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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。
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公开(公告)号：US09289433B2
公开(公告)日：2016-03-22
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 , A61K31/47 , A61K31/522 , A61K31/60 , A61K33/34 , C07K14/47 , C12N9/64 , G01N33/50 , A61K31/52
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。
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Patent Agency Ranking
公开(公告)号：US11230578B2
公开(公告)日：2022-01-25
申请号：US16074086
申请日：2017-02-03
Applicant: Yeda Research and Development Co. Ltd.
Inventor： Varda Rotter , Moshe Oren , Perry Tal , Shay Eizenberger , Avi Ben-Shimon
Abstract: An isolated peptide is provided. The peptide comprises an amino acid sequence arranged in a space and configuration that allow interaction of the peptide with the DNA Binding Domain (DBD) of p53 through at least one residue of the DBD by which pCAP 250 (SEQ ID NO: 1) binds the DBD, wherein the peptide at least partially reactivates a mutant p53 protein, with the proviso that the peptide is not SEQ ID NO: 59-382.
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公开(公告)号：US09856289B2
公开(公告)日：2018-01-02
申请号：US15015208
申请日：2016-02-04
Applicant: Yeda Research and Development Co. Ltd.
Inventor： Moshe Oren , Varda Rotter , Perry Tal
CPC classification number: C07K7/06 , A61K38/00 , A61K38/08 , A61K38/16 , C07K7/08 , C07K14/00 , C07K14/4746
Abstract: The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.
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公开(公告)号：US11028127B2
公开(公告)日：2021-06-08
申请号：US16704010
申请日：2019-12-05
Applicant: Yeda Research and Development Co. Ltd.
Inventor： Moshe Oren , Varda Rotter , Perry Tal
Abstract: The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.
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公开(公告)号：US10550152B2
公开(公告)日：2020-02-04
申请号：US16451081
申请日：2019-06-25
Applicant: Yeda Research and Development Co. Ltd.
Inventor： Moshe Oren , Varda Rotter , Perry Tal
Abstract: The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.
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公开(公告)号：US10336789B2
公开(公告)日：2019-07-02
申请号：US15796811
申请日：2017-10-29
Applicant: Yeda Research and Development Co. Ltd.
Inventor： Moshe Oren , Varda Rotter , Perry Tal
Abstract: The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.
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