURAL N-TERMINAL GROUPS AND APPLICATIONS THEREOF 有权
    含有未知N末端组的多肽的RIBOSOMAL合成方法及其应用

    公开(公告)号:US20110275119A1

    公开(公告)日:2011-11-10

    申请号:US12515074

    申请日:2007-11-13

    IPC分类号: C12P21/00 C12N9/10

    CPC分类号: C12N15/67 C12P21/02

    摘要: The present invention aims to synthesize a polypeptide having an unnatural structure at the N-terminus via a biosynthetic process by translation of amino acid sequence information encoded by a nucleic acid. A polypeptide having any amino acid at the N-terminus is synthesized by using an ARS ribozyme that catalyzes the acylation of tRNA with any amino acid to attach any amino acid to an initiator tRNA, thereby initiating a translation with the initiator tRNA.

    摘要翻译: 本发明旨在通过生物合成方法通过翻译由核酸编码的氨基酸序列信息在N末端合成具有非天然结构的多肽。 通过使用催化tRNA与任何氨基酸酰化以将任何氨基酸连接至引发剂tRNA的ARS核酶合成在N末端具有任何氨基酸的多肽,从而开始与引发剂tRNA的翻译。

    PROCESS FOR SYNTHESIZING CYCLIC PEPTIDE COMPOUND
    6.
    发明申请
    PROCESS FOR SYNTHESIZING CYCLIC PEPTIDE COMPOUND 有权
    合成环化合物的方法

    公开(公告)号:US20100168380A1

    公开(公告)日:2010-07-01

    申请号:US12593221

    申请日:2008-03-26

    IPC分类号: C07K1/00 C12P21/00

    摘要: The objective is to provide a novel process for synthesizing a cyclic peptide compound. It is also an objective to provide a novel cyclic peptide compound. The novel process for synthesizing a cyclic peptide compound comprises the steps of: (1) translationally synthesizing a non-cyclic peptide compound having in a molecule a functional group 1 and a functional group 2, which are a pair of functional groups capable of reacting to form a bond, and (2) cyclizing the non-cyclic peptide compound by the reaction of the functional groups 1 and 2 to form a bond. The novel cyclic peptide compound can be synthesized by the process.

    摘要翻译: 目的是提供一种合成环肽化合物的新方法。 提供新的环肽化合物也是目的。 用于合成环肽化合物的新方法包括以下步骤:(1)在分子中转化合成具有官能团1和官能团2的能够对 形成键,和(2)通过官能团1和2的反应使非环肽化合物环化以形成键。 可以通过该方法合成新的环肽化合物。

    Process for synthesizing cyclic peptide compound
    8.
    发明授权
    Process for synthesizing cyclic peptide compound 有权
    环肽化合物的合成方法

    公开(公告)号:US09090668B2

    公开(公告)日:2015-07-28

    申请号:US12593221

    申请日:2008-03-26

    摘要: The objective is to provide a novel process for synthesizing a cyclic peptide compound. It is also an objective to provide a novel cyclic peptide compound. The novel process for synthesizing a cyclic peptide compound comprises the steps of: (1) translationally synthesizing a non-cyclic peptide compound having in a molecule a functional group 1 and a functional group 2, which are a pair of functional groups capable of reacting to form a bond, and (2) cyclizing the non-cyclic peptide compound by the reaction of the functional groups 1 and 2 to form a bond. The novel cyclic peptide compound can be synthesized by the process.

    摘要翻译: 目的是提供一种合成环肽化合物的新方法。 提供新的环肽化合物也是目的。 用于合成环肽化合物的新方法包括以下步骤:(1)在分子中转化合成具有官能团1和官能团2的非环状肽化合物,所述官能团是能够使 形成键,和(2)通过官能团1和2的反应使非环肽化合物环化以形成键。 可以通过该方法合成新的环肽化合物。

    Inhibitors
    9.
    发明申请
    Inhibitors 审中-公开
    抑制剂

    公开(公告)号:US20070037841A1

    公开(公告)日:2007-02-15

    申请号:US10547234

    申请日:2004-02-26

    IPC分类号: A61K31/4745 C07D471/02

    CPC分类号: C07D471/04

    摘要: An inhibitor contains naphthyridine dimer, a naphthyridine-azaquinolone hybrid, a trinaphthyridine-azaquinolone hybrid, or a trinaphthyridine-azaquinolone hybrid derivative. In order to inhibit binding of 100 nM of RRE to 100 nM of Rev protein, for example, an inhibitor containing naphthyridine dimer is used at a molarity of 1.2 μM to 12 μM, an inhibitor containing the naphthyridine-azaquinolone hybrid is used at a molarity of 2 μM to 20 μM, or an inhibitor containing the trinaphthyridine-azaquinolone hybrid derivative is used at a molarity of 200 nM to 2 μM. This makes it possible to effectively inhibit binding of RRE to Rev protein.

    摘要翻译: 抑制剂含有萘啶二聚体,萘啶 - 氮杂喹诺酮杂环,三萘啶 - 氮杂喹诺酮杂环或三萘并氮杂喹啉酮杂合衍生物。 为了抑制100nM的RRE与100nM的Rev蛋白的结合,例如,使用含有萘啶二聚体的抑制剂,摩尔浓度为1.2μM至12μM,含有萘啶 - 氮杂喹诺酮杂化物的抑制剂的摩尔浓度 或者含有三萘并氮杂喹啉酮杂化衍生物的抑制剂的摩尔浓度为200nM至2μM。 这使得有可能有​​效地抑制RRE与Rev蛋白的结合。