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eLife:合成和天然配体与核受体PPARγ的协同组合

2019-01-13 MedSci MedSci原创

过氧化物酶体增殖物激活受体γ(PPARγ)的晶体结构揭示了合成和天然/内源配体的重叠结合模式,表明对正位囊的竞争。在这里,我们显示合成配体与正位囊的结合可以将天然和内源性PPARγ配体(脂肪酸)从正位囊中推向功能上重要的ω(Ω)-环附近的替代配体结合位点。X射线晶体学,核磁共振光谱,全原子分子动力学模拟,以及与定量生化功能和细胞测定相结合的诱变表明,合成配体和脂肪酸结合可形成与Ω环的“配体连接”并

过氧化物酶体增殖物激活受体γ(PPARγ)的晶体结构揭示了合成和天然/内源配体的重叠结合模式,表明对正位囊的竞争。

在这里,我们显示合成配体与正位囊的结合可以将天然和内源性PPARγ配体(脂肪酸)从正位囊中推向功能上重要的ω(Ω)-环附近的替代配体结合位点。X射线晶体学,核磁共振光谱,全原子分子动力学模拟,以及与定量生化功能和细胞测定相结合的诱变表明,合成配体和脂肪酸结合可形成与Ω环的“配体连接”并协同影响结构和PPARγ的功能。

总之,该研究发现也表明,配体与核受体的结合可能比天然或内源配体与合成配体的经典一对一正交交换更复杂。

原始出处:

Jinsai Shang, Richard Brust, et al., Cooperative cobinding of synthetic and natural ligands to the nuclear receptor PPARγ. eLife. 2018; 7: e43320.

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    2019-03-05 ysjykql
  2. [GetPortalCommentsPageByObjectIdResponse(id=1677273, encodeId=805316e727389, content=<a href='/topic/show?id=6e7462063f0' target=_blank style='color:#2F92EE;'>#核受体#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=73, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=62063, encryptionId=6e7462063f0, topicName=核受体)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=d24727466716, createdName=ysjykql, createdTime=Tue Mar 05 09:38:00 CST 2019, time=2019-03-05, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=2068587, encodeId=e806206858e87, content=<a href='/topic/show?id=59371088215' target=_blank style='color:#2F92EE;'>#Life#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=65, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=10882, encryptionId=59371088215, topicName=Life)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=fc8528, createdName=clmlylxy, createdTime=Fri Mar 15 05:38:00 CST 2019, time=2019-03-15, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1973063, encodeId=05d719e30635b, content=<a href='/topic/show?id=72d566e3a6' target=_blank style='color:#2F92EE;'>#eLife#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=70, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=6673, encryptionId=72d566e3a6, topicName=eLife)], attachment=null, authenticateStatus=null, createdAvatar=http://thirdqq.qlogo.cn/qqapp/1103841572/C2EFD5CFB07FE291138AD4FD0C98E3DE/100, createdBy=e3d52500031, createdName=膀胱癌, createdTime=Fri Jun 21 04:38:00 CST 2019, time=2019-06-21, status=1, ipAttribution=)]
    2019-03-15 clmlylxy
  3. [GetPortalCommentsPageByObjectIdResponse(id=1677273, encodeId=805316e727389, content=<a href='/topic/show?id=6e7462063f0' target=_blank style='color:#2F92EE;'>#核受体#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=73, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=62063, encryptionId=6e7462063f0, topicName=核受体)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=d24727466716, createdName=ysjykql, createdTime=Tue Mar 05 09:38:00 CST 2019, time=2019-03-05, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=2068587, encodeId=e806206858e87, content=<a href='/topic/show?id=59371088215' target=_blank style='color:#2F92EE;'>#Life#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=65, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=10882, encryptionId=59371088215, topicName=Life)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=fc8528, createdName=clmlylxy, createdTime=Fri Mar 15 05:38:00 CST 2019, time=2019-03-15, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1973063, encodeId=05d719e30635b, content=<a href='/topic/show?id=72d566e3a6' target=_blank style='color:#2F92EE;'>#eLife#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=70, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=6673, encryptionId=72d566e3a6, topicName=eLife)], attachment=null, authenticateStatus=null, createdAvatar=http://thirdqq.qlogo.cn/qqapp/1103841572/C2EFD5CFB07FE291138AD4FD0C98E3DE/100, createdBy=e3d52500031, createdName=膀胱癌, createdTime=Fri Jun 21 04:38:00 CST 2019, time=2019-06-21, status=1, ipAttribution=)]
    2019-06-21 膀胱癌
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