CONJUGATE OF A FLUORESCENT DYE WITH A PEPTIDE SUBSTANCE WHICH CONTAINS A PSMA-BINDING LIGAND BASED ON A UREA DERIVATIVE FOR VISUALIZING CELLS EXPRESSING PSMA, A METHOD FOR PRODUCTION THEREOF AND USE THEREOF
Obshchestvo s ogranichennoj otvetstvennostyu "Izvarino Farma"
发明人:
Machulkin Aleksej Eduardovich (RU),Мачулкин Алексей Эдуардович (RU),Uspenskaya Anastasiya Alekseevna (RU),Успенская Анастасия Алексеевна (RU),Ber Anton Petrovich (RU),Бер Антон Петрович (RU),Petrov St
申请号：
RU2019120551
公开号：
RU0002713151C1
申请日:
2019.07.02
申请国别(地区):
RU
年份:
2020
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention refers to organic and medical chemistry, as well as molecular biology and concerns a new class of compounds for visualizing cells and tissues expressing PSMA, including such as prostate cancer cells. Novel diagnostic conjugates are used to visualize pathogenic cells or tissues expressing PSMA, including PSMA ligand with a linker and a fluorescent dye, a method for preparing and using it. These compounds enable extending the range of diagnostic agents for imaging cells with high PSMA expression. Using the azido derivative of aminopentanoic acid enables to obtain a PSMA vector with a long hydrophobic linker and protected carboxy groups, which in turn facilitates its modification, increases output and reduces the amount of solvents used in the process due to considerable increase in solubility of the starting compound (PSMA vector with a long hydrophobic linker and protected carboxy groups). A key feature of the disclosed conjugate is the presence in the structure of a long hydrophobic linker, as well as additional aromatic fragments, presence of which promotes better binding of the disclosed conjugate with a protein target, by involving additional interactions between the compound and hydrophobic pockets in the structure of the hydrophobic tunnel of the protein target.EFFECT: high affinity and selectivity of action of the disclosed conjugates with respect to cells expressing PSMA.18 cl, 29 dwg, 8 tbl, 3 exИзобретение относится к области органической и медицинской химии, а также молекулярной биологии и касается нового класса соединений для визуализации клеток и тканей, экспрессирующих ПСМА, в том числе таких, как клетки рака предстательной железы. Заявляются новые диагностические конъюгаты для визуализации патогенных клеток либо тканей, экспрессирующих ПСМА, включающих ПСМА-лиганд с линкером и флуоресцентный краситель, способ его получения и применения. Техническим результатом заявляемой группы изобретений является высокая аффиннос
