2024年3月12日发(作者：太史悦来)
专利内容由知识产权出版社提供
专利名称：COMPOSITIONS AND METHODS FOR
INDUCING CONFORMATIONAL CHANGES IN
CEREBLON AND OTHER E3 UBIQUITIN
LIGASES
发明人：CHAMBERLAIN, Philip Paul,CATHERS, Brian
Edwin,LOPEZ-GIRONA, Antonia
申请号：EP20207173.4
申请日：20150626
公开号：EP3827836A1
公开日：20210602
摘要：Provided herein are methods of identifying a test compound that induces a
CRBN conformational change or otherwise alters the properties of a CRBN surface as
defined herein, wherein conformational change or alteration has an effect on W380, W386
and/or W400 of the CRBN; has an effect on E377 of the CRBN; or has an effect on V388 of
the CRBN. Also provided is a method of inducing a CRBN conformational change or
otherwise altering the properties of a CRBN surface, comprising contacting the CRBN
with such a test compound. Also provided is a method of identifying a substrate
ubiquitinated by a E3 ubiquitination ligase complex comprising CRBN as defined herein,
wherein the method comprises contacting the CRBN with said text compound. Also
provided is a method of designing a test compound based on fit within CMA binding
pocket of CRBN as defined herein, wherein said conformational change has an effect on
W380, W386 and/or W400 of CRBN; has an effect on E377 of CRBN; or has an effect on
V388 of CRBN.
申请人：Celgene Corporation
地址：86 Morris Avenue Summit, NJ 07901 US
国籍：US
代理机构：Jones Day
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2024年3月12日发(作者：太史悦来)
专利内容由知识产权出版社提供
专利名称：COMPOSITIONS AND METHODS FOR
INDUCING CONFORMATIONAL CHANGES IN
CEREBLON AND OTHER E3 UBIQUITIN
LIGASES
发明人：CHAMBERLAIN, Philip Paul,CATHERS, Brian
Edwin,LOPEZ-GIRONA, Antonia
申请号：EP20207173.4
申请日：20150626
公开号：EP3827836A1
公开日：20210602
摘要：Provided herein are methods of identifying a test compound that induces a
CRBN conformational change or otherwise alters the properties of a CRBN surface as
defined herein, wherein conformational change or alteration has an effect on W380, W386
and/or W400 of the CRBN; has an effect on E377 of the CRBN; or has an effect on V388 of
the CRBN. Also provided is a method of inducing a CRBN conformational change or
otherwise altering the properties of a CRBN surface, comprising contacting the CRBN
with such a test compound. Also provided is a method of identifying a substrate
ubiquitinated by a E3 ubiquitination ligase complex comprising CRBN as defined herein,
wherein the method comprises contacting the CRBN with said text compound. Also
provided is a method of designing a test compound based on fit within CMA binding
pocket of CRBN as defined herein, wherein said conformational change has an effect on
W380, W386 and/or W400 of CRBN; has an effect on E377 of CRBN; or has an effect on
V388 of CRBN.
申请人：Celgene Corporation
地址：86 Morris Avenue Summit, NJ 07901 US
国籍：US
代理机构：Jones Day
更多信息请下载全文后查看