Enzyme-based approach to probe the specificity of heparanase and its inhibitor

基于酶的方法探测乙酰肝素酶及其抑制剂的特异性

• 批准号: 7808617
• 负责人: Sherket Breshon Peterson
• 金额: $ 3.22万
• 依托单位: UNIV OF NORTH CAROLINA CHAPEL HILL
• 依托单位国家: 美国
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-02-01 至 2013-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7808617
• 关键词: Acute Myelocytic Leukemia; Adverse effects; Affect; Animals; Baculoviruses; Beta-glucuronidase; Biological Process; Bladder; Brain; Breast; Cell Proliferation; Cleaved cell; Colon; Development; Disaccharides; Enzymes; Esophageal; Extracellular Matrix; Glucosamine; Glucosamine Sulfate; Glucuronic Acids; Glycoside Hydrolases; Goals; Heparan Sulfate Proteoglycan; Heparin; Heparitin Sulfate; Iduronic Acid; Immunologic Surveillance; Inflammatory; Inorganic Sulfates; Lead; Length; Link; Literature; Location; Malignant Neoplasms; Methods; Monosaccharides; Neoplasm Metastasis; Oligosaccharides; Oral; Pancreas; Pattern; Pattern Recognition; Phenotype; Physiological Processes; Play; Polysaccharides; Predisposition; Process; Role; Series; Specificity; Stomach; Structure; Substrate Specificity; Techniques; Thrombocytopenia; Transferase; Unspecified or Sulfate Ion Sulfates; Variant; Vertebral column; Wound Healing; angiogenesis; base; cancer therapy; design; heparanase; improved; inhibitor/antagonist; mimetics; novel; novel strategies; success; sulfation; sulfotransferase; tissue regeneration; tumor; tumor progression; tumorigenesis

DESCRIPTION (provided by applicant): The degradation of various constituents of the extracellular matrix including, heparan sulfate proteoglycans, represents a critical step in the process of cancer invasion and metastasis. Heparanase, an endo-p-D- glycosidase which degrades HS, has emerged as a promising target for the development of anti-cancer treatment because of its pro-metastatic, pro-inflammatory, and pro-angiogenic activity. Therefore we sought to utilize a novel enzymatic approach to probe the specificity of heparanase and its inhibitor.

描述（由申请人提供）：细胞外基质的各种成分（包括硫酸乙酰肝素蛋白聚糖）的降解代表了癌症侵袭和转移过程中的关键步骤。乙酰肝素酶是一种降解HS的内切-β-D-糖苷酶，由于其促转移、促炎症和促血管生成活性，已成为开发抗癌治疗的有希望的靶标。因此，我们试图利用一种新的酶的方法来探测乙酰肝素酶及其抑制剂的特异性。