Design of MHC class II (DR4) ligands using conformationally restricted imino acids at p3 and p5
| Autor: | Susan L. Woulfe, Michelle L. Zacheis, Jennifer L. Vuletich, Louis J. Bedell, Christine P. Bono, Susan C. Howard, Joseph K. Welply, Gunnar J. Hanson |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
musculoskeletal diseases
chemistry.chemical_classification MHC class II Imino acid biology Stereochemistry Ligand Organic Chemistry Clinical Biochemistry Pharmaceutical Science Major histocompatibility complex Biochemistry Pentapeptide repeat chemistry.chemical_compound chemistry Drug Discovery biology.protein Molecular Medicine Proline Molecular Biology IC50 Pipecolic acid |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 6:1931-1936 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/0960-894x(96)00348-4 |
| Popis: | High potency synthetic ligands were designed for rheumatoid arthritis linked Class II MHC, DR4 Dw4. The design strategy utilized isosteric replacements at the p1 and p7 positions and conformational restriction with imino acids pipecolic acid (Pec) and proline at the solvent exposed residues p3 and p5. In particular, SC-67655, (S)-CBA-Val-Pec-Asp-Pro-Thr-NH-n-Pr (IC50 = 50 nM) is a potent and stable pentapeptide DR4 ligand. |
| Databáze: | OpenAIRE |
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