Immunosuppression modulating compounds
A compound, animal technology, applied in the field of modification or derivatives of therapeutic agents, modification and derivatives of therapeutic agents, and can solve problems such as unmet medical needs
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Embodiment 1
[0435]
[0436] Synthesis of (SEQUENCE ID NO47)
[0437] Linear Fragment: Synthesis of FRVTQKFRVTQ[Ahx]LAPKAQIKE-NH2
[0438] Desiccated CLEAR-amide resin ((100-200 mesh) 0.4 mmol / g, 0.5 g) was dispensed in two polyethylene containers equipped with polypropylene filters. The synthesis of linear peptides in solid phase was automated using the Symphony parallel synthesizer (PTI) using the synthesis programs mentioned in the table below. Expansion (growth, swelling, swelling), C-terminal amino acid [Fmoc-Glu(OtBu)-OH] linkage and capping of the peptidyl resin were performed following the scheme in Table I. Subsequent amino acid couplings were performed as mentioned in Table II. The amino acids used in the synthesis are Fmoc Phe-OH, Fmoc-Arg(Pbf)-OH, Fmoc-Val-OH, Fmoc-Thr(OtBu)-OH, Fmoc-Gln(Trt)-OH, Fmoc-Lys(Boc )-OH, Fmoc-Ahx-OH (Fmoc-6-aminocaproic acid), Fmoc-Leu-OH, Fmoc-Ala-OH, Fmoc-Pro-OH, Fmoc-Ile-OH. After linear synthesis of fragments in an automated peptide synthe...
Embodiment 2
[0441]
[0442] Synthesis of (SEQUENCE ID NO49)
[0443] Synthesis of Linear Fragment-Fmoc-FRVTQLAPKAQIKE
[0444] Powdered CLEAR-amide resin ((100-200 mesh) 0.4 mmol / g, 0.5 g) was dispensed in two polyethylene containers equipped with polypropylene filters. The synthesis of linear peptides in solid phase was automated using the Symphony Parallel Synthesizer (PTI) using the synthesis programs mentioned in the table below. Follow the protocol in Table I for extension (growth), C-terminal amino acid [Fmoc-Glu(OtBu)-OH] linkage, and capping of the peptidyl resin. Subsequent amino acid couplings were performed as mentioned in Table II. The amino acids used in the synthesis are Fmoc Phe-OH, Fmoc-Arg(Pbf)-OH, Fmoc-Val-OH, Fmoc-Thr(OtBu)-OH, Fmoc-Gln(Trt)-OH, Fmoc-Lys(Boc )-OH, Fmoc-Leu-OH, Fmoc-Ala-OH, Fmoc-Pro-OH, Fmoc-Ile-OH. After completion of the Fmoc-Phe-OH coupling, the resin was removed from the peptide synthesizer and manually coupled as follows.
[0445]The Fmoc-Ph...
Embodiment 3
[0447]
[0448] Synthesis of (SEQUENCE ID NO102)
[0449] Powdered CLEAR-amide resin ((100-200 mesh) 0.49 mmol / g, 0.5 g) was dispensed in two polyethylene containers equipped with polypropylene filters. The synthesis of linear peptides in solid phase was automated using the Symphony Parallel Synthesizer (PTI) using the synthesis programs mentioned in the table below. Follow the protocol in Table I for extension (growth), C-terminal amino acid [Fmoc-Ser(OtBu)-OH] linkage, and capping of the peptidyl resin. Subsequent Fmoc-amino acids were coupled as mentioned in Table II. The amino acids used in the synthesis are Fmoc-Glu(OtBu)-OH, Fmoc-Tyr(OtBu)-OH, Fmoc-Trp(Boc)-OH, Fmoc-Asp(OtBu)-OH, Fmoc-Val-OH, Fmoc -Thr(OtBu)-OH, Fmoc-Gln(Trt)-OH, Fmoc-Lys(Boc)-OH, Fmoc-Leu-OH, Fmoc-Asn(Trt)-OH, Fmoc-Ala-OH, Fmoc-Pro -OH, Fmoc-Ile-OH, Fmoc-Ahx-OH. In the case of biotin coupling, biotin (0.15 g in 2.5 mL DMF) was dissolved in DMF / DMSO (1:1) and added manually to the reaction vessel ...
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