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ProteomicsBruton’s Tyrosine Kinase Degradation as a Therapeutic Strategy for Cancer
The covalent Bruton’s Tyrosine Kinase (BTK) inhibitor ibrutinib is highly efficacious against multiple B-cell malignancies. However, it also has off-target effects and multiple mechanisms of resistance, including the C481S mutation. We hypothesized that small molecule-induced BTK degradation might ...
ORGANISM(S): Homo sapiens (Human) 
2019-01-25 | PXD010568 | Pride
Imids Protac Crl4 Btk Ubiquitin Cullin 
ProteomicsDevelopment and Characterization of a Wee1 Kinase Degrader
The G1/S cell-cycle checkpoint is frequently dysregulated in cancer, leaving cancer cells particularly reliant on a functional G2/M checkpoint to prevent excessive DNA damage. Inhibiting regulators of the G2/M checkpoint can therefore drive cancer cells into premature mitosis, ultimately causing cel...
ORGANISM(S): Homo sapiens (Human) 
2019-11-18 | PXD015513 | Pride
Cancer Wee1 Crl4 Crbn Protac Ubiquitin 
ProteomicsDegraders of the dengue virus capsid protein exhibit differentiated pharmacology relative to capsid inhibitors
Due to the limited size of viral genomes, most viral proteins are multifunctional; yet most direct-acting antivirals are designed as single-function inhibitors. The dengue virus (DENV) capsid protein serves as a building block for new virions while also interacting with multiple host factors to remo...
ORGANISM(S): Homo sapiens (Human) 
2026-03-30 | PXD063557 | Pride
Degrader Dengue Capsin Virus Crbn Chemical biology Protac Ubiquitin 
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 
ProteomicsThalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome, part 2
Frequently used to treat morning sickness, the drug thalidomide led to the birth of thousands of children with severe birth defects. Despite their teratogenicity, thalidomide and related IMiD drugs are now a mainstay of cancer treatment, however, the molecular basis underlying the pleiotropic biolog...
ORGANISM(S): Homo sapiens (Human) 
2018-08-09 | PXD010417 | Pride
Crl4 Thalidomide Ubiquitin Imids Cullin 
ProteomicsThalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome, part 3
Frequently used to treat morning sickness, the drug thalidomide led to the birth of thousands of children with severe birth defects. Despite their teratogenicity, thalidomide and related IMiD drugs are now a mainstay of cancer treatment, however, the molecular basis underlying the pleiotropic biolog...
ORGANISM(S): Homo sapiens (Human) 
2018-08-09 | PXD010418 | Pride
Crl4 Thalidomide Ubiquitin Imids Cullin 
ProteomicsThalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome, part 1
Frequently used to treat morning sickness, the drug thalidomide led to the birth of thousands of children with severe birth defects. Despite their teratogenicity, thalidomide and related IMiD drugs are now a mainstay of cancer treatment, however, the molecular basis underlying the pleiotropic biolog...
ORGANISM(S): Homo sapiens (Human) 
2018-08-09 | PXD010416 | Pride
Crl4 Thalidomide Ubiquitin Imids Cullin 
ProteomicsThalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome, part 6
Frequently used to treat morning sickness, the drug thalidomide led to the birth of thousands of children with severe birth defects. Despite their teratogenicity, thalidomide and related IMiD drugs are now a mainstay of cancer treatment, however, the molecular basis underlying the pleiotropic biolog...
ORGANISM(S): Homo sapiens (Human) 
2018-08-10 | PXD010428 | Pride
Crl4 Thalidomide Ubiquitin Imids Cullin 
ProteomicsThalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome, part 5
Frequently used to treat morning sickness, the drug thalidomide led to the birth of thousands of children with severe birth defects. Despite their teratogenicity, thalidomide and related IMiD drugs are now a mainstay of cancer treatment, however, the molecular basis underlying the pleiotropic biolog...
ORGANISM(S): Homo sapiens (Human) 
2018-08-09 | PXD010420 | Pride
Crl4 Thalidomide Ubiquitin Imids Cullin 
ProteomicsAcute pharmacological degradation of ERK5 does not inhibit cellular immune response or proliferation
Over the past few decades, interest in the role that extracellular signal-regulated kinase 5 (ERK5) plays in various diseases, particularly cancer and inflammation, has grown. Phenotypes observed from genetic knockdown or deletion of ERK5 suggested that targeting ERK5 could have therapeutic potentia...
ORGANISM(S): Homo sapiens (Human) 
2022-10-13 | PXD036104 | Pride
Targeted protein degradation Erk5 Degrader 
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