Exploring Raloxifene-based Metallodrugs: A Versatile Vector Combined with Pt(II), Palladium(II) and Nickel(II) Dichlorides and Carborates against Triple-Negative Breast Cancer
This study provides valuable insights into the development of hybrid therapeutics against TNBC.PMID:38642018 | DOI:10.1002/cmdc.202400006 (Source: ChemMedChem)
Source: ChemMedChem - April 20, 2024 Category: Chemistry Authors: Aleksandr Kazimir Tom G ötze Peter L önnecke Blagoje Murgani ć Sanja Mijatovi ć Danijela Maksimovi ć-Ivanić Evamarie Hey-Hawkins Source Type: research
Enhanced oral bioavailability of levormeloxifene and raloxifene by nanoemulsion: simultaneous bioanalysis using liquid chromatography-tandem mass spectrometry
Nanomedicine, Ahead of Print. (Source: Future Medicine: Nanomedicine)
Source: Future Medicine: Nanomedicine - April 19, 2024 Category: Nanotechnology Authors: Divya Chauhan Debalina Maity Pavan K Yadav Sachin Vishwakarma Arun Agarwal Manish K Chourasia Jiaur R Gayen Source Type: research
Enhanced oral bioavailability of levormeloxifene and raloxifene by nanoemulsion: simultaneous bioanalysis using liquid chromatography-tandem mass spectrometry
Nanomedicine, Ahead of Print. (Source: Nanomedicine)
Source: Nanomedicine - April 19, 2024 Category: Nanotechnology Authors: Divya Chauhan Debalina Maity Pavan K Yadav Sachin Vishwakarma Arun Agarwal Manish K Chourasia Jiaur R Gayen Source Type: research
Clinical characteristics, densitometric parameters and outcomes of patients with atypical femoral fractures related to bisphosphonate treatment for osteoporosis
ConclusionAFF was characterised by usually long duration of bisphosphonate use, higher BMD and more acute neck-shaft angle. AFF did not confer significant impairment in mobility or mortality. Nonetheless, further research work is necessary to optimise bone health among patients who develop AFF. (Source: Endocrine)
Source: Endocrine - April 1, 2024 Category: Endocrinology Source Type: research
Raloxifene-driven benzothiophene derivatives: Discovery, structural refinement, and biological evaluation as potent PPAR γ modulators based on drug repurposing
Eur J Med Chem. 2024 Mar 15;269:116325. doi: 10.1016/j.ejmech.2024.116325. Online ahead of print.ABSTRACTBy virtue of the drug repurposing strategy, the anti-osteoporosis drug raloxifene was identified as a novel PPARγ ligand through structure-based virtual high throughput screening (SB-VHTS) of FDA-approved drugs and TR-FRET competitive binding assay. Subsequent structural refinement of raloxifene led to the synthesis of a benzothiophene derivative, YGL-12. This compound exhibited potent PPARγ modulation with partial agonism, uniquely promoting adiponectin expression and inhibiting PPARγ Ser273 phosphorylation by CDK5 ...
Source: European Journal of Medicinal Chemistry - March 25, 2024 Category: Chemistry Authors: Qingmei Liu Lei Ma Fangyuan Chen Shuyun Zhang Zexin Huang Xiufen Zheng Zikai Chen Junwei Ye Ning Hou Wei Yi Zhi Zhou Source Type: research
In-silico design of novel potential HDAC inhibitors from indazole derivatives targeting breast cancer through QSAR, molecular docking and pharmacokinetics studies
Comput Biol Chem. 2024 Feb 25;110:108035. doi: 10.1016/j.compbiolchem.2024.108035. Online ahead of print.ABSTRACTLatest studies confirmed that abnormal function of histone deacetylase (HDAC) plays a pivotal role in formation of tumors and is a potential therapeutic target for treating breast cancer. In this research, in-silico drug discovery approaches via quantitative structure activity relationship (QSAR) and molecular docking simulations were adapted to 43 compounds of indazole derivatives with HDAC inhibition for anticancer activity against breast cancer. The QSAR models were built from multiple linear regression (MLR)...
Source: Computational Biology and Chemistry - March 9, 2024 Category: Bioinformatics Authors: Sanjeevi Pandiyan Li Wang Source Type: research
In-silico design of novel potential HDAC inhibitors from indazole derivatives targeting breast cancer through QSAR, molecular docking and pharmacokinetics studies
Comput Biol Chem. 2024 Feb 25;110:108035. doi: 10.1016/j.compbiolchem.2024.108035. Online ahead of print.ABSTRACTLatest studies confirmed that abnormal function of histone deacetylase (HDAC) plays a pivotal role in formation of tumors and is a potential therapeutic target for treating breast cancer. In this research, in-silico drug discovery approaches via quantitative structure activity relationship (QSAR) and molecular docking simulations were adapted to 43 compounds of indazole derivatives with HDAC inhibition for anticancer activity against breast cancer. The QSAR models were built from multiple linear regression (MLR)...
Source: Computational Biology and Chemistry - March 9, 2024 Category: Bioinformatics Authors: Sanjeevi Pandiyan Li Wang Source Type: research
GSE207739 Evaluating the toxicity of two endocrine disrupting chemicals, Raloxifene and Resorcinol using a larval zebrafish transcriptomic approach
Contributors : Michael G Morash ; Morgan Kirzinger ; Lee D EllisSeries Type : Expression profiling by high throughput sequencingOrganism : Danio rerioWe use a larval zebrafish model to assess the transcriptomic alterations caused by sub-phenotypic concentrations of two endocrine disrupting drugs: Raloxifene and Resorcinol. (Source: GEO: Gene Expression Omnibus)
Source: GEO: Gene Expression Omnibus - March 8, 2024 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Danio rerio Source Type: research
Maternal immune activation and estrogen receptor modulation induce sex-specific dopamine-related behavioural and molecular alterations in adult rat offspring
Brain Behav Immun. 2024 Feb 29:S0889-1591(24)00279-4. doi: 10.1016/j.bbi.2024.02.034. Online ahead of print.ABSTRACTDopamine dysregulation contributes to psychosis and cognitive deficits in schizophrenia that can be modelled in rodents by inducing maternal immune activation (MIA). The selective estrogen receptor (ER) modulator, raloxifene, can improve psychosis and cognition in men and women with schizophrenia. However, few studies have examined how raloxifene may exert its therapeutic effects in mammalian brain in both sexes during young adulthood (age relevant to most prevalent age at diagnosis). Here, we tested the exte...
Source: Brain, Behavior, and Immunity - March 2, 2024 Category: Neurology Authors: Sophie R Debs Illya Conn Brendan Navaneethan Andriane G Penklis Urs Meyer Simon Killcross Cynthia Shannon Weickert Tertia D Purves-Tyson Source Type: research
Maternal immune activation and estrogen receptor modulation induce sex-specific dopamine-related behavioural and molecular alterations in adult rat offspring
Brain Behav Immun. 2024 Feb 29:S0889-1591(24)00279-4. doi: 10.1016/j.bbi.2024.02.034. Online ahead of print.ABSTRACTDopamine dysregulation contributes to psychosis and cognitive deficits in schizophrenia that can be modelled in rodents by inducing maternal immune activation (MIA). The selective estrogen receptor (ER) modulator, raloxifene, can improve psychosis and cognition in men and women with schizophrenia. However, few studies have examined how raloxifene may exert its therapeutic effects in mammalian brain in both sexes during young adulthood (age relevant to most prevalent age at diagnosis). Here, we tested the exte...
Source: Brain, Behavior, and Immunity - March 2, 2024 Category: Neurology Authors: Sophie R Debs Illya Conn Brendan Navaneethan Andriane G Penklis Urs Meyer Simon Killcross Cynthia Shannon Weickert Tertia D Purves-Tyson Source Type: research
Screening of 16 major drug glucuronides for time-dependent inhibition of nine drug-metabolizing CYP enzymes - detailed studies on CYP3A inhibitors
In conclusion, we identified several glucuronide metabolites with CYP inhibitory properties. Based on detailed experiments, the inactivation of CYP3A by carvedilol may cause clinically significant drug-drug interactions.PMID:38423227 | DOI:10.1016/j.ejps.2024.106735 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - February 29, 2024 Category: Drugs & Pharmacology Authors: Helin ä Kahma Marie-No ëlle Paludetto Mikko Neuvonen Mika Kurkela Anne M Filppula Mikko Niemi Janne T Backman Source Type: research
Screening of 16 major drug glucuronides for time-dependent inhibition of nine drug-metabolizing CYP enzymes - detailed studies on CYP3A inhibitors
In conclusion, we identified several glucuronide metabolites with CYP inhibitory properties. Based on detailed experiments, the inactivation of CYP3A by carvedilol may cause clinically significant drug-drug interactions.PMID:38423227 | DOI:10.1016/j.ejps.2024.106735 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - February 29, 2024 Category: Drugs & Pharmacology Authors: Helin ä Kahma Marie-No ëlle Paludetto Mikko Neuvonen Mika Kurkela Anne M Filppula Mikko Niemi Janne T Backman Source Type: research
Screening of 16 major drug glucuronides for time-dependent inhibition of nine drug-metabolizing CYP enzymes - detailed studies on CYP3A inhibitors
In conclusion, we identified several glucuronide metabolites with CYP inhibitory properties. Based on detailed experiments, the inactivation of CYP3A by carvedilol may cause clinically significant drug-drug interactions.PMID:38423227 | DOI:10.1016/j.ejps.2024.106735 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - February 29, 2024 Category: Drugs & Pharmacology Authors: Helin ä Kahma Marie-No ëlle Paludetto Mikko Neuvonen Mika Kurkela Anne M Filppula Mikko Niemi Janne T Backman Source Type: research
Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents
Bioorg Med Chem. 2024 Feb 16;101:117645. doi: 10.1016/j.bmc.2024.117645. Online ahead of print.ABSTRACTAll three possible sulfamate derivatives of the selective estrogen receptor modulator Raloxifene (bis-sulfamate 7 and two mono-sulfamates 8-9) were synthesized and evaluated as inhibitors of the clinical drug target steroid sulfatase (STS), both in cell-free and in cell-based assays, and also as estrogen receptor (ER) modulators. Bis-sulfamate 7 was the most potent STS inhibitor with an IC50 of 12.2 nM in a whole JEG3 cell-based assay, with the two mono-sulfamates significantly weaker. The estrogen receptor-modulating act...
Source: Bioorganic and Medicinal Chemistry - February 24, 2024 Category: Chemistry Authors: Seyed-Omar Zaraei Wolfgang Dohle Hanan S Anbar Randa El-Gamal Bertrand Leblond Paul A Foster Taleb H Al-Tel Barry V L Potter Mohammed I El-Gamal Source Type: research
Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents
Bioorg Med Chem. 2024 Feb 16;101:117645. doi: 10.1016/j.bmc.2024.117645. Online ahead of print.ABSTRACTAll three possible sulfamate derivatives of the selective estrogen receptor modulator Raloxifene (bis-sulfamate 7 and two mono-sulfamates 8-9) were synthesized and evaluated as inhibitors of the clinical drug target steroid sulfatase (STS), both in cell-free and in cell-based assays, and also as estrogen receptor (ER) modulators. Bis-sulfamate 7 was the most potent STS inhibitor with an IC50 of 12.2 nM in a whole JEG3 cell-based assay, with the two mono-sulfamates significantly weaker. The estrogen receptor-modulating act...
Source: Bioorganic and Medicinal Chemistry - February 24, 2024 Category: Chemistry Authors: Seyed-Omar Zaraei Wolfgang Dohle Hanan S Anbar Randa El-Gamal Bertrand Leblond Paul A Foster Taleb H Al-Tel Barry V L Potter Mohammed I El-Gamal Source Type: research
