Synthesis of a protacs compound containing a pure carbon chain targeting acl y and its application in anti-nash

By developing PROTAC compounds with carbon chains as linking chains, and utilizing PROTAC technology to target and degrade ACLY proteins, the problem of single target in NASH treatment has been solved, providing a low-toxicity and highly effective anti-non-alcoholic steatohepatitis drug and broadening the application field of PROTAC technology.

CN119899171BActive Publication Date: 2026-03-10TIANJIN UNIV OF SCI & TECH
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Patent Information

Application Number
CN202411353603.X
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-09-26
Publication Date
2026-03-10
Estimated Expiration
2044-09-26

AI Technical Summary

Technical Problem

Current NASH treatments have single targets and cannot effectively address the complex pathogenesis, and PROTAC technology has not yet been widely used in the field of NASH.

Method used

Develop PROTAC compounds with carbon chains as linkers, target and degrade ACLY proteins using PROTAC technology, and prepare PROTAC compounds with anti-NASH activity for the preparation of drugs that target and degrade ACLY.

Benefits of technology

The synthesized PROTAC compounds exhibited low toxicity and high lipid-lowering activity in human hepatocellular carcinoma cells HepG2, normal human hepatocytes L02, and human umbilical vein endothelial cells HUVEC, effectively reducing TG content. They have become a new generation of low-toxicity and high-efficiency anti-non-alcoholic steatohepatitis drugs, expanding the application field of PROTAC technology.

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Abstract

The application belongs to the technical field of biology and medicine, and discloses a PROTAC compound with a carbon chain as a connecting chain, which is developed based on a PROTAC technology, and a structural general formula of the PROTAC compound is formula 1: wherein R is -(CH2) n -, and n is 3-8. The synthesized PROTAC compound is a new compound, has a TG content reducing activity in a high-fat model established by L02 and HepG2, and has a low-toxicity activity in human hepatoma cells HepG2, human normal liver cells L02 and human umbilical vein endothelial cells HUVEC compared with a warhead. The synthesized PROTAC compound is a new type of anti-non-alcoholic fatty liver disease drug with low toxicity and high efficiency. The application of the PROTAC technology is widened while developing an efficient treatment of anti-non-alcoholic fatty liver disease.
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