PROTAC: Difference between revisions
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[[Image:PROTAC_70.png|thumb|right|200px|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>]] | |||
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>. | ||
==PROTACpedia== | ==PROTACpedia== | ||
[https://protacpedia.weizmann.ac.il/ PROTACpedia] <ref>PROTACpedia https://protacpedia.weizmann.ac.il/, a resource of manually curated data on Proteolysis Targeting Chimeras (PROTACs).</ref> is a collaborative and comprehensive, high-quality and freely accessible resource of manually curated data on Proteolysis Targeting Chimeras (PROTACs). | [https://protacpedia.weizmann.ac.il/ PROTACpedia] <ref>PROTACpedia https://protacpedia.weizmann.ac.il/, a resource of manually curated data on Proteolysis Targeting Chimeras (PROTACs).</ref> is a collaborative and comprehensive, high-quality and freely accessible resource of manually curated data on Proteolysis Targeting Chimeras (PROTACs). Users can search PROTACpedia by various parameters such as Target name, UniProt ID, SMILES substructure or by details regarding a publication or patent. | ||
The [https://protacpedia.weizmann.ac.il/ptcb/stats statistics] page of PROTACpedia allows to overview current distribution on PROTACs of IC<sub>50</sub>, DC<sub>50</sub>, linker, etc. | The [https://protacpedia.weizmann.ac.il/ptcb/stats statistics] page of PROTACpedia allows to overview current distribution on PROTACs of IC<sub>50</sub>, DC<sub>50</sub>, linker, etc. | ||
{| class="wikitable" | {| class="wikitable" | ||
|+PROTACs on PDB | |||
|- | |||
|- valign="top" | |- valign="top" | ||
! PROTAC Target | ! PROTAC Target | ||
! Structure | ! 3D Structure | ||
|- valign="top" | |- valign="top" | ||
| Bcl-Xl | | Bcl-Xl | ||