COMPOUNDS FOR PROTEASOME ENZYME INHIBITION

    公开(公告)号:US20210179663A1

    公开(公告)日:2021-06-17

    申请号:US17169990

    申请日:2021-02-08

    摘要: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION
    3.
    发明申请
    COMPOUNDS FOR PROTEASOME ENZYME INHIBITION 审中-公开
    抗生素抑制剂的化合物

    公开(公告)号:US20140342977A1

    公开(公告)日:2014-11-20

    申请号:US14452844

    申请日:2014-08-06

    IPC分类号: C07K5/117

    摘要: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

    摘要翻译: 包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂(Ntn)水解酶的比活性。 具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。 例如,本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。 肽类化合物包括环氧化物或氮丙啶,并且在N-末端官能化。 除了其他治疗用途之外,预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

    COMPOUNDS FOR PROTEASOME
    10.
    发明申请

    公开(公告)号:US20200071356A1

    公开(公告)日:2020-03-05

    申请号:US16669601

    申请日:2019-10-31

    摘要: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.