会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明申请
    • Regulation of Metalloprotease Cleavage of Cell Surface Proteins
    • 金属蛋白酶切割细胞表面蛋白的调控
    • US20080317763A1
    • 2008-12-25
    • US11721949
    • 2005-12-19
    • Martin LackmannPeter W. JanesDimitar B. NikolovNayanendu Saha
    • Martin LackmannPeter W. JanesDimitar B. NikolovNayanendu Saha
    • A61K39/395C12N9/50C12N15/11C12N15/00C12N5/06A61P43/00C07K16/18C12Q1/37A61K38/43
    • A61K38/57C12N9/6489
    • Elucidation of the crystal structure of an ADAM10 substrate-recognition and proteinase-positioning module comprising the protein cysteine-rich and disintegrin domains, and detailed functional analysis revealed that an acidic pocket within the cysteine-rich domain forms a substrate-recognition site. The binding of this pocket to receptor/ligand complexes facilitates effective ligand cleavage, which is prevented when critical residues within the pocket are changed. This provides use of the surface pocket within the extracellular domain of ADAM10, and the corresponding structure in related proteases such as ADAM17, as a target for structure-based computational and high-throughput screens for small-molecule substrate-specific inhibitors or monoclonal antibodies that inhibit ADAM protease cleavage of ephrins and other ADAM10 or ADAM17 substrates. These inhibitors will be useful in therapeutic intervention of tumour development, invasion and metastasis and other diseases which involve the activity of the ADAM10 and ADAM17 proteases, such as inflammation, cardio-vascular disease, arthritis and other auto-immune diseases.
    • 阐明ADAM10底物识别和蛋白酶定位模块的晶体结构,其包含富含蛋白质的富含蛋白酶和去整合素结构域,以及详细的功能分析表明,富含半胱氨酸的结构域内的酸性口袋形成底物识别位点。 该口袋与受体/配体复合物的结合有助于有效的配体切割,这在口袋中的关键残基改变时被阻止。 这提供了ADAM10细胞外结构域中的表面袋的使用以及相关蛋白酶如ADAM17中相应的结构,作为用于小分子底物特异性抑制剂或单克隆抗体的基于结构的计算和高通量筛选的靶标 抑制ephrins和其他ADAM10或ADAM17底物的ADAM蛋白酶切割。 这些抑制剂可用于涉及ADAM10和ADAM17蛋白酶如炎症,心血管疾病,关节炎和其他自身免疫疾病的活动的肿瘤发展,侵袭和转移以及其他疾病的治疗性干预。
    • 7. 发明授权
    • Antibody against a human ADAM protease
    • 针对人ADAM蛋白酶的抗体
    • US07960513B2
    • 2011-06-14
    • US11721949
    • 2005-12-19
    • Martin LackmannPeter W. JanesDimitar B. NikolovNayanendu Saha
    • Martin LackmannPeter W. JanesDimitar B. NikolovNayanendu Saha
    • C07K16/40
    • A61K38/57C12N9/6489
    • Elucidation of the crystal structure of an ADAM10 substrate-recognition and proteinase-positioning module comprising the protein cysteine-rich and disintegrin domains, and detailed functional analysis revealed that an acidic pocket within the cysteine-rich domain forms a substrate-recognition site. The binding of this pocket to receptor/ligand complexes facilitates effective ligand cleavage, which is prevented when critical residues within the pocket are changed. This provides use of the surface pocket within the extracellular domain of ADAM10, and the corresponding structure in related proteases such as ADAM17, as a target for structure-based computational and high-throughput screens for small-molecule substrate-specific inhibitors or monoclonal antibodies that inhibit ADAM protease cleavage of ephrins and other ADAM10 or ADAM17 substrates. These inhibitors will be useful in therapeutic intervention of tumour development, invasion and metastasis and other diseases which involve the activity of the ADAM10 and ADAM17 proteases, such as inflammation, cardio-vascular disease, arthritis and other auto-immune diseases.
    • 阐明ADAM10底物识别和蛋白酶定位模块的晶体结构,其包含富含蛋白质的富含蛋白酶和去整合素结构域,以及详细的功能分析表明,富含半胱氨酸的结构域内的酸性口袋形成底物识别位点。 该口袋与受体/配体复合物的结合有助于有效的配体切割,这在口袋中的关键残基改变时被阻止。 这提供了ADAM10细胞外结构域中的表面袋的使用以及相关蛋白酶如ADAM17中相应的结构,作为用于小分子底物特异性抑制剂或单克隆抗体的基于结构的计算和高通量筛选的靶标 抑制ephrins和其他ADAM10或ADAM17底物的ADAM蛋白酶切割。 这些抑制剂可用于涉及ADAM10和ADAM17蛋白酶如炎症,心血管疾病,关节炎和其他自身免疫疾病的活动的肿瘤发展,侵袭和转移以及其他疾病的治疗性干预。