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公开(公告)号:US20160215019A1
公开(公告)日:2016-07-28
申请号:US15015208
申请日:2016-02-04
发明人: Moshe OREN , Varda Rotter , Perry Tal
IPC分类号: C07K7/06
摘要: 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.
摘要翻译: 本发明提供可以有效和特异地重新激活p53突变体的肽,以及允许以精确,成本和时间有效的方式鉴定,选择和分离这些肽的方法。 特别地,提供突变型p53再激活肽,其可以恢复突变型p53蛋白质的天然野生型p53折叠,并因此恢复肿瘤抑制活性。 这样的肽可用于治疗其中p53突变的各种病症和疾病。
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2.
公开(公告)号:US20190048053A1
公开(公告)日:2019-02-14
申请号:US16074086
申请日:2017-02-03
发明人: Varda ROTTER , Moshe OREN , Perry TAL , Shay EIZENBERGER , Avi BEN-SHIMON
摘要: 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:US20160166582A1
公开(公告)日:2016-06-16
申请号:US15050502
申请日:2016-02-23
发明人: Irina LAVELIN , Varda ROTTER , Moshe OREN , Ami NAVON , Zvi KAM , Benjamin GEIGER
IPC分类号: A61K31/555 , G01N33/50 , C07K14/47 , A61K31/522 , A61K31/47
CPC分类号: A61K31/555 , A61K31/47 , A61K31/52 , A61K31/522 , A61K31/60 , A61K33/34 , C07K14/4746 , C07K2319/40 , C07K2319/60 , C12N9/6421 , C12Y304/25001 , G01N33/5035
摘要: 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.
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公开(公告)号:US20230127559A1
公开(公告)日:2023-04-27
申请号:US17911277
申请日:2021-03-15
发明人: Varda ROTTER , Moshe OREN , Perry TAL , Fernando ALBERICIO
摘要: Peptide analogs which are endowed with the property of at least partially reactivating a mutant p53 protein are provided. Also provided are uses thereof in the treatment of diseases associated with mutant p53.
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公开(公告)号:US20180057533A1
公开(公告)日:2018-03-01
申请号:US15796811
申请日:2017-10-29
发明人: Moshe OREN , Varda ROTTER , Perry TAL
摘要: 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:US20220251159A1
公开(公告)日:2022-08-11
申请号:US17549369
申请日:2021-12-13
发明人: Varda ROTTER , Moshe OREN , Perry TAL , Shay EIZENBERGER , Avi BEN-SHIMON
摘要: 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:US20200095282A1
公开(公告)日:2020-03-26
申请号:US16704010
申请日:2019-12-05
发明人: Moshe OREN , Varda ROTTER , Perry TAL
摘要: 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:US20190315804A1
公开(公告)日:2019-10-17
申请号:US16451081
申请日:2019-06-25
发明人: Moshe OREN , Varda ROTTER , Perry TAL
摘要: 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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