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    FRET-based mesoporous silica nanoparticles for real-time monitoring of drug release
    21.
    发明授权
    FRET-based mesoporous silica nanoparticles for real-time monitoring of drug release 有权
    基于FRET的介孔二氧化硅纳米粒子用于实时监测药物释放

    公开(公告)号：US09408918B1

    公开(公告)日：2016-08-09

    申请号：US14203559

    申请日：2014-03-10

    Applicant: Rutgers, The State University of New Jersey

    Inventor： Ki-Bum Lee ,  Jinping Lai ,  Birju Shah

    IPC: A61K47/00 ,  A61K47/40 ,  A61K47/02

    CPC classification number: A61K47/40 ,  A61K9/5115 ,  A61K41/0028 ,  A61K47/6923 ,  A61K49/0039 ,  G01N33/52

    Abstract: A compound comprising: (a) a drug carrier comprising coumarin-labeled-cysteine tethered mesoporous silica nanoparticles (MSNs) loaded with a pharmaceutically active agent, and (b) a fluorescein isothiocyanate-β-cyclodextrin (FITC-β-CD) covalently linked to said cysteine and blocking the release of said pharmaceutically active agent from said nanoparticles, wherein cleavage of said covalent linkage removes said cyclodextrin and releases said pharmaceutically active agent, and said coumarin and said fluorescin form a donor-acceptor pair so that said drug carrier has a first emission wavelength when the covalent linkage is intact and the cyclodextrin said present and a second emission wavelength after cleavage of said covalent linkage to remove said cyclodextrin and release said pharmaceutically active agent.

    Abstract translation: 一种化合物，其包含：（a）包含负载有药物活性剂的香豆素标记的半胱氨酸束缚介孔二氧化硅纳米颗粒（MSN）的药物载体，和（b）共价连接的异硫氰酸荧光素-β-环糊精（FITC-β-CD） 所述半胱氨酸并阻断所述药物活性剂从所述纳米颗粒的释放，其中所述共价键的切割除去所述环糊精并释放所述药物活性剂，并且所述香豆素和所述荧光素形成供体 - 受体对，使得所述药物载体具有 当共价连接是完整的并且所述环糊精所述的第一发射波长和在所述共价键断裂之后的第二发射波长以除去所述环糊精并释放所述药物活性剂。

    Site-specific labeling of affinity tags in fusion proteins
    22.
    发明授权
    Site-specific labeling of affinity tags in fusion proteins 有权
    融合蛋白中亲和标签的位点特异性标记

    公开(公告)号：US09164099B2

    公开(公告)日：2015-10-20

    申请号：US13890137

    申请日：2013-05-08

    Applicant: LIFE TECHNOLOGIES CORPORATION

    Inventor： Kyle Gee ,  Aleksey Rukavishnikov ,  Courtenay Hart Kerndt ,  Richard Haugland ,  Wai-Yee Leung ,  Wayne Patton ,  Zhenjun Diwu

    IPC: G01N33/533 ,  C07D239/00 ,  C07F5/02 ,  G01N33/58 ,  A61K49/00 ,  C07D311/12 ,  C07D311/18

    CPC classification number: G01N33/52 ,  A61K49/0021 ,  A61K49/0039 ,  A61K49/0041 ,  A61K49/0052 ,  C07D311/12 ,  C07D311/16 ,  C07D311/18 ,  C07F5/022 ,  G01N33/533 ,  G01N33/582

    Abstract: The present invention provides methods and fluorescent compounds that facilitate detecting and labeling of a fusion protein by being capable of selectively binding to an affinity tag. The fluorescent compounds have the general formula A(B)n, wherein A is a fluorophore, B is a binding domain that is a charged chemical moiety, a protein or fragment thereof and n is an integer from 1-6 with the proviso that the protein or fragment thereof not be an antibody or generated from an antibody. The present invention provides specific fluorescent compounds and methods used to detect and label fusion proteins that contain a poly-histidine affinity tag. These compounds have the general formula A(L)m(B)n wherein A is a fluorophore, L is a linker, B is an acetic acid binding domain, m is an integer from 1 to 4 and n is an integer from 1 to 6. The acetic acid groups interact directly with the positively charged histidine residues of the affinity tag to effectively label and detect a fusion protein containing such an affinity tag when present in an acidic or neutral environment.

    Abstract translation: 本发明提供了通过能够选择性地结合亲和标签来促进融合蛋白的检测和标记的方法和荧光化合物。 荧光化合物具有通式A（B）n，其中A是荧光团，B是作为带电化学部分的结合结构域，其蛋白质或片段，n是1-6的整数，条件是 蛋白质或其片段不是抗体或从抗体产生。 本发明提供用于检测和标记含有多组氨酸亲和标签的融合蛋白的特异性荧光化合物和方法。 这些化合物具有通式A（L）m（B）n，其中A是荧光团，L是连接体，B是乙酸结合域，m是1至4的整数，n是1至 乙酸基团与亲和标签的带正电荷的组氨酸残基直接相互作用，以有效地标记和检测当存在于酸性或中性环境中时含有这种亲和标签的融合蛋白。

    PROCESS FOR PRODUCING RADIOHALOGENATED BIOCONJUGATES AND PRODUCTS THEREOF
    24.
    发明申请
    PROCESS FOR PRODUCING RADIOHALOGENATED BIOCONJUGATES AND PRODUCTS THEREOF 审中-公开
    生产放射性生物素化合物及其制品的方法

    公开(公告)号：US20130209361A1

    公开(公告)日：2013-08-15

    申请号：US13817785

    申请日：2011-08-12

    Applicant: Erik Arstad ,  Ran Yan

    Inventor： Erik Arstad ,  Ran Yan

    IPC: A61K51/04

    CPC classification number: A61K51/0453 ,  A61K49/0002 ,  A61K49/0039 ,  A61K49/0041 ,  A61K49/0058 ,  A61K51/1048 ,  A61K51/1093

    Abstract: The present invention relates to a new synthetic process in which an alkyne and an azide react to form a radioisotopic bioconjugate construct. The reaction is particularly useful for producing compounds for use in imaging and radiotherapy applications. The present invention also provides bioconjugate labels and further relates to the use of these compounds in diagnostic and therapeutic methods. In addition, the invention provides a related process for introducing a radioisotopic halogen atom into a terminal alkyne.

    Abstract translation: 本发明涉及一种新的合成方法，其中炔和叠氮化物反应形成放射性同位素生物缀合物构建体。 该反应对于制备用于成像和放射治疗应用的化合物特别有用。 本发明还提供了生物缀合物标记，并且还涉及这些化合物在诊断和治疗方法中的用途。 此外，本发明提供了将放射性同位素卤素原子引入末端炔烃的相关方法。

    METHOD FOR FLUORESCENTLY LABELING PROTEIN
    26.
    发明申请
    METHOD FOR FLUORESCENTLY LABELING PROTEIN 审中-公开
    荧光标记蛋白的方法

    公开(公告)号：US20110319603A1

    公开(公告)日：2011-12-29

    申请号：US13255431

    申请日：2010-03-10

    Applicant: Kazuya Kikuchi ,  Yuichirou Hori ,  Hideki Ueno

    Inventor： Kazuya Kikuchi ,  Yuichirou Hori ,  Hideki Ueno

    IPC: C07K14/00 ,  C12N15/63 ,  C07C245/04 ,  C07D249/04

    CPC classification number: C07K14/215 ,  A61K49/0039 ,  A61K49/0043 ,  A61K49/0045 ,  A61K49/0056 ,  C07D311/82 ,  C07D405/12 ,  C07D405/14 ,  C07K1/13 ,  G01N33/533

    Abstract: A method for fluorescently labeling a protein is provided that can also be used for labeling a biomolecule (a protein) in vivo with fluorescence. The method for fluorescently labeling a protein includes obtaining a fusion protein of a target protein to be labeled and, for example, a photoactive yellow protein (PYP), and fluorescently labeling the target protein by reacting the fusion protein with a compound represented by Formula (I), wherein in the compound represented by Formula (I), a coumarin skeleton in Formula (A) or a benzene skeleton in Formula (B) is intramolecnlarly associated with a group X and as a result, fluorescence derived from the group X is suppressed and when in the compound of Formula (I), the coumarin skeleton in Formula (A) or the benzene skeleton in Formula (B) is bound to the PYP or the PYP-derived protein contained in the fusion protein, the coumarin skeleton in Formula (A) or the benzene skeleton in Formula (B) is intramolecnlarly dissociated from the group X, and thereby fluorescence derived from the group X can be emitted.

    Abstract translation: 提供了荧光标记蛋白质的方法，其也可用于在体内用荧光标记生物分子（蛋白质）。 荧光标记蛋白质的方法包括获得要标记的靶蛋白质和例如光活性黄蛋白（PYP）的融合蛋白，并通过使融合蛋白与式（ I）表示的化合物，式（I）表示的化合物中，式（A）中的香豆素骨架或式（B）中的苯骨架与基团X进行内分子结合，结果，衍生自基团X的荧光 抑制，当式（I）的化合物中，式（A）中的香豆素骨架或式（B）中的苯骨架与所述融合蛋白中所含的PYP或PYP衍生的蛋白质结合时，所述香豆素骨架在 通式（A）或式（B）中的苯骨架从基团X离子解离，从而可以发射衍生自基团X的荧光。

    Compositions, probes and conjugates and uses thereof
    29.
    发明授权
    Compositions, probes and conjugates and uses thereof 有权
    组合物，探针和缀合物及其用途

    公开(公告)号：US08003771B2

    公开(公告)日：2011-08-23

    申请号：US12714983

    申请日：2010-03-01

    Applicant: Zbigniew Skrzypczynski ,  Sarah R Wayland

    Inventor： Zbigniew Skrzypczynski ,  Sarah R Wayland

    IPC: C07H21/00 ,  C07H21/04 ,  C07C247/00 ,  A61K31/41 ,  C12P13/06 ,  C12P13/02

    CPC classification number: C07H21/00 ,  A61K49/0039 ,  A61K49/0054

    Abstract: The present invention relates to compositions useful as probes and in other applications and methods of their use. In some embodiments, nucleotides are prepared and functionalized with dyes. In some embodiments a first molecule is functionalized with an alkynyl group, a second molecule is functionalized with an azide group, and said first and second molecules are mixed under conditions to form a conjugate with a 1,2,3-triazol group. In further embodiments, a nucleotide is functionalized with an alkynyl group, a dye is functionalized with an azide group, and mixing the nucleotide and the dye forms a conjugate capable of emitting light.

    Abstract translation: 本发明涉及可用作探针的组合物及其应用和使用方法。 在一些实施方案中，制备核苷酸并用染料官能化。 在一些实施方案中，第一分子用炔基官能化，第二分子用叠氮基官能化，并且所述第一和第二分子在条件下混合以形成具有1,2,3-三唑基团的缀合物。 在另外的实施方案中，核苷酸用炔基官能化，染料用叠氮化物官能化，并且混合核苷酸和染料形成能发光的共轭体。

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