Phosphoramidon inhibits the integral membrane protein zinc metalloprotease ZMPSTE24

Goblirsch Brandon R.; Arachea Buenafe T.; Councell Daniel J.Wiener Michael C.

首页> 外文期刊>Acta crystallographica. Section D, Structural biology. >Phosphoramidon inhibits the integral membrane protein zinc metalloprotease ZMPSTE24

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Phosphoramidon inhibits the integral membrane protein zinc metalloprotease ZMPSTE24

机译：Phosphoramidon抑制膜的积分蛋白锌metalloprotease ZMPSTE24

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The integral membrane protein zinc metalloprotease ZMPSTE24 possesses a completely novel structure, comprising seven long kinked transmembrane helices that encircle a voluminous 14?000?? 3 cavity within the membrane. Functionally conserved soluble zinc metalloprotease residues are contained within this cavity. As part of an effort to understand the structural and functional relationships between ZMPSTE24 and soluble zinc metalloproteases, the inhibition of ZMPSTE24 by phosphoramidon [ N ‐(α‐rhamnopyranosyl‐oxyhydroxyphosphinyl)‐Leu‐Trp], a transition‐state analog and competitive inhibitor of multiple soluble zinc metalloproteases, especially gluzincins, has been characterized functionally and structurally. The functional results, the determination of preliminary IC 50 values by the use of an intramolecular quenched‐fluorescence fluorogenic peptide assay, indicate that phosphoramidon inhibits ZMPSTE24 in a manner consistent with competitive inhibition. The structural results, a 3.85?? resolution X‐ray crystal structure of a ZMPSTE24–phosphoramidon complex, indicate that the overall binding mode observed between phosphoramidon and soluble gluzincins is conserved. Based on the structural data, a significantly lower potency than that observed for soluble gluzincins such as thermolysin and neprilysin is predicted. These results strongly suggest a close relationship between soluble gluzincins and the integral membrane protein zinc metalloprotease ZMPSTE24.

机译：膜蛋白锌metalloprotease积分ZMPSTE24拥有一个全新的结构,由七个长弯折的跨膜螺旋线,包围的14 000 ? ?腔内的膜。守恒的可溶性锌metalloprotease残留都包含在这个空腔。努力理解结构和功能性ZMPSTE24和之间的关系可溶性锌metalloproteases,抑制由phosphoramidon ZMPSTE24 [N

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来源
《Acta crystallographica. Section D, Structural biology.》 |2018年第8期|739-747|共8页
作者
Goblirsch Brandon R.; Arachea Buenafe T.; Councell Daniel J.Wiener Michael C.;
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Department of Molecular Physiology and Biological Physics, University of Virginia, Charlottesville;

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正文语种英语
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Integral Membrane Proteins; phosphoramidon; MetalloproteasesZMPSTE24 gene;

机译：积分膜蛋白质;phosphoramidon MetalloproteasesZMPSTE24基因;

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Phosphoramidon inhibits the integral membrane protein zinc metalloprotease ZMPSTE24

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