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    Compound for use in peptide synthesis
    1.
    发明授权
    Compound for use in peptide synthesis 有权
    用于肽合成的化合物

    公开(公告)号：US09023957B2

    公开(公告)日：2015-05-05

    申请号：US13808303

    申请日：2011-07-06

    申请人： Chuan Fa Liu

    发明人： Chuan Fa Liu

    IPC分类号： C07K1/107 ,  C07K1/04 ,  C07C323/29 ,  C07K1/08

    CPC分类号： C07K1/1077 ,  C07C323/29 ,  C07K1/04 ,  C07K1/086

    摘要： The present invention generally relates to processes and methods of peptide and protein synthesis. The present invention also relates to specific compounds for use in such processes and methods. It is shown herein that peptides with a C-terminal tertiary N,N-bis(2-mercaptoethyl)-amide (BMEA) undergo N-to-S acyl transfer at weakly acidic pH to form a transient thioester which can be captured for direct ligation with a cysteinyl peptide. These C-terminal BMEA peptides are easily prepared with standard Fmoc solid-phase synthesis protocols, thus giving a very convenient access to the thioester components for native chemical ligation.

    摘要翻译： 本发明一般涉及肽和蛋白质合成的方法和方法。 本发明还涉及用于这些方法和方法的具体化合物。 在本文中显示，具有C末端叔N，N-双（2-巯基乙基） - 酰胺（BMEA）的肽在弱酸性pH下经历N-to-S酰基转移以形成可以直接捕获的瞬时硫酯 与半胱氨酰肽连接。 这些C末端BMEA肽可以用标准的Fmoc固相合成方案容易地制备，从而使得非常方便地获得用于天然化学连接的硫酯组分。

    COMPOUND FOR USE IN PEPTIDE SYNTHESIS
    2.
    发明申请
    COMPOUND FOR USE IN PEPTIDE SYNTHESIS 有权
    化合物用于肽合成

    公开(公告)号：US20130131286A1

    公开(公告)日：2013-05-23

    申请号：US13808303

    申请日：2011-07-06

    申请人： Chuan Fa Liu

    发明人： Chuan Fa Liu

    IPC分类号： C07K1/107

    CPC分类号： C07K1/1077 ,  C07C323/29 ,  C07K1/04 ,  C07K1/086

    摘要： The present invention generally relates to processes and methods of peptide and protein synthesis. The present invention also relates to specific compounds for use in such processes and methods. It is shown herein that peptides with a C-terminal tertiary N,N-bis(2-mercaptoethyl)-amide (BMEA) undergo N-to-S acyl transfer at weakly acidic pH to form a transient thioester which can be captured for direct ligation with a cysteinyl peptide. These C-terminal BMEA peptides are easily prepared with standard Fmoc solid-phase synthesis protocols, thus giving a very convenient access to the thioester components for native chemical ligation.

    摘要翻译： 本发明一般涉及肽和蛋白质合成的方法和方法。 本发明还涉及用于这些方法和方法的具体化合物。 在本文中显示，具有C末端叔N，N-双（2-巯基乙基） - 酰胺（BMEA）的肽在弱酸性pH下经历N-to-S酰基转移以形成可以直接捕获的瞬时硫酯 与半胱氨酰肽连接。 这些C末端BMEA肽可以用标准的Fmoc固相合成方案容易地制备，从而使得非常方便地获得用于天然化学连接的硫酯组分。

    Modulators of receptors for parathyroid hormone and parathyroid hormone-related protein
    6.
    发明授权
    Modulators of receptors for parathyroid hormone and parathyroid hormone-related protein 失效
    甲状旁腺激素和甲状旁腺激素相关蛋白受体的调节剂

    公开(公告)号：US06756480B2

    公开(公告)日：2004-06-29

    申请号：US09843221

    申请日：2001-04-26

    申请人： Paul Kostenuik ,  Chuan-Fa Liu ,  David Lee Lacey

    发明人： Paul Kostenuik ,  Chuan-Fa Liu ,  David Lee Lacey

    IPC分类号： C07K1600

    CPC分类号： C07K14/635 ,  A61K38/00 ,  A61K47/60 ,  A61K47/61 ,  A61K47/6425 ,  C07K2319/00

    摘要： The present invention concerns therapeutic agents that modulate the activity of PTH and PTHrP. In accordance with the present invention, modulators of PTH and PTHrP comprise: (a) a PTH/PTHrP modulating domain; and (b) a vehicle, such as a polymer (e.g., PEG or dextran) or an Fc domain, which is preferred; wherein the vehicle is covalently attached to the C-terminus of the PTH/PTHrP modulating domain. The vehicle and the PTH/PTHrP modulating domain may be linked through the N- or C-terminus of the PTH/PTHrP modulating domain, as described further below. The preferred vehicle is an Fc domain, and the preferred Fc domain is an IgG Fc domain. Preferred PTH/PTHrP modulating domains comprise the PTH and PTHrP-derived amino acid sequences described hereinafter. Other PTH/PTHrP modulating domains can be generated by phage display, RNA-peptide screening and the other techniques mentioned herein. Such peptides typically will be modulators of both PTH activity and PTHrP activity, although such techniques can be used to generate peptide sequences that serve as selective modulators (e.g., agonists of PTH activity but not PTHrP activity).

    摘要翻译： 本发明涉及调节PTH和PTHrP活性的治疗剂。 根据本发明，PTH和PTHrP的调节剂包括：（a）PTH / PTHrP调节结构域; 和（b）优选的载体，例如聚合物（例如PEG或葡聚糖）或Fc结构域;其中载体共价连接到PTH / PTHrP调节结构域的C末端。 载体和PTH / PTHrP调节结构域可以通过PTH / PTHrP调节结构域的N末端或C末端连接，如下文进一步描述的。 优选的载体是Fc结构域，优选的Fc结构域是IgG Fc结构域。 优选的PTH / PTHrP调节结构域包含下文描述的PTH和PTHrP衍生的氨基酸序列。 其他PTH / PTHrP调节结构域可以通过噬菌体展示，RNA-肽筛选和本文提及的其他技术产生。 尽管这样的技术可用于产生用作选择性调节剂的肽序列（例如，PTH活性的激动剂但不是PTHrP活性），但是这些肽通常将是PTH活性和PTHrP活性的调节剂。

    METHOD FOR MODIFICATION OF ORGANIC MOLECULES
    7.
    发明申请
    METHOD FOR MODIFICATION OF ORGANIC MOLECULES 有权
    有机分子修饰方法

    公开(公告)号：US20140316105A1

    公开(公告)日：2014-10-23

    申请号：US14116623

    申请日：2012-05-14

    申请人： Chuan-Fa Liu ,  Fupeng Li

    发明人： Chuan-Fa Liu ,  Fupeng Li

    IPC分类号： C07K1/113 ,  C07C233/05 ,  C07K14/00 ,  C07C69/533

    CPC分类号： C07K1/113 ,  C07C69/533 ,  C07C233/05 ,  C07C319/18 ,  C07D277/04 ,  C07D277/06 ,  C07K1/1077 ,  C07K14/00 ,  G01N2440/10 ,  G01N2440/12 ,  C07C323/41

    摘要： The present invention is directed to a method of alkylating a thiol group (R—S—H) or seleno group (R—Se—H) in a target molecule wherein the method comprises: reacting a target molecule comprising at least one thiol group with a compound of formula (I) or (II): wherein R is an acetyl group or any other acyl group or is a group comprising any one of: or wherein R in formula (II) can also be an alkyl group; and wherein R′ is selected from a group consisting of a hydrogen, a methyl group and an ethyl group.

    摘要翻译： 本发明涉及在目标分子中烷基化硫醇基（R-S-H）或硒基（R-Se-H）的方法，其中所述方法包括：将包含至少一个硫醇基的靶分子与 式（I）或（II）的化合物：其中R是乙酰基或任何其它酰基，或是包含以下任何一种的基团：或其中式（II）中的R也可以是烷基; 并且其中R'选自氢，甲基和乙基。