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CD25 targeting polypeptide, molecular probe and application

A technology targeting peptides and molecular probes, applied in peptides, peptide preparation methods, organic chemistry, etc., can solve problems such as slow removal speed, difficult imaging effect, patient pain, etc., achieve high affinity, and improve signal-to-noise ratio , the effect of high intake

Active Publication Date: 2022-07-22
BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since IL-2 is a biologically active molecule, it will produce certain biological effects after intravenous injection into the human body, and may bring discomfort such as pain and fever to patients after injection.
Moreover, due to the relatively large molecular weight of IL-2, its clearance rate in the body is relatively slow, and it is difficult to obtain high-quality imaging effects in a short time by labeling IL-2 molecules with short half-life radionuclides

Method used

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  • CD25 targeting polypeptide, molecular probe and application
  • CD25 targeting polypeptide, molecular probe and application
  • CD25 targeting polypeptide, molecular probe and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation of DA-1 RFK(GGG-DOTA)FY[OBn];

[0051] .

[0052] (1) Resin swelling, put 2-CTC resin (50 mg, 0.015 mmol~0.15 mmol) into the reaction tube, add DCM (4 mL), and shake for 30 min. (2) Connect the first amino acid, filter out the solvent through sand core, add 2 times molar excess of Fmoc-L-Tyr(Bzl)-OH (148 mg, 0.30 mmol), add DMF to dissolve, and then add 10 times molar Excess DIEA (261 μL, 1.50 mmol) was shaken for 60 min. Block with methanol. (3) Deprotection, remove methanol, add 20% piperidine DMF solution (3 mL) for 5 min, remove and add 20% piperidine DMF solution (3 mL) for 15 min. (4) Detection, remove the piperidine solution, take more than ten resins, wash with ethanol three times, add detection reagent for detection, heat at 105℃-110℃ for 5min, and it turns dark blue as a positive reaction. (E) Wash, DMF (4 mL) twice, DCM (4 mL) twice, DMF (4 mL) twice. (VI) Condensation, adding the next Fmoc-protected amino acid Fmoc-L-Phe-OH (116 mg, 0.30 ...

Embodiment 2

[0054] Preparation of DA-3 DOTA-(PEG)2-RFKFYE.

[0055] .

[0056] (1) Resin swelling: Put 2-CTC resin (50 mg, 0.015 mmol~0.15 mmol) into the reaction tube, add dichloromethane (4 mL), and shake for 30 min. (2) Connection of the first amino acid: The solvent was filtered off through a sand core, and a 2-fold molar excess of N-fluorenemethoxycarbonyl-L-glutamic acid-γ-tert-butyl ester monohydrate (133 mg, 0.30 mmol) was added, Add DMF to dissolve, then add 10-fold molar excess DIEA (261 μL, 1.50 mmol), shake for 60 min, and block with methanol. (3) Deprotection: remove methanol, add 20% piperidine DMF solution (3 mL), stir for 5 min, remove the solvent, add 20% piperidine DMF solution (3 mL), and stir for 15 min. (4) Detection: remove the piperidine solution, take more than ten resins, wash with ethanol three times, add detection reagent for detection, heat at 105 ℃-110 ℃ for 5 min, and it turns dark blue as a positive reaction. (5) Washing: DMF (4 mL) twice, DCM (4 mL) tw...

Embodiment 3

[0058] Preparation of DA-6 DOTA-(PEG)2-RFrFY:

[0059] .

[0060](1) Resin swelling: Put 2-CTC resin (50 mg, 0.015 mmol~0.15 mmol) into the reaction tube, add dichloromethane (4 mL), and shake for 30 min. (2) First amino acid connection: filter out the solvent through sand core, add 2 times molar excess of Fmoc-O-tert-butyl-L-tyrosine (137.70 mg, 0.30 mmol), add DMF to dissolve, and then add 10 times more Molar excess of DIEA (261 μL, 1.50 mmol), shaken for 60 min, and blocked with methanol. (3) Deprotection: remove methanol, add 20% piperidine DMF solution (3 mL), stir for 5 min, remove the solvent, add 20% piperidine DMF solution (3 mL), and stir for 15 min. (4) Detection: Remove the piperidine solution, take more than ten resins, wash with ethanol three times, add detection reagents for detection, heat at 105℃-110℃ for 5 minutes, and turn dark blue as a positive reaction. (5) Washing: DMF (4 mL) twice, DCM (4 mL) twice, DMF (4 mL) twice. (VI) Condensation: Add 2 times...

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Abstract

The invention belongs to the field of nuclear medicine imaging agents, and relates to a CD25 targeting polypeptide, a molecular probe and application. The amino acid sequence of the polypeptide is as follows: i) X1X2X3X4X5; or ii) an amino acid sequence formed by connecting a tag to the N terminal or C terminal of i); wherein X1 is arginine, lysine or histidine; x2 is phenylalanine, tyrosine, benzyl tyrosine or halogenated phenylalanine; x3 is arginine, lysine or histidine; x4 is phenylalanine, tyrosine, benzyl tyrosine or halogenated phenylalanine; and X5 is phenylalanine, tyrosine, benzyl tyrosine or halogenated phenylalanine. The CD25 polypeptide and the nuclide labeled probe thereof provided by the invention have obvious tumor uptake and clear tumor-to-noise ratio, effectively improve the signal-to-noise ratio in the imaging diagnosis process, and have relatively high application value.

Description

technical field [0001] The invention belongs to the field of nuclear medicine imaging agents, and in particular, relates to a class of polypeptide derivatives and molecular probes that can be used to target the CD25 target of CAR-T cells, as well as preparation methods and applications thereof. Background technique [0002] CAR-T (Chimeric Antigen Receptor T Cell) therapy, that is, chimeric antigen receptor T cell therapy, is currently a hot research frontier in clinical tumor treatment. According to the official website of Clinical Trials, there are hundreds of CAR-T clinical trials underway around the world, including not only CAR-T therapy targeting CD19, CD20, etc., but also targeting mesothelial tumors. Solid tumor CAR-T therapy targeting targets such as Mesothelin (MSLN) and human epidermal growth factor receptor-2 (HER-2). [0003] Despite great success in clinical trials, in some patients, CAR-T cells have limited ability to survive and sustain expansion, or produce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/13C07K1/06A61K51/08A61K51/04A61K103/00
CPCC07K7/06A61K51/08A61K51/0482
Inventor 杨志刘福涛王帅亮朱华王培王风
Owner BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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