PROTAC: Difference between revisions

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~~PROTAC (PROteolysis TArgeting Chimera) is a small protein with two active domains joined by a linker.~~

[[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. target binding ligandlinkerE3 binder]]

[[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. target binding ligandlinkerE3 binder]]

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==

[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 IC50, DC50, linker, etc.

{| class="wikitable"

|+PROTACs on PDB

|-

|- valign="top"

! PROTAC Target

! 3D Structure

|- valign="top"

| Bcl-Xl

| [[6zhc]]

|- valign="top"

| BRD4

| [[5t35]] [[6bn7]] [[6bn8]] [[6bn9]] [[6bnb]] [[6boy]] [[6sis]] [[7khh]]

|- valign="top"

| BTK

| [[6w7o]] [[6w8i]]

|- valign="top"

| SMARCA2

| [[6hax]] [[6hay]] [[6hr2]]

|}

==Predicting PROTAC-induced ternary complexes==

PRosettaC <ref>PRosettaC https://prosettac.weizmann.ac.il, a computational resource for the prediction of PROTAC-induced ternary complexes.</ref> is a computational resource for the prediction of PROTAC-induced ternary complexes <ref>pmid 32976709</ref>. PRosettaC receives as input, two protein structures (protein target and E3 ligase), including their appropriate ligands (binders), as well as the PROTAC chemical structure in a SMILES representation, and outputs predicted models for the ternary complex. Other methods become available <ref>pmid 32969649</ref><ref>pmid 33625214</ref>.

== References ==

[[Category:Protac]]

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@@ Line 1: / Line 1: @@
-PROTAC (PROteolysis TArgeting Chimera) is a small protein with two active domains joined by a linker.
+[[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>]]
-[[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>]]
+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==
+[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.
+{| class="wikitable"
+|+PROTACs on PDB
+|-
+|- valign="top"
+! PROTAC Target
+! 3D Structure
+|- valign="top"
+| Bcl-Xl
+| [[6zhc]]
+|- valign="top"
+| BRD4
+| [[5t35]] [[6bn7]] [[6bn8]] [[6bn9]] [[6bnb]] [[6boy]] [[6sis]] [[7khh]]
+|- valign="top"
+| BTK
+| [[6w7o]] [[6w8i]]
+|- valign="top"
+| SMARCA2
+| [[6hax]] [[6hay]] [[6hr2]]
+|}
+==Predicting PROTAC-induced ternary complexes==
+PRosettaC <ref>PRosettaC https://prosettac.weizmann.ac.il, a computational resource for the prediction of PROTAC-induced ternary complexes.</ref> is a computational resource for the prediction of PROTAC-induced ternary complexes <ref>pmid 32976709</ref>. PRosettaC receives as input, two protein structures (protein target and E3 ligase), including their appropriate ligands (binders), as well as the PROTAC chemical structure in a SMILES representation, and outputs predicted models for the ternary complex. Other methods become available <ref>pmid  32969649</ref><ref>pmid  33625214</ref>.
 == References ==
 <references/>
+[[Category:Protac]]