摘要:
The present invention relates to polyethylene glycol (PEG) modified protein drugs, and a PEGylated tissue kallikrein, a preparation method and use thereof are disclosed. The tissue kallikrein has a sequence as shown in SEQ ID No. 1 or SEQ ID No. 2, and the tissue kallikrein may be natural or recombinant. The PEG has a molecular weight of 20 to 40 kDa, and is conjugated to the N-terminal primary amino of the tissue kallikrein. In addition to the advantages of significantly extended half-life, significantly reduced immunogenicity and stable and uniform structure, the biological activity of the PEGylated KLK1 provided in the present invention is improved to a higher extent, which is more significant in the treatment of cerebral apoplexy and diabetic nephropathy in particular.
摘要翻译:本发明涉及聚乙二醇(PEG)改性蛋白质药物和聚乙二醇化组织激肽释放酶,其制备方法和用途被公开。 组织激肽释放酶具有SEQ ID No.1或SEQ ID No.2所示的序列,组织激肽释放酶可以是天然的或重组的。 PEG具有20至40kDa的分子量,并且与组织激肽释放酶的N-末端的初级氨基缀合。 除了显着延长半衰期,免疫原性显着降低和结构稳定均匀的优点外,本发明提供的聚乙二醇化KLK1的生物活性也提高到更高程度,这在治疗脑中风中更为显着 特别是糖尿病肾病。
摘要:
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor X and factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of reversing anticoagulation, stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
摘要:
Embodiments of the present invention relate to compositions and methods of treating patients for type 1 diabetes mellitus (T1D) by administering a therapeutically effective dose of recombinant human KLK1, variants of KLK1, or active fragments thereof. Such patients may be increase risk patients for developing T1D or T1D patients in the Honeymoon Phase. Such treatment may be expected to prevent or delay the onset of T1D, to ameliorate the symptoms of T1D, or to ameliorate the extent to which the T1D manifests.
摘要:
This document provides methods and materials involved in modulating a cell's ability to be resistant to apoptosis. For example, methods and materials for exposing cells to KLK6 polypeptides, or increased KLK6 polypeptide activity, to promote resistance to apoptosis are provided. In addition, methods and materials for reducing the ability of KLK6 polypeptides to promote resistance to apoptosis are provided.
摘要:
The present invention relates to pharmaceutical compositions comprising glandular kallikrein in combination with myelin basic protein or copaxone for use in the treatment of multiple sclerosis. The present invention further relates to a method of suppressing autoimmune responses in a patient afflicted with or suffering at least one clinical sign of multiple sclerosis, comprising administering to said patient a therapeutically effective amount of glandular kallikrein in combination with a therapeutically effective amount of myelin basic protein or copaxone.
摘要:
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor X and factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of reversing anticoagulation, stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
摘要:
The invention relates to pharmaceutical compositions comprising tissue kallikrem (TK), and optionally a diabetes drug, a method of screening for a metabolic disorder by determining the concentration of TK and insulin in a biological sample from a test subject, a method of screening for a therapeutic agent for the treatment or prevention of a metabolic disorder, and a method for treating or preventing a metabolic disorder using a pharmaceutical composition comprising TK.
摘要:
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
摘要:
Compositions and methods for regulating angiogenesis wherein the compositions comprise cancer markers are provided. Serine proteases and kallikreins exhibit potent antiangiogenic activity on human and other animal cells, particularly endothelial cells. More particularly, the use of a cancer marker, such as PSA, CEA, HCG, NSE, or CA19-9, to inhibit or ameliorate angiogenesis and angiogenesis-related diseases such as cancer, arthritis, macular degeneration, and diabetic retinopathy is disclosed.
摘要:
The present invention relates to methods of treating cancer using a combination of a compound which is a PSA conjugate and a compound which is a inhibitor of angiogenesis, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is a PSA conjugate and a compound which is a inhibitor of angiogenesis. The invention also relates to methods of preparing such compositions.