Chemically induced proximity and molecular glue
10.16438/j.0513-4870.2024-0092
- VernacularTitle:化学诱导临近效应和分子胶药物
- Author:
Zong-ru GUO
- Publication Type:Research Article
- Keywords:
chemically induced proximity;
molecular glue;
triad complex;
ubiquitin-proteasome system
- From:
Acta Pharmaceutica Sinica
2024;59(4):789-800
- CountryChina
- Language:Chinese
-
Abstract:
The chemically induced proximity (CIP) in biological realm is an important way to maintain the function of organism and cells. In recent years, CIP has been paid attention to and applied in the field of bio-medicines. Molecular glue and PROTAC are widely investigated for the treatment of tumors and immunopathy. Based upon the CIP principle molecular glue and PROTAC promote two proteins to approach each other, induce the complementary binding to triads, and then degrade the target protein or regulate functions. Different from conventional drugs, molecular glue acts as a catalyst, which induces two proteins to approach, bind and ubiquitinate, without taking part in the subsequent degradation process, so it can theoretically function in an infinite cycle. In this article, the development process, structural characteristics and functional characteristics of some molecular glues in clinical trials are briefly discussed from the viewpoint of medicinal chemistry.
