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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 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 
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 
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