Article
Pharmacology & Pharmacy
Adam Olaitan Abdulkareem, Priya Tiwari, Zahid Rasool Lone, Hina Iqbal, Satish Gupta, Rajesh Kumar Jha, Debabrata Chanda, Kumaravelu Jagavelu, Kashif Hanif
Summary: This study investigated the ameliorative effects of ormeloxifene, a selective estrogen receptor modulator, in pulmonary hypertension. The results showed that ormeloxifene promoted the synthesis of 17β-estradiol, alleviated inflammation, and improved the NOX4/HO1/Nrf/PPAR gamma/PGC-1 alpha axis, thereby attenuating pulmonary hypertension.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Chemistry, Medicinal
Ravindran Vini, Vishnu Sunil Jaikumar, Viji Remadevi, Swathy Ravindran, Juberiya M. Azeez, Anjana Sasikumar, Shankar Sundaram, Sreeharshan Sreeja
Summary: 27-hydroxycholesterol (27-HC) is an endogenous selective estrogen receptor modulator (SERM) that has adverse effects on breast cancer. Pomegranate extract, which contains ellagitannins and ellagic acid, can compete with 27-HC. Urolithins, especially urolithin A (UA) and urolithin B (UB), derived from pomegranate, have antiproliferative and estrogenic activities, and UA can act as an antagonist to 27-HC in breast cancer cells, making it a potential SERM.
PHYTOTHERAPY RESEARCH
(2023)
Article
Microbiology
Renu Sudhakar, Navin Adhikari, Saniya Pamnani, Abhipsa Panda, Manish Bhattacharjee, Zeba Rizvi, Sadaf Shehzad, Dinesh Gupta, Puran Singh Sijwali
Summary: Despite the challenges posed by drug-resistant parasite strains, repurposing existing drugs for malaria treatment is an attractive option. Bazedoxifene, a selective estrogen receptor modulator, has shown potent inhibitory activity against Plasmodium falciparum and Plasmodium berghei. It inhibits the formation of hemozoin, a byproduct of hemoglobin degradation by the malaria parasite, and could potentially be repurposed as an antimalarial drug.
MICROBIOLOGY SPECTRUM
(2022)
Article
Pharmacology & Pharmacy
Liping Zhou, Ka-Ying Wong, Wenxuan Yu, Christina Chui-Wa Poon, Huihui Xiao, Chi-On Chan, Daniel Kam-Wah Mok, Yan Zhang, Man-Sau Wong
Summary: Herba epimedii (HEP) shows bone protective activity when used alone or in combination with Selective Estrogen Receptor Modulators (SERMs) in rat models with estrogen deficiency, restoring changes in bone mineral density and turnover biomarkers. HEP interacts with SERMs to promote bone health without altering the individual effects of both substances in preventing bone loss caused by hormonal deficiency.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Biochemical Research Methods
Masato Okano, Mitsuhiko Sato, Shinji Kageyama
Summary: Bazedoxifene, a selective estrogen receptor modulator, is included in the prohibited list by WADA. A method was developed to detect and quantify bazedoxifene and its metabolites in human urine.
DRUG TESTING AND ANALYSIS
(2022)
Article
Endocrinology & Metabolism
Christine A. Cabelka, Cory W. Baumann, Angus Lindsay, Andrew Norton, Nick C. Blixt, Gengyun Le, Gordon L. Warren, Kim C. Mansky, Susan A. Novotny, Dawn A. Lowe
Summary: The tissue-selective effects of Bazedoxifene (BZA) on musculoskeletal system in Ovariectomized (OVX) female mice indicate that BZA may act as an estrogen receptor agonist in skeletal muscle, as it has been seen in bone, providing minor benefits to the musculoskeletal system.
JOURNAL OF ENDOCRINOLOGY
(2021)
Article
Endocrinology & Metabolism
Edmund Charles Jenkins, Gabriella Casalena, Maria Gomez, Dazhi Zhao, Timothy C. Kenny, Nagma Shah, Giovanni Manfredi, Doris Germain
Summary: Dysfunctions in proteasome and protein aggregation are key features of several neurodegenerative disorders. The study found distinct effects of different selective estrogen receptor modulators (SERMs) on gene expression in the spinal cord, with raloxifene showing significant regulation of deubiquitinating enzymes, proteasome subunits and assembly factors. In a mouse model of amyotrophic lateral sclerosis, even a low dose of raloxifene reduced mutant SOD1 aggregates in females and delayed muscle strength decline. These results highlight the importance of considering sex-specific and SERM-selective effects in clinical trials for neurodegenerative diseases.
Review
Chemistry, Medicinal
Neha Bhatia, Shreejita Hazra, Suresh Thareja
Summary: The discovery of SERDs has revolutionized anticancer research, particularly in the treatment of ER+ breast cancer. These drugs are considered essential due to the high prevalence of ER+ breast cancer cases and the development of endocrine resistance. This review provides an overview of the pathophysiology of SERDs, their interaction with FDA-approved drugs, and the current research and design strategy for these therapeutics.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Yiyoung Kim, Eun Ji Roh, Hari Prasad Joshi, Hae Eun Shin, Hyemin Choi, Su Yeon Kwon, Seil Sohn, Inbo Han
Summary: BZA has shown neuroprotection and remyelination effects in central nervous system injuries. Research demonstrated that BZA could suppress inflammatory response, promote oligodendrocyte precursor cell differentiation, and reduce blood-spinal cord barrier disruption. BZA also improved locomotor recovery in rats with spinal cord injury.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Multidisciplinary Sciences
Jian Min, Jerome C. Nwachukwu, Charles K. Min, Jacqline W. Njeri, Sathish Srinivasan, Erumbi S. Rangarajan, Charles C. Nettles, Valeria Sanabria Guillen, Yvonne Ziegler, Shunchao Yan, Kathryn E. Carlson, Yingwei Hou, Sung Hoon Kim, Scott Novick, Bruce D. Pascal, Rene Houtman, Patrick R. Griffin, Tina Izard, Benita S. Katzenellenbogen, John A. Katzenellenbogen, Kendall W. Nettles
Summary: Efforts to improve estrogen receptor-alpha (ER)-targeted therapies in breast cancer have led to the development of dual-mechanism ER inhibitors (DMERIs) that generate full antagonism using alternate structural mechanisms, effectively suppressing ER activity and proliferation in breast cancer cells and resistance models. These findings highlight the enhanced flexibility of the ER LBD in response to DMERI binding, distinguishing them from current single-mechanism antiestrogens.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Biotechnology & Applied Microbiology
Sisi Qin, James N. Ingle, Wootae Kim, Huanyao Gao, Richard M. Weinshilboum, Liewei Wang
Summary: The study identified potential pathways, including ribosome and AMP-activated protein kinase (AMPK) signaling, regulated by ZNF423 or ZNF423 rs9940645 SNP. The findings suggest that AMPK signaling is modulated by the ZNF423 rs9940645 SNP and may affect metformin response in breast cancer, potentially serving as a biomarker for personalized metformin treatment.
PHARMACOGENETICS AND GENOMICS
(2021)
Article
Obstetrics & Gynecology
Joann V. Pinkerton
Summary: Selective estrogen receptor (ER) modulators have variable tissue-specific estrogen agonist and antagonist activities. Ospemifene is approved to treat dyspareunia, while lasofoxifene is in development for resistant ER positive breast cancer.
CLINICAL OBSTETRICS AND GYNECOLOGY
(2021)
Article
Medicine, General & Internal
Iwona Szydlowska, Marta Grabowska, Jolanta Nawrocka-Rutkowska, Malgorzata Piasecka, Andrzej Starczewski
Summary: The results of the study suggest that a good response to UPA treatment in fibroids may be associated with a decrease in fibrosis, ER/PR and PCNA and Ki67 immunoexpression, as well as an increase in cell apoptosis.
JOURNAL OF CLINICAL MEDICINE
(2021)
Article
Virology
Scott F. Grady, Amelia K. Pinto, Mariah Hassert, June A. D'Angelo, James D. Brien, Christopher K. Arnatt
Summary: Zika virus has been identified as an increasing risk, prompting urgent development of treatment options. Research has found that tamoxifen may be repurposed as a promising antiviral drug against ZIKV.
JOURNAL OF MEDICAL VIROLOGY
(2021)
Article
Biotechnology & Applied Microbiology
Hanbit Song, Pyung-Gang Lee, Junyeob Kim, Joonwon Kim, Sang-Hyuk Lee, Hyun Kim, Uk-Jae Lee, Jin Young Kim, Eun-Jung Kim, Byung-Gee Kim
Summary: Multiple regiospecific enantiomers of hydroxy-(S)-equol were synthesized from daidzein and genistein through consecutive reduction and oxidation reactions. A one-pot synthesis pathway for 6-hydroxyequol was developed, and the estrogenic and antioxidative activities of each regio-isomer were evaluated.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2022)
Review
Medicine, Research & Experimental
David L. Kendler, Felicia Cosman, Robert Kees Stad, Serge Ferrari
Summary: Denosumab, a fully human monoclonal antibody, has shown to be highly effective in treating osteoporosis and reducing fracture risk in high-risk patients. Long-term studies have demonstrated gradual increases in bone mineral density and sustained low rates of fractures with minimal side effects.
ADVANCES IN THERAPY
(2022)
Article
Endocrinology & Metabolism
Danielle E. Whittier, Elizabeth J. Samelson, Marian T. Hannan, Lauren A. Burt, David A. Hanley, Emmanuel Biver, Pawel Szulc, Elisabeth Sornay-Rendu, Blandine Merle, Roland Chapurlat, Eric Lespessailles, Andy Kin On Wong, David Goltzman, Sundeep Khosla, Serge Ferrari, Mary L. Bouxsein, Douglas P. Kiel, Steven K. Boyd
Summary: The prevalence of osteoporosis in older adults is high, but current clinical methods fail to detect most fragility fracture cases. High-resolution peripheral quantitative computed tomography (HR-pQCT) provides additional information about bone density and structure, but interpretation is challenging. In this study, the authors identified common bone phenotypes associated with fracture risk using HR-pQCT data from a multinational cohort. They found that different phenotypes had significantly different fracture risks and identified imaging biomarkers for fractures within each phenotype.
JOURNAL OF BONE AND MINERAL RESEARCH
(2022)
Editorial Material
Endocrinology & Metabolism
Serge Ferrari
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
(2022)
Article
Endocrinology & Metabolism
Felicia Cosman, David L. Kendler, Bente L. Langdahl, Benjamin Z. Leder, E. Michael Lewiecki, Akimitsu Miyauchi, Maria Rojeski, Michele McDermott, Mary K. Oates, Cassandra E. Milmont, Cesar Libanati, Serge Ferrari
Summary: This analysis evaluated the impact of treatment sequence on the response to romosozumab. The findings suggest that initiating treatment with romosozumab followed by an antiresorptive agent leads to greater increases in bone mineral density and higher response rates.
OSTEOPOROSIS INTERNATIONAL
(2022)
Article
Endocrinology & Metabolism
E. H. S. Koy, A. Amouzougan, E. Biver, R. Chapurlat, T. Chevalley, S. L. Ferrari, A. Fouilloux, H. Locrelle, H. Marotte, M. Normand, R. Rizzoli, L. Vico, T. Thomas
Summary: This study presents reference values of HR-pQCT measurements in a Franco-Swiss female cohort at the distal radius and tibia sites, considering specific age bounds. Microarchitectural parameters start to decline before the age of 30, with the optimal bone profile observed between the ages of 22 to 27 in this population.
OSTEOPOROSIS INTERNATIONAL
(2022)
Review
Endocrinology & Metabolism
Maria Fusaro, Francesco Tondolo, Lorenzo Gasperoni, Giovanni Tripepi, Mario Plebani, Martina Zaninotto, Thomas L. Nickolas, Markus Ketteler, Andrea Aghi, Cristina Politi, Gaetano La Manna, Maria Luisa Brandi, Serge Ferrari, Maurizio Gallieni, Maria Cristina Mereu, Giuseppe Cianciolo
Summary: This review discusses the mechanism of action of vitamin K and its implications in cardiovascular disease, bone fractures, and inflammation. It highlights the protective role of vitamin K, especially in chronic kidney disease (CKD), and emphasizes the importance of vitamin K dosage in reducing bone fractures and improving vascular calcifications.
CURRENT OSTEOPOROSIS REPORTS
(2022)
Article
Surgery
Nikola Saulacic, Gordana Vunjak-Novakovic, Maiko Haga-Tsujimura, Ken Nakahara, Maude Coline Gerbaix, Serge Livio Ferrari
Summary: The study aimed to evaluate the benefit of periosteal distraction osteogenesis (PDO) on de novo bone formation in rats. The results showed that bone volumes significantly increased in both the periosteal pumping (PP) group and the PDO group, with different degrees of maturity at different time points.
ANNALS OF PLASTIC SURGERY
(2022)
Article
Nutrition & Dietetics
Maria Papageorgiou, Fanny Merminod, Serge Ferrari, Rene Rizzoli, Emmanuel Biver
Summary: This study examined the relationship between calcium intake from various sources and blood lipids in community-dwelling elderly individuals. The results showed that increasing total calcium intake was associated with lower risks of high total cholesterol, triglycerides, and low HDL-cholesterol. Specifically, calcium from dairy products, especially milk and milk-based desserts, was linked to a lower risk of high total cholesterol. Higher calcium intakes from total dairies, milk, and non-fermented dairies were associated with a lower risk of hypertriglyceridemia. No association was found between calcium from non-dairy sources, cheese, or high-fat dairies and blood lipids. Increasing calcium intake through supplements was associated with lower risks of hypertriglyceridemia and low HDL-cholesterol. However, this association was no longer significant after adjusting for other factors.
Review
Nutrition & Dietetics
Maria Fusaro, Giulia Vanessa Re Sarto, Maurizio Gallieni, Laura Cosmai, Piergiorgio Messa, Maurizio Rossini, Iacopo Chiodini, Mario Plebani, Pieter Evenepoel, Nicholas Harvey, Serge Ferrari, Jorge Cannata-Andia, Andrea Trombetti, Maria Luisa Brandi, Markus Ketteler, Thomas L. Nickolas, John Cunningham, Syazrah Salam, Carlo Della Rocca, Aldo Scarpa, Salvatore Minisola, Fabio Malberti, Filomena Cetani, Mario Cozzolino, Sandro Mazzaferro, Luigi Morrone, Giovanni Tripepi, Martina Zaninotto, Maria Cristina Mereu, Maura Ravera, Giuseppe Cianciolo, Gaetano La Manna, Andrea Aghi, Sandro Giannini, Luca Dalle Carbonare
Summary: Bone biopsy with histomorphometric analysis is the gold standard for diagnosing and classifying renal osteodystrophy. However, its use has declined due to various reasons. This position paper from Italian scientific societies aims to promote the use of bone biopsy and improve the management and prognosis of CKD patients through optimization and standardization of the procedure, establishment of a network, and reimbursement adjustments.
Review
Endocrinology & Metabolism
Lorenz C. Hofbauer, Bjoern Busse, Richard Eastell, Serge Ferrari, Morten Frost, Ralph Mueller, Andrea M. Burden, Fernando Rivadeneira, Nicola Napoli, Martina Rauner
Summary: Increased fracture risk is a serious complication of diabetes, leading to prolonged immobility and hospitalizations that can result in significant morbidity and mortality. In type 1 diabetes, bone mass and strength are reduced, leading to a five-fold increased risk of lifelong fractures. In type 2 diabetes, fracture risk is increased despite normal bone mass. The fragility of bones in diabetes can be attributed to cellular abnormalities, matrix interactions, immune and vascular changes, and musculoskeletal maladaptation to chronic hyperglycemia.
LANCET DIABETES & ENDOCRINOLOGY
(2022)
Article
Endocrinology & Metabolism
Maria Papageorgiou, Emmanuel Biver, Julie Mareschal, Nicholas Edward Phillips, Alexandra Hemmer, Emma Biolley, Nathalie Schwab, Emily N. C. Manoogian, Elena Gonzalez Rodriguez, Daniel Aeberli, Didier Hans, Caroline Pot, Satchidananda Panda, Nicolas Rodondi, Serge L. Ferrari, Tinh-Hai Collet
Summary: This study investigated the impact of time-restricted eating (TRE) versus standard dietary advice (SDA) on bone health. The results showed that TRE had no detrimental effects on bone health in the overall population, but in weight loss responders, it was associated with some bone-sparing effects compared with SDA.
Article
Endocrinology & Metabolism
Francesca Marini, Francesca Giusti, Elena Marasco, Luciano Xumerle, Katarzyna Malgorzata Kwiatkowska, Paolo Garagnani, Emmanuel Biver, Serge Ferrari, Giovanni Iolascon, Teresa Iantomasi, Maria Luisa Brandi
Summary: Atypical femur fractures (AFFs) are rare fractures that occur at the lateral cortex of the femur and are associated with rare genetic bone disorders and long-term use of antiresorption drugs. Genetic screening of unrelated patients with AFFs revealed a high frequency of rare variants in the SLC34A1 and SLC9A3R1 genes, suggesting a possible genetic risk factor for AFFs.
EUROPEAN JOURNAL OF ENDOCRINOLOGY
(2023)
Article
Rheumatology
Serge Ferrari, Bente Langdahl
Summary: Denosumab, a human monoclonal antibody against RANKL, inhibits osteoclast differentiation and activity, leading to anti-resorptive properties and anti-fracture efficacy. Compared with bisphosphonates, denosumab results in continuous bone mineral density gain during long-term treatment and rapid bone loss upon withdrawal. The underlying mechanisms for these effects are not fully understood, but emerging data suggest that denosumab may affect both osteoclasts and osteoblasts, causing sustained bone gain and bone loss. Future studies and clinical implications are discussed in this Perspective.
NATURE REVIEWS RHEUMATOLOGY
(2023)
Article
Endocrinology & Metabolism
J. A. Kanis, H. Johansson, E. McCloskey, E. Liu, K. E. Akesson, F. A. Anderson, R. Azagra, C. L. Bager, C. Beaudart, H. A. Bischoff-Ferrari, E. Biver, O. Bruyere, J. A. Cauley, J. R. Center, R. Chapurlat, C. Christiansen, C. Cooper, C. J. Crandall, S. R. Cummings, J. A. P. da Silva, B. Dawson-Hughes, A. Diez-Perez, A. B. Dufour, J. A. Eisman, P. J. M. Elders, S. Ferrari, Y. Fujita, S. Fujiwara, C. -c. Glueer, I. Goldshtein, D. Goltzman, V. Gudnason, J. Hall, D. Hans, M. Hoff, R. J. Hollick, M. Huisman, M. Iki, S. Ish-Shalom, G. Jones, M. K. Karlsson, S. Khosla, D. P. Kiel, W. -p. Koh, F. Koromani, M. A. Kotowicz, H. Kroger, T. Kwok, O. Lamy, A. Langhammer, B. Larijani, K. Lippuner, D. Mellstrom, T. Merlijn, A. Nordstrom, P. Nordstrom, T. W. O'Neill, B. Obermayer-Pietsch, C. Ohlsson, E. S. Orwoll, J. A. Pasco, F. Rivadeneira, A. -M. Schott, E. J. Shiroma, K. Siggeirsdottir, E. M. Simonsick, E. Sornay-Rendu, R. Sund, K. M. A. Swart, P. Szulc, J. Tamaki, D. J. Torgerson, N. M. van Schoor, T. P. van Staa, J. Vila, N. J. Wareham, N. C. Wright, N. Yoshimura, M. C. Zillikens, M. Zwart, L. Vandenput, N. C. Harvey, M. Lorentzon, W. D. Leslie
Summary: A large international meta-analysis finds that a previous history of fracture is associated with an increased risk of future fractures, regardless of age, sex, and bone mineral density. The study highlights the importance of considering previous fracture history as a risk factor for fracture prevention strategies.
OSTEOPOROSIS INTERNATIONAL
(2023)
Article
Endocrinology & Metabolism
Eleni Tsiantouli, Emmanuel Biver, Thierry Chevalley, Robert Petrovic, Didier Hannouche, Serge Ferrari
Summary: Hypophosphatasia (HPP) is a rare genetic disorder characterized by low serum alkaline phosphatase (ALP). This study found that low ALP values are common in patients with atypical femoral fractures (AFF) and are mainly related to antiresorptive medication. Therefore, low serum ALP has low specificity for HPP among AFF patients.
CALCIFIED TISSUE INTERNATIONAL
(2022)