VHL, with its widespread expression across tissue types, has become one of the most extensively used E3 ligases in PROTAC development. It has been demonstrated that the composition and length of the linker play a crucial role in influencing the spatial orientation and physicochemical properties of the POI-PROTAC-E3 ternary complex. In this review, the authors focus on providing an overview of the synthesis strategies for the linker component in current VHL PROTAC compositions.
Lenalidomide Used in Cancer Therapies Based on Targeted Protein DegradationPublished on November 10, 2023 Inhibitors/Agonists
Lenalidomide stands as a remarkable example of targeted protein degradation in cancer therapy. This drug, originally developed as an immunomodulatory agent, has garnered significant attention for its ability to harness the cellular machinery for protein degradation, specifically in the context of oncology.
Cholesterol-lowering Star - PCSK9 InhibitorsPublished on November 3, 2023 Inhibitors/Agonists
PCSK9 inhibitors are a class of drugs used to lower LDL cholesterol levels. They work by blocking the PCSK9 enzyme, which normally hinders the liver’s ability to remove LDL cholesterol from the bloodstream. By inhibiting PCSK9, these medications increase the number of LDL receptors on liver cells, allowing for more effective clearance of LDL cholesterol. This class of drugs has shown significant promise in managing high cholesterol levels, particularly in individuals with familial hypercholesterolemia or those with a history of cardiovascular disease.
Advances in Modern ImmunologyPublished on November 3, 2023 Inhibitors/Agonists
In recent decades, concurrent with the evolution of modern immunology, researchers have achieved significant breakthroughs in unraveling the cellular and molecular intricacies of immune regulation across various domains, including infectious diseases, allergic conditions, and neurological disorders. A deeper comprehension of the roles, interplay, and equilibrium among different immune cells and molecules promises to underpin effective scientific foundations and approaches for immune intervention, paving the way for novel treatments in the realm of immune-related illnesses.
Is Obesity a Disease? —Latest Results for RemaglutidePublished on October 27, 2023 Inhibitors/Agonists
Heart disease is the leading cause of death worldwide, and obesity is considered one of its major risk factors. The relationship between obesity and heart health is complex, and there is ongoing debate over whether obesity is a disease or simply a health condition. As a result, there is growing interest in developing drugs that aid weight loss and improve cardiovascular health. Recently, a study found that semaglutide, known as the “miracle drug for weight loss,” not only helps reduce weight, but also reduces the risk of major cardiovascular complications. This raises hope for potential cardiovascular benefits of other weight-loss drugs.
Modulating Treg Homeostasis - Improving Cancer ImmunotherapyPublished on October 26, 2023 Cancer
Immunosuppressive regulatory T cells (Tregs) are the main mechanism of tumor immune evasion. Targeting Tregs, especially in the tumor microenvironment (TME), could improve cancer immunotherapy. Research in recent years has revealed the heterogeneity and plasticity of Tregs within tumors, further deepening the complexity of the role of Tregs in tumor immunity and immune response therapy. The phenotypic and functional diversity of Tregs within tumors can influence their response to therapy and may provide new targets for modulating specific Treg subsets
AI for Natural Product Drug DiscoveryPublished on October 20, 2023 Inhibitors/Agonists
A Review about EquolPublished on October 20, 2023 Inhibitors/Agonists
Equol, derived from daidzein in soy-based foods, is a focus of intense research due to its potential health benefits. Its unique interaction with estrogen receptors is valuable for hormone-related conditions like breast and prostate cancers. Produced in the gut by specific bacteria, equol’s synthesis varies individually, prompting personalized nutrition studies. Notably, it lowers LDL cholesterol, aids postmenopausal bone health, and exhibits neuroprotective antioxidant properties. Ongoing research explores its use in tailored functional foods and pharmaceuticals, promising individualized solutions for diverse health needs.
The Efficacy and Safety of Immune Checkpoint Inhibitors in Treating MelanomaPublished on October 12, 2023 Inhibitors/Agonists
This comprehensive review explores the impact of Immune Checkpoint Inhibitors (ICIs) on advanced melanoma treatment. ICIs enhance T-cell activity against cancer cells by blocking immune checkpoints, leading to enduring immune responses. The study reveals substantial improvements in progression-free and overall survival rates, particularly with combination therapies. However, ICI treatment may trigger chronic immune-related adverse events, emphasizing the need for vigilant, long-term monitoring.
New Opportunities for PROTACPublished on October 12, 2023 Inhibitors/Agonists
PROTAC is a bifunctional molecule. In recent years, PROTAC technology has developed rapidly, opening up new paths for research, development, and experimentation. Then, a brief introduction to the related PROTAC knowledge is made today
Opportunities and Challenges for DeuterationPublished on September 27, 2023 Inhibitors/Agonists
In the process of drug development, academic employ various methods to enhance the activity and safety of small-molecule compounds, aiming to improve the compound’s other characteristics while maintaining its original activity. Deuterium modification refers to the strategy of replacing specific hydrogen atoms with deuterium atoms within a molecule.