A5063847298- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Monoclonal and Polyclonal Antibodies Research
- Cytokine Signaling Pathways and Interactions
- Asthma and respiratory diseases
- T-cell and B-cell Immunology
- Bioactive Compounds and Antitumor Agents
- HER2/EGFR in Cancer Research
- Immune Response and Inflammation
- Pain Mechanisms and Treatments
- Ion Channels and Receptors
- Immunotherapy and Immune Responses
- Biotechnology and Related Fields
AbbVie (United States)
2016-2024
Glucocorticoids (GCs) are efficacious drugs used for treating many inflammatory diseases, but the dose and duration of administration limited because severe side effects. We therefore sought to identify an approach selectively target GCs inflamed tissue. Previous work identified that anti–tumor necrosis factor (TNF) antibodies bind transmembrane TNF undergo internalization; therefore, anti-TNF antibody-drug conjugate (ADC) would be mechanistically similar, where lysosomal catabolism could...
Using a convergent synthetic route to enable multiple points of diversity, series glucocorticoid receptor modulators (GRM) were profiled for potency, selectivity, and drug-like properties in vitro. Despite covering large range profiling the nonconjugated small molecule was suboptimal they conjugated mouse antitumor necrosis factor (TNF) antibody using MP-Ala-Ala linker. Screening resulting drug conjugates (ADCs) provided better assessment efficacy physical properties, reinforcing need...
Transient receptor potential vanilloid 3 (TRPV3) is a Ca(2+)- and Na(+)-permeable channel with unique expression pattern. TRPV3 found in both neuronal non-neuronal tissues, including dorsal root ganglia, spinal cord, keratinocytes. Recent studies suggest that may play role inflammation, pain sensation, skin disorders. have been challenging, part due to lack of research tools such as selective antagonists. Herein, we provide the first detailed report on development potent antagonists...
We describe the discovery of a thioester-containing glucocorticoid receptor modulator (GRM) payload and corresponding antibody-drug conjugate (ADC). Payload