进展

订阅

MedSci主页 / 所有栏目 / 进展

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

关注

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.

版权声明：
本网站所有内容来源注明为“梅斯医学”或“MedSci原创”的文字、图片和音视频资料，版权均属于梅斯医学所有。非经授权，任何媒体、网站或个人不得转载，授权转载时须注明来源为“梅斯医学”。其它来源的文章系转载文章，或“梅斯号”自媒体发布的文章，仅系出于传递更多信息之目的，本站仅负责审核内容合规，其内容不代表本站立场，本站不负责内容的准确性和版权。如果存在侵权、或不希望被转载的媒体或个人可与我们联系，我们将立即进行删除处理。
在此留言
评论区 (3)
#插入话题
  1. [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=29, 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=24, 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=17, 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=)]
    2019-03-05 ysjykql

    #核受体#

    0

  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=29, 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=24, 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=17, 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

    #Life#

    0

  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=29, 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=24, 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=17, 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

    #eLife#

    0