Enhancing delivery of large neutral amino acid drugs
    4.
    发明授权
    Enhancing delivery of large neutral amino acid drugs 失效
    加强大中性氨基酸药物的输送

    公开(公告)号:US5695751A

    公开(公告)日:1997-12-09

    申请号:US531586

    申请日:1995-09-21

    Abstract: L-amino acid oxidase is utilized to reduce the plasma level of large neutral amino acids to allow the opportunity of increased large neutral amino acid drug transport across the blood brain barrier. Preferably anti L-amino acid oxidase antibody is administered intermediate to the L-amino acid oxidase and large neutral amino acid drug administrations to deplete L-amino acid oxidase activity once the L-amino acid oxidase has caused the large neutral amino acid drug transport improving level plasma reduction of large neutral amino acids thereby to reduce or eliminate degrading of large neutral amino acid drugs by L-amino acid oxidase. The large neutral amino acid drugs include levodopa, melphalan, L-DON, azaserine, acivicin, L-alanosine and 3-(phosphonomethyl)phenylalanines. For treatment of brain tumors, the drug administration is preferably preceded by the administration of a large neutral amino acid glutathione depleting agent, e.g., L-buthionine-SR-sulfoximine. L-Amino acid oxidase is also utilized to enhance the transport of large neutral amino acid glutathione depleting agent across the blood brain barrier as an adjunct to radiation therapy of brain tumors.

    Abstract translation: 利用L-氨基酸氧化酶来降低大的中性氨基酸的血浆水平,以允许增加大的中性氨基酸药物在血脑屏障上的转运的机会。 优选地,抗L-氨基酸氧化酶抗体在L-氨基酸氧化酶和大的中性氨基酸药物给药中间给药,以在L-氨基酸氧化酶引起大的中性氨基酸药物转运改善后消耗L-氨基酸氧化酶活性 从而降低或消除大中性氨基酸药物由L-氨基酸氧化酶的降解。 大的中性氨基酸药物包括左旋多巴,美法仑,L-DON,重氮丝氨酸,acivicin,L-脯氨酸和3-(膦酰基甲基)苯丙氨酸。 为了治疗脑肿瘤,药物给药优选之前是施用大量中性氨基酸谷胱甘肽消耗剂,例如L-丁硫氨酸-SR-亚砜亚胺。 L-氨基酸氧化酶还用于增强大中性氨基酸谷胱甘肽消耗剂在血脑屏障上的转运,作为脑肿瘤放射治疗的辅助物质。

    Preparation of L-amino acid deaminase mutant and application thereof

    公开(公告)号:US11781118B2

    公开(公告)日:2023-10-10

    申请号:US17351318

    申请日:2021-06-18

    CPC classification number: C12N9/0022 C12P7/40 C12Y104/03002

    Abstract: The disclosure discloses preparation of an L-amino acid deaminase mutant and application thereof, belonging to the technical field of gene engineering. Through pmirLAAD protein modification, analysis of a flexible loop structure around a binding site of the pmirLAAD product, and design of the best mutant, the modification method of the disclosure overcomes the defect that the catalytic efficiency of the previous wild-type enzyme is reduced due to product inhibition, and is tested by experiments. Compared with the control, the catalytic efficiency (1.61 mM−1·min−1) and the product inhibition constant (5.4 mM) of the finally obtained best mutant pmirLAADM4 are respectively increased by 5.2 times and 5.7 times. The yield of α-ketoisovaleric acid can reach 96.5 g/L, and the transformation rate is greater than 97%. By adopting the method of the disclosure, the cost can be greatly reduced, and the industrialization process of production of α-ketoisovaleric acid by an enzymatic transformation method is accelerated.

    Enzymatic powder milk
    8.
    发明授权
    Enzymatic powder milk 失效
    酶粉奶

    公开(公告)号:US4617190A

    公开(公告)日:1986-10-14

    申请号:US644395

    申请日:1984-08-27

    Abstract: Aqueous reconstitutible, powder milk incorporates an enzyme system for providing a bacteriostatic effect upon aqueous reconstitution. The enzyme system contains (a) oxidoreductase enzyme that is hydro-interactable with and specific to oxidizable substrate in the powder milk for producing hydrogen peroxide and (b) peroxidatic peroxidase for interacting with the hydrogen peroxide and oxidizable anion from the powder milk to produce, in the reconstituted milk, oxidized anionic bacterial inhibitor. In an illustrative embodiment, powder milk incorporates (a) glucose oxidase that interacts with glucose in powder milk, upon aqueous dilution, to produce hydrogen peroxide and (b) lactoperoxidase for interacting with hydrogen peroxide and, for example the chloride ion from the powder milk to produce, in the reconstituted milk, the hypochlorite ion, a bacterial inhibitor.

    Abstract translation: 水性可重构的粉末奶结合了一种酶系统,用于在水重构时提供抑菌作用。 酶系统包含(a)氧化还原酶,其与用于产生过氧化氢的粉末乳中可氧化底物水合相互作用和特异性氧化还原酶,和(b)过氧化物过氧化物酶与来自粉末奶的过氧化氢和可氧化阴离子相互作用, 在复原乳中,氧化阴离子细菌抑制剂。 在一个示例性实施方案中,粉末奶合并(a)在水性稀释时与粉末状乳中的葡萄糖相互作用的葡萄糖氧化酶,以产生过氧化氢,和(b)与过氧化氢相互作用的乳过氧化物酶,例如来自粉末奶的氯离子 在再生牛奶中产生次氯酸根离子,即细菌抑制剂。

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