A5036282788- Monoclonal and Polyclonal Antibodies Research
- Crystallization and Solubility Studies
- Cytokine Signaling Pathways and Interactions
- X-ray Diffraction in Crystallography
- Asthma and respiratory diseases
- T-cell and B-cell Immunology
- Extracellular vesicles in disease
- MicroRNA in disease regulation
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Protein purification and stability
- HER2/EGFR in Cancer Research
- Bone and Joint Diseases
Tianjin Economic-Technological Development Area
2022-2023
WuXi AppTec (China)
2022-2023
Union Hospital
2022
Huazhong University of Science and Technology
2022
Glucocorticoid receptor modulators (GRM) are the first-line treatment for many immune diseases, but unwanted side effects restrict chronic dosing. However, targeted delivery of a GRM payload via an immunology antibody-drug conjugate (iADC) may deliver significant efficacy at doses that do not lead to effects. We initiated our α-TNF-GRM ADC project focusing on identifying optimal and linker afforded stable attachment both antibody, resulting in identification synthetically accessible...
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...
A glucocorticoid receptor modulator (GRM) was conjugated to a mouse anti-TNF antibody using various dipeptide linkers. Impact of linkers on ADC physical properties, including solubility, hydrophobicity, and aggregation were evaluated.
Maleimide is used in antibody–drug conjugate (ADC) generation to attach the drug-linker antibody. linkers with hydrolysis-enabled maleimides were designed. Corresponding ADCs made and subjected thermal stress, succinimide ring hydrolysis drug release measured.