Learning from COVID-19: How drug hunters can prepare for the next pandemic
Drug Discov Today. 2023 Jul 21:103723. doi: 10.1016/j.drudis.2023.103723. Online ahead of print.ABSTRACTOver 3 years, the SARS-CoV-2 pandemic killed nearly 7 million people and infected more than 767 million globally. During this time, our very small company was able to contribute to antiviral drug discovery efforts through global collaborations with other researchers, which enabled the identification and repurposing of multiple molecules with activity against SARS-CoV-2 including pyronaridine tetraphosphate, tilorone, quinacrine, vandetanib, lumefantrine, cetylpyridinium chloride, raloxifene, carvedilol, olmutinib, dacomi...
Source: Drug Discovery Today - July 23, 2023 Category: Drugs & Pharmacology Authors: Ana C Puhl Thomas Lane Sean Ekins Source Type: research
Tamoxifen and the risk of breast cancer in women with a BRCA1 or BRCA2 mutation
ConclusionChemoprevention may be an effective risk-reduction option forBRCA mutation carriers, but further studies with longer follow-up are necessary. (Source: Breast Cancer Research and Treatment)
Source: Breast Cancer Research and Treatment - July 22, 2023 Category: Cancer & Oncology Source Type: research
The role of PKN1 in glioma pathogenesis and the antiglioma effect of raloxifene targeting PKN1
J Cell Mol Med. 2023 Jul 21. doi: 10.1111/jcmm.17860. Online ahead of print.ABSTRACTPKN1 (protein kinase N1), a serine/threonine protein kinase family member, is associated with various cancers. However, the role of PKN1 in gliomas has rarely been studied. We suggest that PKN1 expression in glioma specimens is considerably upregulated and positively correlates with the histopathological grading of gliomas. Knocking down PKN1 expression in glioblastoma (GBM) cells inhibits GBM cell proliferation, invasion and migration and promotes apoptosis. In addition, yes-associated protein (YAP) expression, an essential effector of the...
Source: J Cell Mol Med - July 22, 2023 Category: Molecular Biology Authors: Yubing Hao Zelin Li Anling Zhang Li Sun Guangxiu Wang Hu Wang Zhifan Jia Source Type: research
The role of PKN1 in glioma pathogenesis and the antiglioma effect of raloxifene targeting PKN1
J Cell Mol Med. 2023 Jul 21. doi: 10.1111/jcmm.17860. Online ahead of print.ABSTRACTPKN1 (protein kinase N1), a serine/threonine protein kinase family member, is associated with various cancers. However, the role of PKN1 in gliomas has rarely been studied. We suggest that PKN1 expression in glioma specimens is considerably upregulated and positively correlates with the histopathological grading of gliomas. Knocking down PKN1 expression in glioblastoma (GBM) cells inhibits GBM cell proliferation, invasion and migration and promotes apoptosis. In addition, yes-associated protein (YAP) expression, an essential effector of the...
Source: Molecular Medicine - July 22, 2023 Category: Molecular Biology Authors: Yubing Hao Zelin Li Anling Zhang Li Sun Guangxiu Wang Hu Wang Zhifan Jia Source Type: research
The role of PKN1 in glioma pathogenesis and the antiglioma effect of raloxifene targeting PKN1
J Cell Mol Med. 2023 Jul 21. doi: 10.1111/jcmm.17860. Online ahead of print.ABSTRACTPKN1 (protein kinase N1), a serine/threonine protein kinase family member, is associated with various cancers. However, the role of PKN1 in gliomas has rarely been studied. We suggest that PKN1 expression in glioma specimens is considerably upregulated and positively correlates with the histopathological grading of gliomas. Knocking down PKN1 expression in glioblastoma (GBM) cells inhibits GBM cell proliferation, invasion and migration and promotes apoptosis. In addition, yes-associated protein (YAP) expression, an essential effector of the...
Source: J Cell Mol Med - July 22, 2023 Category: Molecular Biology Authors: Yubing Hao Zelin Li Anling Zhang Li Sun Guangxiu Wang Hu Wang Zhifan Jia Source Type: research
The role of PKN1 in glioma pathogenesis and the antiglioma effect of raloxifene targeting PKN1
J Cell Mol Med. 2023 Jul 21. doi: 10.1111/jcmm.17860. Online ahead of print.ABSTRACTPKN1 (protein kinase N1), a serine/threonine protein kinase family member, is associated with various cancers. However, the role of PKN1 in gliomas has rarely been studied. We suggest that PKN1 expression in glioma specimens is considerably upregulated and positively correlates with the histopathological grading of gliomas. Knocking down PKN1 expression in glioblastoma (GBM) cells inhibits GBM cell proliferation, invasion and migration and promotes apoptosis. In addition, yes-associated protein (YAP) expression, an essential effector of the...
Source: Molecular Medicine - July 22, 2023 Category: Molecular Biology Authors: Yubing Hao Zelin Li Anling Zhang Li Sun Guangxiu Wang Hu Wang Zhifan Jia Source Type: research
The immune activity of selective estrogen receptor modulators is gene and macrophage subtype-specific yet converges on Il1b downregulation
Biomed Pharmacother. 2023 Jul 11;165:115008. doi: 10.1016/j.biopha.2023.115008. Online ahead of print.ABSTRACTRaloxifene belongs to the family of Selective Estrogen Receptor Modulators (SERMs), which are drugs widely prescribed for Estrogen Receptor alpha (ERα)-related pathologies. Recently, SERMs are being tested in repurposing strategies for ERα-independent clinical indications, including a wide range of microbial infections. Macrophages are central in the fight against pathogen invasion. Despite estrogens have been shown to regulate macrophage phenotype, SERMs activity in these cells is still poorly defined. We invest...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - July 13, 2023 Category: Drugs & Pharmacology Authors: Chiara Sfogliarini Giovanna Pepe Candida Maria Cesta Marcello Allegretti Massimo Locati Elisabetta Vegeto Source Type: research
The immune activity of selective estrogen receptor modulators is gene and macrophage subtype-specific yet converges on Il1b downregulation
Biomed Pharmacother. 2023 Jul 11;165:115008. doi: 10.1016/j.biopha.2023.115008. Online ahead of print.ABSTRACTRaloxifene belongs to the family of Selective Estrogen Receptor Modulators (SERMs), which are drugs widely prescribed for Estrogen Receptor alpha (ERα)-related pathologies. Recently, SERMs are being tested in repurposing strategies for ERα-independent clinical indications, including a wide range of microbial infections. Macrophages are central in the fight against pathogen invasion. Despite estrogens have been shown to regulate macrophage phenotype, SERMs activity in these cells is still poorly defined. We invest...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - July 13, 2023 Category: Drugs & Pharmacology Authors: Chiara Sfogliarini Giovanna Pepe Candida Maria Cesta Marcello Allegretti Massimo Locati Elisabetta Vegeto Source Type: research
Novel pharmacotherapy targeting the positive symptoms of schizophrenia
Expert Opin Pharmacother. 2023 Jul 4. doi: 10.1080/14656566.2023.2231346. Online ahead of print.ABSTRACTINTRODUCTION: The severity of positive symptoms in schizophrenia is associated with poor prognosis. About one third of schizophrenia patients partially respond to treatment with available antipsychotics. Purpose of the present manuscript is to provide an updated overview of novel pharmacotherapy targeting positive symptoms in schizophrenia.AREAS COVERED: A comprehensive research on the main database sources (PubMed, PsychINFO, Isi Web of Knowledge, MEDLINE and EMBASE) was performed to obtain original articles published t...
Source: Expert Opinion on Pharmacotherapy - July 4, 2023 Category: Drugs & Pharmacology Authors: Enrico Capuzzi Alice Caldiroli Cecilia Quitadamo Francesco Butturini Teresa Surace Massimo Clerici Massimiliano Buoli Source Type: research
Novel pharmacotherapy targeting the positive symptoms of schizophrenia
Expert Opin Pharmacother. 2023 Jul 10:1-26. doi: 10.1080/14656566.2023.2231346. Online ahead of print.ABSTRACTINTRODUCTION: The severity of positive symptoms in schizophrenia is associated with poor prognosis. About one-third of schizophrenia patients partially respond to treatment with available antipsychotics. The purpose of the present manuscript is to provide an updated overview of novel pharmacotherapy targeting positive symptoms in schizophrenia.AREAS COVERED: A comprehensive research on the main database sources (PubMed, PsychINFO, Isi Web of Knowledge, MEDLINE, and EMBASE) was performed to obtain original articles ...
Source: Expert Opinion on Pharmacotherapy - July 4, 2023 Category: Drugs & Pharmacology Authors: Enrico Capuzzi Alice Caldiroli Cecilia Quitadamo Francesco Butturini Teresa Surace Massimo Clerici Massimiliano Buoli Source Type: research
Cardioprotective effect of tamoxifen and raloxifene: Preventing proteoglycan synthesis by modulating non-canonical TGF- β signalling through NADPH oxidase and ERK phosphorylation
This study sought to investigate the impact of tamoxifen and raloxifene on TGF-β-induced CHSY1 expression and Smad2 linker region phosphorylation in VSMCs and to elucidate the role of reactive oxygen species (ROS), NADPH oxidase (NOX), and kinase pathways in mediating these effects. Employing a comprehensive experimental strategy, VSMCs were treated with TGF-β in the presence or absence of tamoxifen, raloxifene, and various pharmacological inhibitors. Subsequently, CHSY1 mRNA expression, Smad2C and Smad2L phosphorylation, ROS production, p47phox and ERK 1/2 phosphorylation were assessed. Our results revealed that tamoxif...
Source: Biochemical and Biophysical Research communications - June 12, 2023 Category: Biochemistry Authors: Vahid Zarezade Narges Mohammadtaghvaei Mojtaba Rashidi Hossein Babaahmadi-Rezaei Source Type: research
