Polypeptide with CXCR4 protein agonizing activity and application and medicinal composition thereof
A mixture and pharmaceutical technology, applied in the field of polypeptides with CXCR4 protein agonistic activity and their applications and pharmaceutical compositions, can solve the problems of lack of treatment methods
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Embodiment 1
[0083] Example 1: Synthesis of H0001
[0084] Adopt Fmoc solid-phase synthesis method to synthesize, and concrete preparation method is as follows:
[0085] Weigh 357mg of Rink Amide-MBHA resin with a substitution degree of 0.28mmol / g in a solid phase reactor, add DCM to swell for 30min, then add 20% PIP / DMF solution for deprotection twice, the first time is 5min, and the second time is 20min . Wash several times with DCM and DMF respectively, and drain. It was detected by Kaiser test, and the resin or solution showed blue color, indicating that it had been deprotected.
[0086] Add Fmoc-D-Pro-OH (169mg, 0.5mmol), DIC (103mg, 0.5mmol), HOBt (68mg, 0.5mmol), DMF (4mL) into the solid phase reactor, and react at room temperature for 2h. After the coupling is completed, wash with DCM and DMF several times, and drain. Then use the Kaiser test to detect, and proceed to the next step after the detection is passed. Wash and dry the resin to obtain Fmoc-Pro-Rink Amide-MBHA resin. ...
Embodiment 2
[0089] The synthesis of embodiment 2 H0006
[0090] Weigh 357mg of Rink Amide-MBHA resin with a substitution degree of 0.28mmol / g in a solid phase reactor, add DCM to swell for 30min, then add 20% PIP / DMF solution for deprotection twice, the first time is 5min, and the second time is 20min . Wash several times with DCM and DMF respectively, and drain. It was detected by Kaiser test, and the resin or solution showed blue color, indicating that it had been deprotected.
[0091]Add Fmoc-Lys(Dde)-OH (266mg, 0.5mmol), DIC (103mg, 0.5mmol), HOBt (68mg, 0.5mmol), DMF (4mL) into the solid phase reactor, and react at room temperature for 2h. After the coupling is completed, the resin is washed and dried to obtain Fmoc-Lys(Dde)-Rink Amide-MBHA resin. The Kaiser test is used for detection, and the next reaction is carried out after the detection is passed. Add 20% PIP / DMF solution for deprotection twice, the first time is 5 minutes, the second time is 20 minutes, and the Fmoc protect...
Embodiment 3
[0096] Embodiment 3: polypeptide compound of the present invention
[0097] The amino acid sequence of the CXCR4 activity regulating polypeptide is shown in Table 1, and was synthesized according to the method described in Example 1 or Example 2.
[0098] Table 1 CXCR4 activity regulating polypeptide and its amino acid sequence
[0099]
[0100] a Italics represent D-type amino acids
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