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ProteomicsMechanism of degrader-targeted protein ubiquitinability
Small molecule degraders of disease-driving proteins offer a clinically proven modality with enhanced therapeutic efficacy and the potential to tackle previously undrugged targets. Thermodynamically stable and kinetically long-lived degrader-mediated ternary complexes can drive faster, more profound...
ORGANISM(S): Homo sapiens (Human) 
2024-11-08 | PXD053502 | Pride
Mz1 Vhl Ubiquitination 
ProteomicsVHL inhibitor binding increases intracellular level of VHL
The von–Hippel Lindau (VHL) protein is a tumour suppressor protein frequently mutated in the VHL disease, which functions as substrate recognition subunit of a Cul2 E3 ubiquitin ligase (CRL2VHL). CRL2VHL plays an important role in oxygen sensing, by binding and targeting Hypoxia Inducible Factor-alp...
ORGANISM(S): Homo sapiens (Human) 
2022-02-17 | PXD025743 | Pride
Tmt-labelling Hela Human cells 
ProteomicsSMARCA2/4 degradation tails mediate recruitment of two different E3 ligases 
In this work, we characterise novel SMARCA2/4 degraders using a robust cell biology and structural workflow and reveal for the first time, the recruitment of two E3 ligase substrate receptors: FBXO22 and DCAF16 by the same degradation tail. Furthermore, we were able to chemically fine-tune this dual...
ORGANISM(S): Homo sapiens (Human) 
2026-05-16 | PXD065523 | Pride
E3 ligases  Smarca2/4 Protein degrader 
ProteomicsSMARCA2/4 degradation tails mediate recruitment of two different E3 ligases 
In this work, we characterise novel SMARCA2/4 degraders using a robust cell biology and structural workflow and reveal for the first time, the recruitment of two E3 ligase substrate receptors: FBXO22 and DCAF16 by the same degradation tail. Furthermore, we were able to chemically fine-tune this dual...
ORGANISM(S): Homo sapiens (Human) 
2026-05-16 | PXD065445 | Pride
Smarca2/4 E3 ligases  Protein degrader 
ProteomicsBromoCatch: a self-labelling tag platform for protein analysis and live cell imaging
Visualizing and manipulating proteins in live cells is crucial for studying complex biological processes. Self-labelling protein (SLP) tags such as HaloTag and SNAP-tag can be fused to genes of interest to allow protein labelling in cells. New tools to enable rapid, specific and stable protein label...
ORGANISM(S): Homo sapiens (Human) 
2026-05-04 | PXD074567 | Pride
Bromocatch Cell imaging 
ProteomicsA selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
Targeted protein degradation offers an alternative modality to classical inhibition and holds the promise of addressing previously undruggable targets to provide novel therapeutic options for patients. Heterobifunctional molecules co-recruit the target and an E3 ligase, resulting in ubiquitylation ...
ORGANISM(S): Homo sapiens (Human) 
2022-06-20 | PXD032239 | Pride
Protac Tpd Smarca Oral bioavailability 
ProteomicsTargeting cancer with small molecule panKRAS degraders
Despite the high prevalence of cancers driven by KRAS mutations, to date only the G12C mutation has been clinically proven to be druggable via covalent targeting of the mutated cysteine amino acid residue. However, in many cancer indications other KRAS mutations, such as G12D and -V, are far more pr...
ORGANISM(S): Homo sapiens (Human) 
2024-10-01 | PXD045460 | Pride
Cancer Protac Degradation Kras 
ProteomicsTargeting cancer with small molecule pan-KRAS degraders
Despite the high prevalence of cancers driven by KRAS mutations, to date only the G12C mutation has been clinically proven to be druggable via covalent targeting of the mutated cysteine amino acid residue1. However, in many cancer indications other KRAS mutations, such as G12D and -V, are far more p...
ORGANISM(S): Homo sapiens (Human) 
2024-10-01 | PXD050650 | Pride
Cancer Kras Protac 
ProteomicsConfounding factors in targeted degradation of short-lived proteins
Targeted proTargeted protein degradation has recently emerged as a novel option in drug discovery. Natural protein half-life is expected to affect the efficacy of degrading agents, but it has not been systematically explored to what extent it influences target protein degradation. Using mathematical...
ORGANISM(S): Homo sapiens (Human) 
2024-10-01 | PXD047934 | Pride
Protac. short-lived proteins Cancer Craf 
ProteomicsTargeting cancer with small molecule panKRAS degraders
Despite the high prevalence of cancers driven by KRAS mutations, to date only the G12C mutation has been clinically proven to be druggable via covalent targeting of the mutated cysteine amino acid residue. However, in many cancer indications other KRAS mutations, such as G12D and -V, are far more pr...
ORGANISM(S): Homo sapiens (Human) 
2024-10-02 | PXD045416 | Pride
Degraders Cancer Protac Kras 
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