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PROTACs, molecular glues and other degraders

Overview

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PROTACs (proteolysis targeting chimeras) are hybrid molecules that promote co-localisation of a target protein and cereblon (CRBN) to promote E3 ligase CRL4CRBN-mediated ubiquitination and proteasomal degradation of the chosen target protein [1]. PROTACs effectively remove specific proteins from within cells, and offer therapeutic potential beyond traditional small molecule inhibitors. Molecular 'glues' use a different mechanism. They employ a single interaction with cereblon [2], and via this interaction they alter the substrate specificity of the E3 ligase, so that neo-substrates are targeted for proteasomal degradation. The immunomodulatory imide drug (iMiD) thalidomide and its analogues are the archetypal 'glues'.

Ligands

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Ligands of relevance to immunopharmacology are highlighted in blue

JH-XI-10-02 Show summary » More detailed page

TL13-112 Show summary » More detailed page

BSJ-03-204 Show summary » More detailed page

BSJ-04-132 Show summary » More detailed page

BSJ-03-123 Show summary » More detailed page

dTAG-13 Show summary » More detailed page

dBET6 Show summary » More detailed page

DD-03-171 Show summary » More detailed page

dTRIM24 Show summary » More detailed page

QC-01-175 Show summary » More detailed page

dBRD9 Show summary » More detailed page

dBRD9-A Show summary » More detailed page

THAL-SNS-032 Show summary » More detailed page

avadomide Show summary » More detailed page

ARD-69 Show summary » More detailed page

thalidomide Show summary » More detailed page

pomalidomide Show summary » More detailed page

lenalidomide Show summary » More detailed page

iberdomide Show summary » More detailed page

MS432 Show summary » More detailed page

ARV-771 Show summary » More detailed page

SIAIS178 Show summary » More detailed page

compound 7f [PMID: 31251063] Show summary » More detailed page

ARD-266 Show summary » More detailed page

ERD-308 Show summary » More detailed page

compound 3 [PMID: 31804822] Show summary » More detailed page

MS39 Show summary » More detailed page

MS154 Show summary » More detailed page

PROTAC 3 Show summary » More detailed page

compound 16 [PMID: 31653597] Show summary » More detailed page

(R)-CR8 Show summary » More detailed page

BI-3802 Show summary » More detailed page

CC-90009 Show summary » More detailed page

ARV471 Show summary » More detailed page

ARV110 Show summary » More detailed page

SR-1114 Show summary » More detailed page

compound 17 [PMID: 34176264] Show summary » More detailed page

SD-91 Show summary » More detailed page

TBK1 PROTAC 3i Show summary » More detailed page

References

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How to cite this family page

Database page citation:

PROTACs, molecular glues and other degraders. Accessed on 26/10/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=1030.