Solid-phase preparation method of efficient prostate-specific membrane antigen ligand PSMA-617

A PSMA-617, prostate-specific technology, applied in the field of solid-phase preparation of prostate-specific membrane antigen ligand PSMA-617, can solve the problems of unsuitability for large-scale, industrialized production, high production cost, and low product yield , to achieve the effect of low cost, increased yield and easy purification

Active Publication Date: 2019-01-04
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The technical problem to be solved by the present invention is to provide a preparation method of PSMA-617 aiming at the shortcomings of the existing synthesis method, such as low product yield, poor safety, high production cost, and unsuitability for large-scale and industrialized production

Method used

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  • Solid-phase preparation method of efficient prostate-specific membrane antigen ligand PSMA-617
  • Solid-phase preparation method of efficient prostate-specific membrane antigen ligand PSMA-617
  • Solid-phase preparation method of efficient prostate-specific membrane antigen ligand PSMA-617

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Experimental program
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Embodiment

[0039] 1. Resin Preparation

[0040] 1.1 Preparation of HMPA-PEGA resin

[0041] Weigh 5g of PEGA-AM resin (100-200mesh, 0.58mmol / g) into the polypeptide synthesizer, and DCM swells the resin. Then, HMP-Linker (3eq), HoBt (6eq), and DIC (4eq) were added to the resin to react for 3 hours, and washed with DMF to obtain HMPA-PEGA resin.

[0042] 1.2 Preparation of Fmoc-Lys(Mtt)-O-PEGA resin

[0043]Add the HMPA-PEGA resin (5g) to the polypeptide synthesizer, add the DMF solution of Fmoc-Lys(Mtt)-OH (2eq), DIC (2eq) and DMAP (0.1eq), stir the mixture mechanically under argon protection for 60min, and pump Dry the solvent and wash with 3 x 50 mL DMF. Finally, Fmoc-Lys(Mtt)-O-PEGA resin was obtained.

[0044] 2. Peptide conjugation

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Abstract

The invention discloses a solid-phase preparation method of an efficient prostate-specific membrane antigen ligand PSMA-617. By a solid-phase polypeptide synthesis method of amino acid protected by Fmoc, hydroxyl resin serves a starting point, and PSMA-617 sequences are sequentially synthesized. According to the method, high-risk reagent triphosgene used in the prior art is avoided, Pd(Ph3P)4 is omitted, synthesis safety is improved, the purity of an end-product is higher than 98.5%, the method has the advantages of low cost, less waste liquid, high efficiency and safety and easiness in purification, and large-scale and industrial production is facilitated.

Description

technical field [0001] The invention relates to the field of polypeptide synthesis, in particular to a high-efficiency solid phase preparation method of prostate specific membrane antigen ligand PSMA-617. Background technique [0002] Prostate specific membrane antigen (PSMA) is a type II transmembrane glycoprotein located on the surface of prostate epithelial cells, and its expression is significantly upregulated in most prostate cancer cells. Studies have shown that PSMA monoclonal antibodies and ligands labeled with nuclide and other substances have certain clinical application prospects in molecular imaging diagnosis and targeted therapy of prostate cancer. In order to improve the diagnosis and treatment of prostate cancer, researchers have developed a series of PSMA-targeted small molecule substances in recent years, which can specifically act on prostate cancer cells, including PSMA-617, which is 2-[3-(1- Carboxy-5-{3-naphthalen-2-yl-2-[(4-{[2-(4,7,10-tris-carboxymeth...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/083C07K1/04C07K1/06
CPCC07K5/0806Y02P20/55
Inventor 常民彭雅丽李墅薛宏祥
Owner LANZHOU UNIVERSITY
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