New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic stroke

Ischemic stroke is a high-mortality disease that urgently requires new therapeutic strategies. Insufficient cerebral blood supply can induce poly (ADP-ribose) polymerase (PARP) activation and mitochondrial dysfunction, leading to tissue damage and motor dysfunction. We demonstrate that the expressio...

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Main Authors: Yang Cai, Hongfeng Gu, Lu Li, Xue Liu, Ying Bai, Ling Shen, Bing Han, Yungen Xu, Honghong Yao
Format: Article
Language:English
Published: Elsevier 2024-12-01
Series:Pharmacological Research
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Online Access:http://www.sciencedirect.com/science/article/pii/S1043661824004535
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author Yang Cai
Hongfeng Gu
Lu Li
Xue Liu
Ying Bai
Ling Shen
Bing Han
Yungen Xu
Honghong Yao
author_facet Yang Cai
Hongfeng Gu
Lu Li
Xue Liu
Ying Bai
Ling Shen
Bing Han
Yungen Xu
Honghong Yao
author_sort Yang Cai
collection DOAJ
description Ischemic stroke is a high-mortality disease that urgently requires new therapeutic strategies. Insufficient cerebral blood supply can induce poly (ADP-ribose) polymerase (PARP) activation and mitochondrial dysfunction, leading to tissue damage and motor dysfunction. We demonstrate that the expression of TCDD inducible PARP (TIPARP) is elevated in ischemic stroke patients and mice. Knockdown of Tiparp reduces brain infarction and promotes recovery of motor function in ischemic stroke mice. A rationally designed TIPARP inhibitor, XG-04-B1, promotes repair of brain injury and recovery of motor function in ischemic stroke mice. Mechanistically, XG-04-B1 increases neuronal plasticity and inhibits astrocyte activation in ischemic stroke mice. In addition, eukaryotic translation initiation factor 3 subunit B (EIF3B) is a direct target of TIPARP. TIPARP interacts with EIF3B through nucleoplasmic redistribution, leading to mitochondrial dysfunction. Knockdown of Tiparp and inhibition of TIPARP via XG-04-B1 restore mitochondrial homeostasis in ischemic stroke mice. Taken together, TIPARP activation contributes to mitochondrial dysfunction and subsequent brain injury, and is therefore a promising therapeutic target for stroke.
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institution Kabale University
issn 1096-1186
language English
publishDate 2024-12-01
publisher Elsevier
record_format Article
series Pharmacological Research
spelling doaj-art-6e63ff28802f41c1a8ccd607b387bbe42024-12-18T08:47:20ZengElsevierPharmacological Research1096-11862024-12-01210107508New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic strokeYang Cai0Hongfeng Gu1Lu Li2Xue Liu3Ying Bai4Ling Shen5Bing Han6Yungen Xu7Honghong Yao8Department of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, ChinaState Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, ChinaDepartment of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, ChinaDepartment of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, ChinaDepartment of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, ChinaDepartment of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, ChinaDepartment of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, China; Corresponding authors.State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China; Corresponding authors.Department of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, China; Co-innovation Center of Neuroregeneration, Nantong University, Nantong, China; Institute of Life Sciences, Key Laboratory of Developmental Genes and Human Disease, Southeast University, Nanjing, China; Corresponding author at: Department of Pharmacology, Jiangsu Provincial Key Laboratory of Critical Care Medicine, School of Medicine, Southeast University, Nanjing, China.Ischemic stroke is a high-mortality disease that urgently requires new therapeutic strategies. Insufficient cerebral blood supply can induce poly (ADP-ribose) polymerase (PARP) activation and mitochondrial dysfunction, leading to tissue damage and motor dysfunction. We demonstrate that the expression of TCDD inducible PARP (TIPARP) is elevated in ischemic stroke patients and mice. Knockdown of Tiparp reduces brain infarction and promotes recovery of motor function in ischemic stroke mice. A rationally designed TIPARP inhibitor, XG-04-B1, promotes repair of brain injury and recovery of motor function in ischemic stroke mice. Mechanistically, XG-04-B1 increases neuronal plasticity and inhibits astrocyte activation in ischemic stroke mice. In addition, eukaryotic translation initiation factor 3 subunit B (EIF3B) is a direct target of TIPARP. TIPARP interacts with EIF3B through nucleoplasmic redistribution, leading to mitochondrial dysfunction. Knockdown of Tiparp and inhibition of TIPARP via XG-04-B1 restore mitochondrial homeostasis in ischemic stroke mice. Taken together, TIPARP activation contributes to mitochondrial dysfunction and subsequent brain injury, and is therefore a promising therapeutic target for stroke.http://www.sciencedirect.com/science/article/pii/S1043661824004535PARP7Mitochondrial dysfunctionNeuroprotective agentsPharmacologyStrokeDrug design
spellingShingle Yang Cai
Hongfeng Gu
Lu Li
Xue Liu
Ying Bai
Ling Shen
Bing Han
Yungen Xu
Honghong Yao
New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic stroke
Pharmacological Research
PARP7
Mitochondrial dysfunction
Neuroprotective agents
Pharmacology
Stroke
Drug design
title New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic stroke
title_full New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic stroke
title_fullStr New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic stroke
title_full_unstemmed New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic stroke
title_short New TIPARP inhibitor rescues mitochondrial function and brain injury in ischemic stroke
title_sort new tiparp inhibitor rescues mitochondrial function and brain injury in ischemic stroke
topic PARP7
Mitochondrial dysfunction
Neuroprotective agents
Pharmacology
Stroke
Drug design
url http://www.sciencedirect.com/science/article/pii/S1043661824004535
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