PROTAC
From Proteopedia
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A Proteolysis-Targeting Chimera (PROTAC) is a small protein with two active domains joined by a linker. PROTACs represent an alternative to conventional enzyme inhibitors, by enabling [[Proteasome|proteasome]] induced degradation of the target protein <ref>pmid 28288108</ref>. | A Proteolysis-Targeting Chimera (PROTAC) is a small protein with two active domains joined by a linker. PROTACs represent an alternative to conventional enzyme inhibitors, by enabling [[Proteasome|proteasome]] induced degradation of the target protein <ref>pmid 28288108</ref>. | ||
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[[Image:PROTAC_70.png|thumb|right|300px|Representative PROTAC from [https://protacpedia.weizmann.ac.il/ptcb/detp?i=70 PROTACpedia] targeting EGFR Epidermal growth factor receptor P00533. <span class="bg-lightblue"><b>target binding ligand</b></span><span class="bg-lightmagenta"><b>linker</b></span><span class="bg-lightgreen"><b>E3 binder</b></span>]] | [[Image:PROTAC_70.png|thumb|right|300px|Representative PROTAC from [https://protacpedia.weizmann.ac.il/ptcb/detp?i=70 PROTACpedia] targeting EGFR Epidermal growth factor receptor P00533. <span class="bg-lightblue"><b>target binding ligand</b></span><span class="bg-lightmagenta"><b>linker</b></span><span class="bg-lightgreen"><b>E3 binder</b></span>]] | ||
Revision as of 10:48, 28 February 2021
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References
- ↑ Gadd MS, Testa A, Lucas X, Chan KH, Chen W, Lamont DJ, Zengerle M, Ciulli A. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 Mar 13. doi: 10.1038/nchembio.2329. PMID:28288108 doi:http://dx.doi.org/10.1038/nchembio.2329
- ↑ PRosettaC https://prosettac.weizmann.ac.il, a computational resource for the prediction of PROTAC-induced ternary complexes.
- ↑ Zaidman D, Prilusky J, London N. PRosettaC: Rosetta based modeling of PROTAC mediated ternary complexes. J Chem Inf Model. 2020 Sep 25. doi: 10.1021/acs.jcim.0c00589. PMID:32976709 doi:http://dx.doi.org/10.1021/acs.jcim.0c00589
- ↑ PROTACpedia https://protacpedia.weizmann.ac.il/, a resource of manually curated data on Proteolysis Targeting Chimeras (PROTACs).