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Discovery of a cooperative mode of inhibiting RIPK1 kinase

ABSTRACT: By using Limited Proteolysis-Mass Spectrometry (LiP-MS) and Hydrogen Deuterium Exchange-Mass Spectrometry (HDX-MS) analysis, we identified the binding pocket of Nec-34 in RIPK1 kinase domain. This newly identified binding pocket of Nec-34 is distinct from distinct from that of Nec-1s.

ORGANISM(S): Homo Sapiens

SUBMITTER: Ying Li

PROVIDER: PXD024560 | iProX | Sun Mar 07 00:00:00 GMT 2021

REPOSITORIES: iProX

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Discovery of a cooperative mode of inhibiting RIPK1 kinase.

Meng Huyan H Wu Guowei G Zhao Xinsuo X Wang Anhui A Li Dekang D Tong Yilun Y Jin Taijie T Cao Ye Y Shan Bing B Hu Shichen S Li Ying Y Pan Lifeng L Tian Xiaoxu X Wu Ping P Peng Chao C Yuan Junying J Li Guohui G Tan Li L Wang Zhaoyin Z Li Ying Y

Cell discovery 20210601 1

RIPK1, a death domain-containing kinase, has been recognized as an important therapeutic target for inhibiting apoptosis, necroptosis, and inflammation under pathological conditions. RIPK1 kinase inhibitors have been advanced into clinical studies for the treatment of various human diseases. One of the current bottlenecks in developing RIPK1 inhibitors is to discover new approaches to inhibit this kinase as only limited chemotypes have been developed. Here we describe Necrostatin-34 (Nec-34), a ...[more]

PMID: 34075030

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Discovery of a cooperative mode of inhibiting RIPK1

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