Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain.

Brain kinetics Dihydropyrazole-cored inhibitors Necroptosis PET imaging RIPK1

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
02 Sep 2024
Historique:
received: 24 06 2024
revised: 24 08 2024
accepted: 25 08 2024
medline: 11 9 2024
pubmed: 11 9 2024
entrez: 10 9 2024
Statut: aheadofprint

Résumé

Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) regulates programmed cell death and inflammation, contributing to a wide range of human pathologies, including inflammatory disorders, neurodegenerative conditions, and cancer. Despite this, no RIPK1 positron emission tomography (PET) ligand with significant in vivo specificity has been reported to date. In this work, we designed and synthesized a new family of dihydropyrazole-cored ligands suitable for

Identifiants

DOI: 10.1016/j.ejmech.2024.116803 PMID: 39255641
pubmed: 39255641
pii: S0223-5234(24)00684-6
doi: 10.1016/j.ejmech.2024.116803
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

116803

Informations de copyright

Copyright © 2024 Elsevier Masson SAS. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Wanqing Li (W)

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, PR China.

Xiaojun Zhang (X)

Department of Nuclear Medicine, Chinese PLA General Hospital, Beijing, 100853, PR China.

Jingyin Zhou (J)

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, PR China.

Xuan Di (X)

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, PR China.

Donglan Huang (D)

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, PR China.

Jie Ma (J)

Center of Cyclotron and PET Radiopharmaceuticals, Department of Nuclear Medicine and PET/CT-MRI Center, The First Affiliated Hospital of Jinan University, Guangzhou, 510630, PR China.

Kaixiang Zhou (K)

Center for Advanced Materials Research & Faculty of Arts and Sciences, Beijing Normal University, Zhuhai, 519087, PR China.

Jinming Zhang (J)

Department of Nuclear Medicine, Chinese PLA General Hospital, Beijing, 100853, PR China. Electronic address: zhangjm301@163.com.

Lu Wang (L)

Center of Cyclotron and PET Radiopharmaceuticals, Department of Nuclear Medicine and PET/CT-MRI Center, The First Affiliated Hospital of Jinan University, Guangzhou, 510630, PR China. Electronic address: l_wang1009@jnu.edu.cn.

Hualong Fu (H)

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, PR China. Electronic address: fuhualong@bnu.edu.cn.

Mengchao Cui (M)

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, PR China; Center for Advanced Materials Research & Faculty of Arts and Sciences, Beijing Normal University, Zhuhai, 519087, PR China.

Classifications MeSH