Rapid discovery and classification of inhibitors of coronavirus infection by pseudovirus screen and amplified luminescence proximity homogeneous assay
Antiviral Res. 2022 Nov 23:105473. doi: 10.1016/j.antiviral.2022.105473. Online ahead of print.ABSTRACTTo identify potent antiviral compounds, we introduced a high-throughput screen platform that can rapidly classify hit compounds according to their target. In our platform, we performed a compound screen using a lentivirus-based pseudovirus presenting a spike protein of coronavirus, and we evaluated the hit compounds using an amplified luminescence proximity homogeneous assay (alpha) test with purified host receptor protein and the receptor binding domain of the viral spike. With our screen platform, we were able to identi...
Source: Antiviral Research - November 26, 2022 Category: Virology Authors: Kwiwan Jeong JuOae Chang Sun-Mi Park Jinhee Kim Sangeun Jeon Dong Hwan Kim Young-Eui Kim Joo Chan Lee Somyoung Im Yejin Jo Ji-Young Min Hanbyeul Lee Minjoo Yeom Sang-Hyuk Seok Da In On Hyuna Noh Jun-Won Yun Jun Won Park Daesub Song Je Kyung Seong Kyung-Ch Source Type: research
Combined Thermoneutral Housing and Raloxifene Treatment Improves Trabecular Bone Microarchitecture and Strength in Growing Female Mice
This study will examine the same question within the axial skeleton, which has a higher proportion of trabecular bone. After 6 weeks of treatment with RAL, vertebrae from female C57BL/6 J mice underwent microcomputed tomography (μCT), architectural analysis, and compression testing. Most of the tested geometric properties (bone volume/tissue volume percent, trabecular thickness, trabecular number, trabecular spacing) improved with both the housing and RAL treatment. The effect sizes suggested an additive effect when treating mice housed under thermoneutral conditions. While ultimate force was enhanced with the treatment...
Source: Calcified Tissue International - November 13, 2022 Category: Orthopaedics Source Type: research
A combined treatment with selective androgen and estrogen receptor modulators prevents bone loss in orchiectomized rats
ConclusionThe EN + RAL treatment appeared to be promising in preventing male osteoporosis, but given the observed side effects on liver, kidney, and prostate weights, it requires further investigation. (Source: Journal of Endocrinological Investigation)
Source: Journal of Endocrinological Investigation - November 11, 2022 Category: Endocrinology Source Type: research
Comparisons between different anti-osteoporosis medications on postfracture mortality: A population-based study
CONCLUSION: This real-world mega data study suggests that the usage of osteoporotic medication, especially the long-acting regimen, may lower postfracture mortality.PMID:36317591 | DOI:10.1210/clinem/dgac636 (Source: The Journal of Clinical Endocrinology and Metabolism)
Source: The Journal of Clinical Endocrinology and Metabolism - November 1, 2022 Category: Endocrinology Authors: Chih-Hsing Wu Chia-Chun Li Yu-Hsuan Hsu Fu-Wen Liang Yin-Fan Chang Jawl-Shan Hwang Source Type: research
Comparisons between different anti-osteoporosis medications on postfracture mortality: A population-based study
CONCLUSION: This real-world mega data study suggests that the usage of osteoporotic medication, especially the long-acting regimen, may lower postfracture mortality.PMID:36317591 | DOI:10.1210/clinem/dgac636 (Source: The Journal of Clinical Endocrinology and Metabolism)
Source: The Journal of Clinical Endocrinology and Metabolism - November 1, 2022 Category: Endocrinology Authors: Chih-Hsing Wu Chia-Chun Li Yu-Hsuan Hsu Fu-Wen Liang Yin-Fan Chang Jawl-Shan Hwang Source Type: research
The Selective Estrogen Receptor Modulator, Raloxifene, Is Protective Against Renal Ischemia–reperfusion Injury
Conclusions.
Raloxifene is protective against both acute kidney injury and fibrosis resulting from renal IRI in a mouse model. (Source: Transplantation)
Source: Transplantation - October 28, 2022 Category: Transplant Surgery Tags: Original Basic Science Source Type: research
Molecular Docking Study of Isoxazole Indole Derivatives (B2A2 Series)
as Promising Selective Estrogen Receptor Modulators & Anticancer
Drugs
Drug Res (Stuttg) DOI: 10.1055/a-1958-3823A series of 7 compounds with isoxazole – indole –
γ-resorcylic acid scaffold, segregated into B2 & A2 series,
wherein, B2 comprises Compounds: 13, 14, 15 & 16 and A2 comprises
Compounds: 10, 11 & 12, on the basis of the variable substituents at the
indole, resorcinol and isoxazole end of the scaffold as in Figure: 1, were
designed and docked with human estrogen receptor: 1ERRα. The Binding
affinity (BA) and the interacting amino acids compared with reference selective
estrogen receptor modulator...
Source: Drug Research - October 27, 2022 Category: Drugs & Pharmacology Authors: Iyer, Jayashree Monikanta Khare, Aradhana Pandey, Jaya Yadav, Manish Tags: Original Article Source Type: research
Simultaneous determination of raloxifene and tamoxifen using dispersive micro solid-phase extraction and HPLC method in real water, human hair and serum samples
. (Source: International Journal of Environmental Analytical Chemistry)
Source: International Journal of Environmental Analytical Chemistry - September 2, 2022 Category: Chemistry Authors: Faezeh Rezaei Mahboubeh Masrournia Mehdi Pordel Source Type: research
Association of raloxifene and tamoxifen therapy with cognitive performance, odds of mild cognitive impairment, and brain MRI markers of neurodegeneration
Comparison of outcomes by tamoxifen exposure among 151 women with breast cancer history. AbstractThe aim of this cross-sectional study was to examine whether a history of selective estrogen receptor modifiers (SERMs), tamoxifen and raloxifene, use was associated with cognitive performance, odds of mild cognitive impairment (MCI), or magnetic resonance imaging (MRI) markers of neurodegeneration associated with Alzheimer's disease. We included women with prior history of breast cancer or no prior history of any cancer at enrollment in the Mayo Clinic Study of Aging (MCSA). This information was abstracted using the Rochester ...
Source: Cancer Medicine - August 30, 2022 Category: Cancer & Oncology Authors: Firat Kara,
Christine M. Lohse,
Anna M. Castillo,
Nirubol Tosakulwong,
Timothy G. Lesnick,
Clifford R. Jack,
Ronald C. Petersen,
Janet E. Olson,
Fergus J. Couch,
Kathryn J. Ruddy,
Kejal Kantarci,
Michelle M. Mielke Tags: RESEARCH ARTICLE Source Type: research
Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability
Drug Deliv. 2022 Dec;29(1):2685-2693. doi: 10.1080/10717544.2022.2111479.ABSTRACTOsteoporosis is a disease that reduces bone mass and microarchitecture, which makes bones fragile. Postmenopausal osteoporosis occurs due to estrogen deficiency. Raloxifene is a selective estrogen receptor modulator used to treat postmenopausal osteoporosis. However, it has a low bioavailability, which requires long-term, high-dose raloxifene administration to be effective and causes several side effects. Herein, raloxifene was encapsulated in human serum albumin (HSA)-based nanoparticles (Ral/HSA/PSS NPs) as an intravenous-injection pharmaceu...
Source: Drug Delivery - August 17, 2022 Category: Drugs & Pharmacology Authors: Shu-Jyuan Yang Chih-Hao Chang Tai-Horng Young Chung-Hao Wang Tzu-Hao Tseng Man-Ling Wang Source Type: research
Exploring the Role of Sodium-Glucose Cotransporter as a New Target for Cancer Therapy
CONCLUSION: SGLT2 inhibitors have antiproliferation, anti-tumorigenesis, and anti-migration effects and may induce apoptosis in cancer cells. In addition, treatment with SGLT2 inhibitors resulted in the downregulation of selected genes in the Du-145 cell line.PMID:35977549 | DOI:10.18433/jpps32879 (Source: J Pharm Pharm Sci)
Source: J Pharm Pharm Sci - August 17, 2022 Category: Drugs & Pharmacology Authors: Sanaa Bardaweel Ahmad Issa Source Type: research
Exploring the Role of Sodium-Glucose Cotransporter as a New Target for Cancer Therapy
CONCLUSION: SGLT2 inhibitors have antiproliferation, anti-tumorigenesis, and anti-migration effects and may induce apoptosis in cancer cells. In addition, treatment with SGLT2 inhibitors resulted in the downregulation of selected genes in the Du-145 cell line.PMID:35977549 | DOI:10.18433/jpps32879 (Source: Journal of Pharmacy and Pharmaceutical Sciences)
Source: Journal of Pharmacy and Pharmaceutical Sciences - August 17, 2022 Category: Drugs & Pharmacology Authors: Sanaa Bardaweel Ahmad Issa Source Type: research
Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability
Drug Deliv. 2022 Dec;29(1):2685-2693. doi: 10.1080/10717544.2022.2111479.ABSTRACTOsteoporosis is a disease that reduces bone mass and microarchitecture, which makes bones fragile. Postmenopausal osteoporosis occurs due to estrogen deficiency. Raloxifene is a selective estrogen receptor modulator used to treat postmenopausal osteoporosis. However, it has a low bioavailability, which requires long-term, high-dose raloxifene administration to be effective and causes several side effects. Herein, raloxifene was encapsulated in human serum albumin (HSA)-based nanoparticles (Ral/HSA/PSS NPs) as an intravenous-injection pharmaceu...
Source: Drug Delivery - August 17, 2022 Category: Drugs & Pharmacology Authors: Shu-Jyuan Yang Chih-Hao Chang Tai-Horng Young Chung-Hao Wang Tzu-Hao Tseng Man-Ling Wang Source Type: research
