PROTAC

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

54 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]

Cyclin-dependent kinase 6 (CDK6) as a potent regulator of the ovarian primordial-to-primary follicle transition

26 views | Dec 11 2023

The study reveals that CDK6 inhibition using BSJ disrupts the primordial-to-primary follicle transition, emphasizing the crucial role of precise cell cycle regulation in ovarian follicle development and suggesting potential implications for fertility-related interventions. [Read the Full Post]

Targeting SWI/SNF ATPases in H3.3K27M diffuse intrinsic pontine gliomas

17 views | Dec 02 2023

H3K27M mutations in diffuse midline gliomas reprogram the SWI/SNF complex, leading to upregulated SMARCA4 levels, and therapeutic targeting of SMARCA4, SMARCA2, and PBRM1 using AU-15330 selectively induces cytotoxicity in H3.3K27M-mutant cells, suggesting a potent and specific therapeutic strategy for these deadly childhood brain tumors. [Read the Full Post]

The therapeutic effect of the BRD4-degrading PROTAC A1874 in human colon cancer cells

0 views | Nov 10 2023

A1874, a novel BRD4-degrading PROTAC, demonstrates potent anti-colon cancer activity through both BRD4-dependent and -independent mechanisms, inhibiting cell growth, inducing apoptosis, and showing efficacy in in vivo models. [Read the Full Post]

Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target

82 views | Oct 15 2023

This study identified novel epigenetic regulators of the tfpia gene and demonstrated the potential of UNC6852 as an antithrombotic drug by enhancing tfpia mRNA levels and prolonging the time to occlude the caudal vessel after laser injury in zebrafish larvae and adults. [Read the Full Post]

Modeling the Effect of Cooperativity in Ternary Complex Formation and Targeted Protein Degradation Mediated by Heterobifunctional Degraders

60 views | Sep 16 2023

This study develops a pharmacodynamic model and statistical inference model to investigate the role of cooperativity in ternary complex formation and degradation efficiency, providing insights for the rational design of effective HBF degraders in targeted protein degradation. [Read the Full Post]

Effects of the inclusion of coffee pulp silage in the diet on the performance and profitability of crossbred milk cows in the middle tropics

45 views | Sep 06 2023

The inclusion of coffee pulp silage in the diet of crossbred dairy cows in the middle tropics improved their productive efficiency and nutritional characteristics without affecting milk production. [Read the Full Post]

Glutathione-Scavenging Nanoparticle-Mediated PROTACs Delivery for Targeted Protein Degradation and Amplified Antitumor Effects

34 views | Aug 09 2023

The development of Nano-PROTACs, which involve encapsulating PROTACs in GSH-responsive polymeric nanoparticles, demonstrates improved bioavailability, enhanced protein degradation, and superior anti-tumor efficacy, showing promise for the targeted treatment of diseases. [Read the Full Post]

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

62 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]

BRD4: New hope in the battle against glioblastoma

17 views | Jul 28 2023

This review provides a comprehensive overview of the roles and mechanisms of BRD4 in glioblastoma pathogenesis, as well as evaluates the potential of BRD4 inhibitors and degraders as novel treatment strategies against GBM. [Read the Full Post]