FGFR4 targeting affinity peptide and application thereof
A tumor-targeting, YQGF-2 technology, which is applied in the direction of medical preparations, peptides, preparations for in vivo tests, etc., can solve the problems of high expression level and limited expression, achieve weak autofluorescence, promote Concentration and retention, stability improvement effect
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Embodiment 1
[0048] Example 1 takes the polypeptide YQGF-1 as an example, including the following steps:
[0049] (1) Resin swelling
[0050] Add a certain amount of Rink Amide MBHA resin into the reaction column, then add an appropriate amount of dichloromethane (DCM), and blow nitrogen slightly for 10-30 minutes to fully swell the resin. The dichloromethane solution was sucked dry, washed 3 times with dimethylformamide (DMF) and drained.
[0051] (2) Remove Fmoc
[0052] Add 20% hexahydropyridine in DMF to the reaction column, and deprotect once every 5 minutes and once every 8 minutes. After the reaction, the resin was washed three times with DMF, DCM, and DMF respectively.
[0053] (3) Coupling
[0054] Accurately weigh Fmoc-IIe-OH and O-benzotriazole-tetramethyluronium hexafluorophosphate (HBTU) which is 3 times the mole number of the feed resin, completely dissolve in DMF, add N,N-diisopropyl After diethylamine (DIPEA) activates the carboxyl group, add the solution to the reacti...
Embodiment 2
[0059] Example 2 Preparation of polypeptide YQGF-X (X=2-6)
[0060] Prepare the tumor-targeting peptide YQGF-2 according to the method of Example 1, the sequence is the polypeptide shown in SEQ ID NO: 2, confirmed by mass spectrometry [M-H] - =933. Tumor targeting peptide YQGF-3, the sequence is the polypeptide shown in SEQ ID NO:3, confirmed by mass spectrometry [M-H] - =1953. Tumor targeting peptide YQGF-4, the sequence is the polypeptide shown in SEQ ID NO:4, confirmed by mass spectrometry [M-H] - =943. Tumor targeting peptide YQGF-5, the sequence is the polypeptide shown in SEQ ID NO:5, [M-H] - =933. Tumor targeting peptide YQGF-6, the sequence is the polypeptide shown in SEQ ID NO: 6, [M-H] - =933.
Embodiment 3
[0061] Example 3 Preparation of fluorescent targeting compound MPA-YQGF-1
[0062] MPA comes from an invention patent previously applied by our research group, authorized patent number: CN101440282.
[0063] (1) Dissolve 0.02mmol MPA in 200μL ultra-dry DMSO, add 3.7mg 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride and 2.2mg N-hydroxysuccinyl Amine (EDCI / NHS) (molar ratio MPA:EDCI:NHS=1:1.5:1.5), react in the dark for 4 hours, and carry out carboxyl activation reaction.
[0064] (2) Take 0.02mmol of the solid-phase synthesized polypeptide YQGF-1 (X=1-6), add 0.1mmol triethylamine and 200μL ultra-dry DMSO into a 5mL reaction bottle, and react for 10min under nitrogen protection; the above reaction (1 ) solution into the reaction solution of (2), stirred at room temperature for 12 hours;
[0065] (3) After the reaction, the reaction solution was concentrated by freeze-drying, then diluted with distilled water, and separated and purified with the preparative liquid ph...
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