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Advances in RIPK1 kinase inhibitors.

ABSTRACT: Programmed necrosis is a new modulated cell death mode with necrotizing morphological characteristics. Receptor interacting protein 1 (RIPK1) is a critical mediator of the programmed necrosis pathway that is involved in stroke, myocardial infarction, fatal systemic inflammatory response syndrome, Alzheimer's disease, and malignancy. At present, the reported inhibitors are divided into four categories. The first category is the type I ATP-competitive kinase inhibitors that targets the area occupied by the ATP adenylate ring; The second category is type Ⅱ ATP competitive kinase inhibitors targeting the DLG-out conformation of RIPK1; The third category is type Ⅲ kinase inhibitors that compete for binding to allosteric sites near ATP pockets; The last category is others. This paper reviews the structure, biological function, and recent research progress of receptor interaction protein-1 kinase inhibitors.

SUBMITTER: Chen L

PROVIDER: S-EPMC9554302 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

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Advances in RIPK1 kinase inhibitors.

Chen Lu L Zhang Xiaoqin X Ou Yaqing Y Liu Maoyu M Yu Dongke D Song Zhiheng Z Niu Lihong L Zhang Lijuan L Shi Jianyou J

Frontiers in pharmacology 20220928

Programmed necrosis is a new modulated cell death mode with necrotizing morphological characteristics. Receptor interacting protein 1 (RIPK<b>1</b>) is a critical mediator of the programmed necrosis pathway that is involved in stroke, myocardial infarction, fatal systemic inflammatory response syndrome, Alzheimer's disease, and malignancy. At present, the reported inhibitors are divided into four categories. The first category is the type I ATP-competitive kinase inhibitors that targets the area ...[more]

PMID: 36249746

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