公开(公告)号：US20160166582A1

公开(公告)日：2016-06-16

申请号：US15050502

申请日：2016-02-23

Applicant: Yeda Research and Development Co. Ltd.

Inventor： Irina LAVELIN ,  Varda ROTTER ,  Moshe OREN ,  Ami NAVON ,  Zvi KAM ,  Benjamin GEIGER

IPC: A61K31/555 ,  G01N33/50 ,  C07K14/47 ,  A61K31/522 ,  A61K31/47

CPC classification number: A61K31/555 ,  A61K31/47 ,  A61K31/52 ,  A61K31/522 ,  A61K31/60 ,  A61K33/34 ,  C07K14/4746 ,  C07K2319/40 ,  C07K2319/60 ,  C12N9/6421 ,  C12Y304/25001 ,  G01N33/5035

Abstract: A method of treating a disease in which inhibiting of a proteasome is advantageous is provided. The method comprises administering to the subject a therapeutically effective amount of a compound which binds to a proteasome of a cell, the compound comprising a copper bound to a ligand, the ligand being configured such that upon binding to the proteasome, the copper interacts with cysteine 31 of a Beta2 subunit of the proteasome and further interacts with cysteine 118 of a Beta3 subunit of the proteasome, thereby treating the disease. Additional novel proteasome inhibitors are also provided as well as methods of identifying proteasome inhibitors.

公开(公告)号：US20130225547A1

公开(公告)日：2013-08-29

申请号：US13872247

申请日：2013-04-29

Applicant: Yeda Research and Development Co. Ltd.

Inventor： Irina LAVELIN ,  Varda Rotter ,  Moshe Oren ,  Ami Navon ,  Zvi Kam ,  Benjamin Geiger

IPC: A61K31/555 ,  A61K31/52 ,  G01N33/50 ,  A61K31/47

CPC classification number: A61K31/555 ,  A61K31/47 ,  A61K31/52 ,  A61K31/522 ,  A61K31/60 ,  A61K33/34 ,  C07K14/4746 ,  C07K2319/40 ,  C07K2319/60 ,  C12N9/6421 ,  C12Y304/25001 ,  G01N33/5035

Abstract: A method of treating a disease in which inhibiting of a proteasome is advantageous is provided. The method comprises administering to the subject a therapeutically effective amount of a compound which binds to a proteasome of a cell, the compound comprising a copper bound to a ligand, the ligand being configured such that upon binding to the proteasome, the copper interacts with cysteine 31 of a Beta2 subunit of the proteasome and further interacts with cysteine 118 of a Beta3 subunit of the proteasome, thereby treating the disease. Additional novel proteasome inhibitors are also provided as well as methods of identifying proteasome inhibitors.

Abstract translation: 提供了治疗其中抑制蛋白酶体的优点的疾病的方法。 该方法包括向受试者施用治疗有效量的结合细胞蛋白酶体的化合物，所述化合物包含与配体结合的铜，所述配体被配置为使得在结合蛋白酶体时，铜与半胱氨酸相互作用 31的蛋白酶体的β2亚基，并进一步与蛋白酶体的β3亚基的半胱氨酸118相互作用，从而治疗该疾病。 还提供了另外的新型蛋白酶体抑制剂以及鉴定蛋白酶体抑制剂的方法。