Phase I: Synthesis
Linker Synthesis
- Engineered cleavable Val-Cit/Val-Ala linker
- Activated via NHS/Carbonate chemistry
- Conjugated to TMP778 analog
- Purified via HPLC & SEC
Phase II: Characterization
Structural Analysis
- Validated via ¹H-NMR and FT-IR
- Confirmed purity via LC-MS/HRMS
- Verified correct molecular mass
- Confirmed structural integrity
Phase III: Evaluation (Planned)
Antibody Conjugation
- Incubate in PBS, serum & enzymes
- Complete conjugation to antibody
- Confirm intracellular release via Cathepsin B digestion
Phase IV: Biologicals (Planned)
Biological Assays
- Conjugate via Maleimide–Thiol
- Evaluate RORγt inhibition
- Assays: FRET, Nuclear Receptor, & IL-17F Promoter