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    • 3. 发明申请
    • BINDING-SITE MODIFIED LECTINS AND USES THEREOF
    • 绑定现场修改的条款及其用途
    • WO2010088261A1
    • 2010-08-05
    • PCT/US2010/022213
    • 2010-01-27
    • SMARTCELLS, INC.ZION, Todd, C.LANCASTER, Thomas, M.
    • ZION, Todd, C.LANCASTER, Thomas, M.
    • A01N45/00
    • C07K14/42A61K38/28A61K47/61A61K47/641A61K47/6415C07K14/4726G01N33/66G01N2333/4724
    • In one aspect, the disclosure provides cross-linked materials that include multivalent lectins with at least two binding sites for glucose, wherein the lectins include at least one covalently linked affinity ligand which is capable of competing with glucose for binding with at least one of said binding sites; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with glucose for binding with the lectins at said binding sites and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between lectins and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of glucose. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label.
    • 一方面,本公开提供了交联材料,其包括具有至少两个葡萄糖结合位点的多价凝集素,其中所述凝集素包括至少一个共价连接的亲和配体,其能与葡萄糖竞争与至少一个所述 结合位点 以及包含与缀合物框架结合的两个或更多个分离的亲和配体的缀合物,其中所述两个或更多个亲和配体与葡萄糖竞争与所述结合位点处的凝集素结合,并且其中缀合物在材料内交联, 在不同共轭物上的凝集素和亲和配体之间的共价相互作用。 这些材料被设计为响应于期望的葡萄糖浓度释放结合物的量。 取决于最终应用,在各种实施方案中,缀合物还可以包括药物和/或可检测标记。
    • 5. 发明申请
    • POLYNUCLEOTIDE APTAMER-BASED CROSS -LINKED MATERIALS AND USES THEREOF
    • 基于APTAMER的多晶交联材料及其用途
    • WO2010088276A2
    • 2010-08-05
    • PCT/US2010/022237
    • 2010-01-27
    • SMARTCELLS, INC.ZION, Todd, C.LANCASTER, Thomas, M.
    • ZION, Todd, C.LANCASTER, Thomas, M.
    • A61K48/00
    • C12N15/111A61K47/549C12N2310/16C12N2310/51
    • In one aspect, the disclosure provides cross-linked materials that include multivalent polynucleotide aptamers that bind a target molecule; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with the target molecule for binding with the aptamers and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between aptamers and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of the target molecule. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label. The drug, detectable label and affinity ligands may be covalently or non-covalently bound to the conjugate framework.
    • 一方面,本公开提供交联材料,其包括结合目标分子的多价多核苷酸适体; 以及包含与缀合物框架结合的两个或更多个分离的亲和配体的缀合物,其中所述两个或更多个亲和配体与靶分子竞争与适配体结合,并且其中结合物由于非共价键而在材料内交联 适体与亲和配体在不同共轭物上的相互作用。 这些材料被设计成响应于目标分子的所需浓度释放结合物的量。 根据最终应用,在各种实施方案中,缀合物还可以包括药物和/或可检测标记。 药物,可检测的标记和亲和配体可以共价或非共价结合到缀合物框架。
    • 8. 发明申请
    • RECOMBINANTLY EXPRESSED INSULIN POLYPEPTIDES AND USES THEREOF
    • 重组表达的胰岛素多肽及其用途
    • WO2012015692A2
    • 2012-02-02
    • PCT/US2011/045008
    • 2011-07-22
    • SMARTCELLS, INC.LANCASTER, Thomas, M.MURIKIPUDI, SylajaLALEAU, RassolZION, Todd, C.
    • LANCASTER, Thomas, M.MURIKIPUDI, SylajaLALEAU, RassolZION, Todd, C.
    • C07K14/62
    • C07K14/62A61K38/28
    • The present disclosure provides recombinantly expressed insulin polypeptides that comprise an N-linked glycan motif. The N-linked glycan motif is not present in wild-type insulins and enables the recombinant expression of glycosylated insulin polypeptides (e.g., in yeast cells). Based on results obtained with synthetic glycosylated insulin conjugates we predict that when these recombinant glycosylated insulin polypeptides are administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the glycosylated insulin polypeptide will be sensitive to serum concentrations of glucose (or an exogenous saccharide such as alpha-methyl mannose). Exemplary insulin polypeptides, polynucleotides encoding these insulin polypeptides, glycosylated insulin polypeptides, pharmaceutical formulations and sustained release formulations are provided in addition to methods of use and preparation.
    • 本公开提供了包含N-连接的聚糖基序的重组表达的胰岛素多肽。 N-连接的聚糖基序不存在于野生型胰岛素中并且能够重组表达糖基化胰岛素多肽(例如在酵母细胞中)。 基于用合成糖基化胰岛素缀合物获得的结果,我们预测当将这些重组糖基化胰岛素多肽施用于哺乳动物时,糖基化胰岛素多肽的至少一种药代动力学或药效学性质将对血清葡萄糖浓度(或外源糖类 作为α-甲基甘露糖)。 除了使用和制备方法外,还提供了示例性的胰岛素多肽,编码这些胰岛素多肽的多核苷酸,糖基化的胰岛素多肽,药物制剂和缓释制剂。
    • 10. 发明申请
    • RECOMBINANT LECTINS, BINDING-SITE MODIFIED LECTINS AND USES THEREOF
    • 重组蛋白,结合位点修饰的蛋白及其用途
    • WO2012015691A2
    • 2012-02-02
    • PCT/US2011/044989
    • 2011-07-22
    • SMARTCELLS, INC.LANCASTER, Thomas, M.BUTTERS, RobertCHOODNOVSKIY, Naomi, R.ZION, Todd, C.
    • LANCASTER, Thomas, M.BUTTERS, RobertCHOODNOVSKIY, Naomi, R.ZION, Todd, C.
    • C07K14/42
    • C07K14/42
    • In one aspect, the disclosure provides cross-linked materials that include multivalent lectins with at least two binding sites for glucose, wherein the lectins include at least one affinity ligand which is capable of competing with glucose for binding with at least one of said binding sites and is covalently linked to a cysteine residue of the lectins; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with glucose for binding with the lectins at said binding sites and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between lectins and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of glucose. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label.
    • 一方面,本公开提供了交联材料,其包括具有至少两个葡萄糖结合位点的多价凝集素,其中所述凝集素包括至少一种亲和配体,其能够与葡萄糖竞争与至少一个所述结合位点 并与凝集素的半胱氨酸残基共价连接; 以及包含与缀合物框架结合的两个或多个分离的亲和配体的缀合物,其中所述两个或更多个亲和配体与葡萄糖竞争与所述结合位点处的凝集素结合,并且其中缀合物在材料内交联, 在不同共轭物上的凝集素和亲和配体之间的共价相互作用。 这些材料被设计为响应于期望的葡萄糖浓度释放结合物的量。 根据最终应用,在各种实施方案中,缀合物还可以包括药物和/或可检测标记。