E3 Ligase

Gastrodin overcomes chemoresistance via inhibiting Skp2-mediated glycolysis

42 views | Jan 18 2024

The study highlights the potential of targeting the Skp2-Akt axis and utilizing gastrodin, inhibiting HK2-mediated glucose metabolism and promoting apoptosis, as a promising combined therapeutic approach for overcoming cisplatin resistance in oral squamous cell carcinoma (OSCC). [Read the Full Post]

A Degron Blocking Strategy Towards Improved CRL4CRBN Recruiting PROTAC Selectivity

30 views | Dec 28 2023

Your work addressing selectivity challenges in PROTAC design by leveraging structural insights and computational modeling offers valuable principles and tools crucial for advancing targeted protein degradation strategies. [Read the Full Post]

Degradation of Cyclin-Dependent Kinase 9/Cyclin T1 by Optimized Microtubule-Associated Protein 1 Light Chain 3 Beta-Recruiting Coumarin Analogs

53 views | Dec 24 2023

Researchers systematically optimized coumarin analogs linked with the CDK9 inhibitor SNS-032, potentially enabling simultaneous binding to CDK9 and LC3B, initiating selective autophagic degradation and demonstrating potential for treating diseases associated with intracellular pathogenic proteins. [Read the Full Post]

Therapeutical interference with the epigenetic landscape of germ cell tumors: a comparative drug study and new mechanistical insights

42 views | Dec 15 2023

The study identified seven epigenetic inhibitors that efficiently decreased cell viability in cisplatin-resistant Type II germ cell tumors, highlighting their potential as alternative therapeutic options, and provided comprehensive insights into their off-target effects and modes of action. [Read the Full Post]

Inhibition of CDC20 potentiates anti-tumor immunity through facilitating GSDME-mediated pyroptosis in prostate cancer

41 views | Nov 10 2023

The study reveals that CDC20 negatively regulates pyroptosis by targeting GSDME for ubiquitin-mediated proteolysis in prostate cancer, and its inhibition enhances anti-tumor immunity and synergizes with anti-PD1-based immunotherapy, offering novel therapeutic avenues for this cancer type. [Read the Full Post]

The role of E3 ubiquitin ligase in multiple myeloma: potential for cereblon E3 ligase modulators in the treatment of relapsed/refractory disease

40 views | Sep 13 2023

The emerging field of targeted protein degradation, particularly through the redirection of the ubiquitin-proteasome system, offers promising prospects for novel therapeutic approaches in multiple myeloma and other diseases. [Read the Full Post]

A Phase 1, Multicenter, Open-Label Study to Evaluate the Pharmacokinetics of Iberdomide in Subjects with Mild, Moderate, or Severe Hepatic Impairment Compared with Healthy Subjects

33 views | Aug 24 2023

The phase 1 study demonstrated that hepatic impairment had no clinically significant impact on the pharmacokinetics of iberdomide, supporting the conclusion that no dose adjustment is necessary for patients with hepatic impairment. [Read the Full Post]

Exposure-Response Analysis to Assess the Concentration-QTc Relationship of Iberdomide

54 views | Aug 24 2023

The study suggests that iberdomide, at its maximum plasma concentration, does not have a clinically relevant effect on QT interval prolongation. [Read the Full Post]

VH298-loaded extracellular vesicles released from gelatin methacryloyl hydrogel facilitate diabetic wound healing by HIF-1α-mediated enhancement of angiogenesis

61 views | Aug 03 2023

This study demonstrates the potential of VH298-loaded extracellular vesicles (EVs) and GelMA hydrogel as a promising therapeutic strategy for diabetic wound treatment, promoting angiogenesis and enhancing wound healing. [Read the Full Post]

Lipopolysaccharide sensitizes the therapeutic response of breast cancer to IAP antagonist

37 views | Apr 03 2023

The study shows that LPS enhances the therapeutic response of IAP antagonists in treating triple-negative and ER+ breast cancer by inducing rapid apoptosis of cancer cells through TLR4- and MyD88-mediated production of TNFα, and suggests that antibiotics that can reduce microbiota-derived LPS should not be used together with an IAP antagonist for cancer therapy. [Read the Full Post]