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    Allergoids Derived from Allergens
    22.
    发明申请
    Allergoids Derived from Allergens 审中-公开
    过敏原衍生的过敏原

    公开(公告)号：US20120114699A1

    公开(公告)日：2012-05-10

    申请号：US13059597

    申请日：2009-10-02

    Applicant: Giovanni Mistrello ,  Daniela Roncarolo ,  Dario Zanoni ,  Stefania Zanotta ,  Paolo Falagiani ,  Pietro Falagiani

    Inventor： Giovanni Mistrello ,  Daniela Roncarolo ,  Dario Zanoni ,  Stefania Zanotta ,  Paolo Falagiani ,  Pietro Falagiani

    IPC: A61K39/35 ,  C07K14/77 ,  A61P37/08 ,  C07K1/34 ,  C07K1/107 ,  C07K14/435 ,  C07K14/415

    CPC classification number: C07K1/1077 ,  A61K39/35 ,  A61K39/36 ,  A61K2039/55566 ,  C07K14/415 ,  C07K14/435 ,  C07K17/02

    Abstract: Modified allergens having reduced allergenicity compared to corresponding native allergenic material, wherein all or a part of the primary amine groups of the lysine and arginine residues of the allergenic molecules are functionalized and the modified allergens have the structure wherein R and R2 are independently selected from H, C1-C5 alkyl, phenyl, phenyl substituted in ortho, meta, or para with a hydroxy, C1-C4 alkoxy, halogen, amino, alkylamino, dialkylamino, mercapto, C1-C4 alkylmercapto group; X represents O, S, or NR3, where R3 is H, alkyl with 1-6 carbon atoms, phenyl, or CN; R1 represents H, alkyl with 1-8 carbon atoms, phenyl or arylalkyl with up to 8 carbon atoms, or alkyl containing a heterocyclic ring; prot represents the protein residue of the allergen; n is the number of functionalized arginine groups and ranges between 1 and the number of arginine groups present in the allergen; m is the number of functionalized lysine groups and ranges between 1 and the number of lysine groups present in the allergen.

    Abstract translation: 与相应的天然变应原材料相比具有降低的过敏原性的改性过敏原，其中过敏原分子的赖氨酸和精氨酸残基的全部或部分伯胺基团被官能化，并且经修饰的变应原具有其中R和R 2独立地选自H C 1 -C 4烷基，苯基，在邻，间或对位与羟基，C 1 -C 4烷氧基，卤素，氨基，烷基氨基，二烷基氨基，巯基，C 1 -C 4烷基巯基取代的苯基; X表示O，S或NR 3，其中R 3是H，具有1-6个碳原子的烷基，苯基或CN; R1表示H，具有1-8个碳原子的烷基，具有至多8个碳原子的苯基或芳基烷基，或含有杂环的烷基; prot代表过敏原的蛋白质残基; n是官能化精氨酸基团的数目，范围在1和存在于变应原中的精氨酸基团数之间; m是功能化赖氨酸的数目，范围介于1和存在于变应原中的赖氨酸的数目之间。

    Methods and Reagents for Preparing Multifunctional Probes
    24.
    发明申请
    Methods and Reagents for Preparing Multifunctional Probes 有权
    制备多功能探针的方法和试剂

    公开(公告)号：US20110159566A1

    公开(公告)日：2011-06-30

    申请号：US13054364

    申请日：2009-07-15

    Applicant: Lee Josephson ,  Elisabeth Garanger

    Inventor： Lee Josephson ,  Elisabeth Garanger

    IPC: C12N9/96 ,  C07K1/107

    CPC classification number: C07K17/02 ,  G01N33/531 ,  G01N33/532

    Abstract: Multifunctional probes are synthesized in a single step using peptide scaffold-based multifunctional single-attachment-point reagents. To obtain multifunctional probes using the methods of the invention, a substrate (e.g., a nanoparticle, polymer, antibody, protein, low molecular weight compound, drug, etc.) is reacted with a multifunctional single-attachment-point (MSAP) reagent. The MSAP reagents can include three components: (i) a peptide scaffold, (ii) a single chemically reactive group on the peptide scaffold for reaction of the MSAP with a substrate having a complementary reactive group, and (iii) multiple functional groups on the peptide scaffold. The peptide scaffold can include any number of residues; however, for ease of synthesis and reproducibility in clinical trials, it is preferred to limit the residues in the peptide to 20 or less. The reagent can be prepared to yield a predetermined stoichiometric ratio of the functional groups on the scaffold such that the probe has a fixed stoichiometric ratio of the functional groups.

    Abstract translation: 多功能探针使用基于肽支架的多功能单连接点试剂在一个步骤中合成。 为了使用本发明的方法获得多功能探针，将底物（例如纳米颗粒，聚合物，抗体，蛋白质，低分子化合物，药物等）与多功能单连接点（MSAP）试剂反应。 MSAP试剂可以包括三个组分：（i）肽支架，（ii）肽支架上的单个化学反应性基团，用于使MSAP与具有互补反应性基团的底物反应，和（iii）多个官能团 肽支架。 肽支架可以包括任何数量的残基; 然而，为了便于在临床试验中的合成和再现性，优选将肽中的残基限制在20以下。 可以制备试剂以产生支架上官能团的预定化学计量比，使得探针具有官能团的固定化学计量比。

    Template-directed assembly of receptor signaling complexes
    30.
    发明申请
    Template-directed assembly of receptor signaling complexes 有权
    受体信号传导复合物的模板指导装配

    公开(公告)号：US20100121038A1

    公开(公告)日：2010-05-13

    申请号：US12653507

    申请日：2009-12-14

    Applicant: Robert M. Weis ,  Anthony L. Shrout ,  David J. Montefusco

    Inventor： Robert M. Weis ,  Anthony L. Shrout ,  David J. Montefusco

    IPC: C07K14/47

    CPC classification number: C07K17/02 ,  C07K14/195 ,  C07K14/245

    Abstract: Transmembrane receptors in the signaling pathways of bacterial chemotaxis systems influence cell motility by forming noncovalent complexes with the cytoplasmic signaling proteins to regulate their activity. The requirements for receptor-mediated activation of CheA, the principal kinase of the Escherichia coli chemotaxis signaling pathway, can be demonstrated using self-assembled clusters of a receptor fragment (CF) derived from the cytoplasmic domain of the aspartate receptor, Tar. Histidine-tagged Tar CF can be assembled on the surface of unilamellar vesicles via a lipid containing the Nickel-nitrilotriacetic acid moiety as a headgroup. The stability of such a complex can be controlled by the properties of the template including the size and composition, which can be used, for example, to vary the 2-dimensional concentration of receptor fragments. Surface-assembled CF is also found to serve as a substrate for receptor methylation, which is catalyzed by the receptor transferase. Since neither CheA activation nor CF methylation is observed in comparable samples in the absence of vesicles, it is concluded that surface-templating generates the organization among CF subunits required for biochemical activity.

    Abstract translation: 细菌趋化系统信号通路中的跨膜受体通过与细胞质信号蛋白形成非共价复合物来调节其活性来影响细胞运动性。 使用来自天冬氨酸受体Tar的细胞质结构域的受体片段（CF）的自组装簇可以证明对受体介导的活化CheA（对大肠杆菌趋化性信号通路的主要激酶）的活化的要求。 组氨酸标记的焦油CF可以通过含有镍 - 次氮基三乙酸部分作为头组的脂质组装在单层囊泡的表面上。 这种复合物的稳定性可以通过包括尺寸和组成的模板的性质来控制，其可以用于例如改变受体片段的2维浓度。 还发现表面组装的CF用作受体甲基化的底物，其由受体转移酶催化。 由于在不存在囊泡的可比较样品中既没有观察到CheA活化也没有观察到CF甲基化，因此得出结论，表面模板产生生化活性所需的CF亚基之间的组织。

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