2. Academic Validation
  3. Facilitating the development of molecular glues: Opportunities from serendipity and rational design

Facilitating the development of molecular glues: Opportunities from serendipity and rational design

  • Eur J Med Chem. 2024 Jan 5:263:115950. doi: 10.1016/j.ejmech.2023.115950.
Weiqing Jiang 1,  Yunhan Jiang 2,  Youfu Luo 3,  Wenliang Qiao 4,  Tao Yang 5
Affiliations

Affiliations

  • 1 Laboratory of Human Diseases and Immunotherapies, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China; Institute of Immunology and Inflammation, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, 610041, China.
  • 2 Laboratory of Human Diseases and Immunotherapies, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China; Institute of Immunology and Inflammation, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, 610041, China; Cardiovascular Surgery Research Laboratory, West China Hospital, Sichuan University, Chengdu, 610041, China.
  • 3 Laboratory of Human Diseases and Immunotherapies, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China. Electronic address: luo_youfu@scu.edu.cn.
  • 4 Lung Cancer Center, Laboratory of Lung Cancer, West China Hospital, Sichuan University, Chengdu, 610041, China. Electronic address: qiaowenliang@wchscu.cn.
  • 5 Laboratory of Human Diseases and Immunotherapies, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China; Institute of Immunology and Inflammation, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, 610041, China. Electronic address: yangtao@wchscu.cn.
PMID: 37984298 DOI: 10.1016/j.ejmech.2023.115950
Abstract

Molecular Glues can specifically induce interactions between two or more proteins to modulate biological functions and have been proven to be a powerful therapeutic modality in drug discovery. It plays a variety of vital roles in several biological processes, such as complex stabilization, interactome modulation and transporter inhibition, thus enabling challenging therapeutic targets to be druggable. Most known Molecular Glues were identified serendipitously, such as IMiDs, Auxin, and rapamycin. In recent years, more rational strategies were explored with the development of chemical biology and a deep understanding of the interaction between Molecular Glues and proteins, which led to the rational discovery of several Molecular Glues. Thus, in this review, we aim to highlight the discovery strategies of Molecular Glues from three aspects: serendipitous discovery, screening methods and rational design principles. We expect that this review will provide a reasonable reference and insights for the discovery of Molecular Glues.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z