Discovery of novel serine/threonine protein phosphatase 1 inhibitors from traditional Chinese medicine through virtual screening and biological assays

Zhu, Yehua; Gao, Yi Qin; Sun, Xinjie; Wang, Chao; Rui, Xiyan; Si, Dongjuan; Zhu, Junru; Li, Wei; Liu, Jian

doi:10.1080/07391102.2019.1702588

Cited by 5 publications

(2 citation statements)

References 51 publications

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“…PP1 is a serine/threonine protein phosphatase that dephosphorylates diverse cellular substrates, acting as a key regulator of some cellular processes [ 44 ]. I1PP1 is the first recognized endogenous inhibitor of PP1 and greatly low expressed in cardiomyocytes under basal conditions.…”

Section: Discussionmentioning

confidence: 99%

RIPK3‐Mediated Necroptosis in Diabetic Cardiomyopathy Requires CaMKII Activation

Chen

Hua

et al. 2021

Oxidative Medicine and Cellular Longevity

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Activation of Ca2+/calmodulin-dependent protein kinase (CaMKII) has been proved to play a vital role in cardiovascular diseases. Receptor-interaction protein kinase 3- (RIPK3-) mediated necroptosis has crucially participated in cardiac dysfunction. The study is aimed at investigating the effect as well as the mechanism of CaMKII activation and necroptosis on diabetic cardiomyopathy (DCM). Wild-type (WT) and the RIPK3 gene knockout (RIPK3-/-) mice were intraperitoneally injected with 60 mg/kg/d streptozotocin (STZ) for 5 consecutive days. After 12 w of feeding, 100 μL recombinant adenovirus solution carrying inhibitor 1 of protein phosphatase 1 (I1PP1) gene was injected into the caudal vein of mice. Echocardiography, myocardial injury, CaMKII activity, necroptosis, RIPK1 expression, mixed lineage kinase domain-like protein (MLKL) phosphorylation, and mitochondrial ultrastructure were measured. The results showed that cardiac dysfunction, CaMKII activation, and necroptosis were aggravated in streptozotocin- (STZ-) stimulated mice, as well as in (Lepr) KO/KO (db/db) mice. RIPK3 deficiency alleviated cardiac dysfunction, CaMKII activation, and necroptosis in DCM. Furthermore, I1PP1 overexpression reversed cardiac dysfunction, myocardial injury and necroptosis augment, and CaMKII activity enhancement in WT mice with DCM but not in RIPK3-/- mice with DCM. The present study demonstrated that CaMKII activation and necroptosis augment in DCM via a RIPK3-dependent manner, which may provide therapeutic strategies for DCM.

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Section: Discussionmentioning

confidence: 99%

RIPK3‐Mediated Necroptosis in Diabetic Cardiomyopathy Requires CaMKII Activation

Chen

Hua

et al. 2021

Oxidative Medicine and Cellular Longevity

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“…COVID-19 is an infectious disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) [ 1 ]. The most common symptoms include headache [ 2 ], loss of smell and taste [ 3 , 4 ], nasal congestion and runny nose, cough, muscle aches, sore throat, fever [ 2 ], diarrhea, and dyspnea. Although some infected individuals have no obvious symptoms, they may still transmit the virus, increasing the risk of disease transmission [ 5 , 6 , 7 ].…”

Section: Introductionmentioning

confidence: 99%

Progress on COVID-19 Chemotherapeutics Discovery and Novel Technology

et al. 2022

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COVID-19 is an infectious disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a novel highly contagious and pathogenic coronavirus that emerged in late 2019. SARS-CoV-2 spreads primarily through virus-containing droplets and small particles of air pollution, which greatly increases the risk of inhaling these virus particles when people are in close proximity. COVID-19 is spreading across the world, and the COVID-19 pandemic poses a threat to human health and public safety. To date, there are no specific vaccines or effective drugs against SARS-CoV-2. In this review, we focus on the enzyme targets of the virus and host that may be critical for the discovery of chemical compounds and natural products as antiviral drugs, and describe the development of potential antiviral drugs in the preclinical and clinical stages. At the same time, we summarize novel emerging technologies applied to the research on new drug development and the pathological mechanisms of COVID-19.

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Computer especially AI-assisted drug virtual screening and design in traditional Chinese medicine

et al. 2022

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Discovery of novel serine/threonine protein phosphatase 1 inhibitors from traditional Chinese medicine through virtual screening and biological assays

Cited by 5 publications

References 51 publications

RIPK3‐Mediated Necroptosis in Diabetic Cardiomyopathy Requires CaMKII Activation

RIPK3‐Mediated Necroptosis in Diabetic Cardiomyopathy Requires CaMKII Activation

Progress on COVID-19 Chemotherapeutics Discovery and Novel Technology

Computer especially AI-assisted drug virtual screening and design in traditional Chinese medicine

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