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ProteomicsRedirecting the neo-substrate specificity of Cereblon-targeting PROTACs to Helios
Immunomodulatory imide drugs (IMiDs), such as thalidomide and its analogues, are some of the most commonly utilized E3 ligase ligands for the development of proteolysis targeting chimeras (PROTACs). While the canonical neo-substrates of IMiDs (i.e., Ikaros and Aiolos) are often considered to be unwa...
ORGANISM(S): Homo sapiens (Human) 
2022-09-07 | PXD036170 | Pride
Targeted protein degradation Degrader Helios Cdk4 Protac Cdk6 
UnknownThalidomide and its metabolite 5-hydroxythalidomide induce teratogenicity via the cereblon neo-substrate PLZF
Not available
S-SCDT-EMBOJ-2020-105375 | biostudies-other
ProteomicsNeo-substrate selectivity of IMiDs on biotinylation by AirID-CRBN
MM1.S cells stably expressing AGIA-AirID-CRBN-WT were treated with DMSO, 20 µM thalidomide, 10 µM lenalidomide, 10 µM pomalidomide or 20 µM 5-hydroxythalidomide (5HT) in the presence of 10 µM biotin and 5 µM MG132 for 8 h in three biological replicates. After tryptic digestion, biotinylated peptides...
ORGANISM(S): Homo Sapiens (human) 
2021-11-06 | PXD028755 | JPOST Repository
TranscriptomicsDisease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradation
E3 ubiquitin ligases of the Cullin RING Ligase (CRL) family assemble into multiprotein complexes to diversify substrate adaptors and ensure selectivity in substrate engagement for degradation. Here we show a novel mechanism whereby mutations in substrate adaptors can drive neo-substrate degradation ...
ORGANISM(S): Homo sapiens 
2022-03-30 | GSE197240 | GEO
ProteomicsA degron blocking strategy towards improved CRBN recruiting PROTAC selectivity
The different layers of complexity in PROTAC design have slowed the broad implementation of this novel pharmacological approach. Given the challenges and opportunities of CRL4CRBN hijacking PROTACs we set out to identify and develop broadly implementable strategies to generate PROTACs with improved ...
ORGANISM(S): Homo sapiens (Human) 
2023-07-10 | PXD038298 | Pride
Lc-msms Human Protacs 
ProteomicsA degron blocking strategy towards improved CRBN recruiting PROTAC selectivity
The different layers of complexity in PROTAC design have slowed the broad implementation of this novel pharmacological approach. Given the challenges and opportunities of CRL4CRBN hijacking PROTACs we set out to identify and develop broadly implementable strategies to generate PROTACs with improved ...
ORGANISM(S): Homo sapiens (Human) 
2023-07-10 | PXD038503 | Pride
Cereblon Protacs 
ProteomicsThe Identification of Proteolytic Substrates of Calpain-5 with N-terminomics
Calpain-5/CAPN5 is a calcium-activated, non-lysosomal cysteine (thiol) protease. The substrate spectrum repertoire of CAPN5 is not known. Calpains catalyze limited proteolysis of their substrates, generating novel neo protein N-termini that correspond to internal residues of their nascent substrate ...
ORGANISM(S): Homo sapiens (Human) 
2025-07-21 | PXD064313 | Pride
Capn5 Protease Disease Tails N-terminomics Calpain-5 
ProteomicsTAILS identifies candidate substrates and biomarkers of ADAMTS7, a therapeutic protease target in coronary artery disease
MacDonald BT, Keshishian H, Mundorff CC, Arduini A, Lai D, Bendinelli K, Popp NR, Bhandary B, Clauser KR, Specht H, Elowe NH, Laprise D, Xing Y, Kaushik VK, Carr SA, Ellinor PT. Loss-of-function mutations in the secreted enzyme ADAMTS7 (a disintegrin and metalloproteinase with thrombospondin motifs ...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2021-12-03 | MSV000088508 | MassIVE
ProteomicsDisease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradationDisease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradation
E3 ubiquitin ligases of the Cullin RING Ligase (CRL) family assemble into multiprotein complexes to diversify substrate adaptors and ensure selectivity in substrate engagement for degradation. Here we show a novel mechanism whereby mutations in substrate adaptors can drive neo-substrate degradation ...
ORGANISM(S): Homo sapiens (Human) 
2022-10-14 | PXD031683 | Pride
Medulloblastoma Kbtbd4 Ubiquitin Corest Epigenetic remodelling 
ProteomicsSystematic characterization of cancer-associated SPOP mutants reveals novel and reprogrammable degradative activities
Speckle-type POZ protein (SPOP) functions as the substrate adaptor of the Cullin3-RING ligase (CRL3) complex and is recurrently mutated in multiple cancer types. Among these, F102C and F133L are frequent prostate cancer mutations within the substrate-binding domain, yet their biochemical consequence...
ORGANISM(S): Homo sapiens (Human) 
2025-12-17 | PXD071054 | Pride
E3 ligase Targeted protein degradation Proteomics 
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