Article
Oncology
Sofia Xanthoulea, Gonda F. J. Konings, Niina Saarinen, Bert Delvoux, Loes F. S. Kooreman, Pasi Koskimies, Merja R. Hakkinen, Seppo Auriola, Elisabetta D'Avanzo, Youssef Walid, Frank Verhaegen, Natasja G. Lieuwes, Florian Caiment, Roy Kruitwagen, Andrea Romano
Summary: The study demonstrates that pharmacological inhibition of 17β-HSD-1 can inhibit the development of endometrial cancer. Through experiments on mice, it was found that treatment with the inhibitor significantly reduces tumor growth and metastatic spread.
Article
Chemistry, Medicinal
Mohamed Salah, Mariam Tahoun, Jeannette Rudzitis-Auth, Lisa Stotz, Chris J. J. van Koppen, Matthias W. W. Laschke, Ahmed S. S. Abdelsamie, Martin Frotscher
Summary: Treating estrogen-dependent diseases with novel dual STS/17β-HSD1 inhibitors (DSHIs) may provide a superior alternative to existing endocrine therapies. Compound 5 showed irreversible inhibition of STS and potent, reversible inhibition of 17 β-HSD1 in T47D cells. It exhibited high selectivity and metabolic stability, with no effect on cell viability or activation of the aryl hydrocarbon receptor (AhR).
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Engineering, Environmental
Weiliang Xiong, Wanli Peng, Yali Fu, Zixin Deng, Shuangjun Lin, Rubing Liang
Summary: Microbacterium hominis SJTG1 is an efficient and adaptive strain that can degrade 17β-estradiol under harsh conditions, providing potential for the remediation of hormone pollution in the environment.
JOURNAL OF HAZARDOUS MATERIALS
(2023)
Article
Biochemistry & Molecular Biology
Swanand Kulkarni, Yogesh Singh, Avadh Biharee, Neha Bhatia, Vikram Deep Monga, Suresh Thareja
Summary: Excess of androgens can cause various diseases. This study identifies the pharmacophoric features of indole-based compounds as potent 17 beta-HSD5 inhibitors through molecular docking, 3D-QSAR, pharmacophore mapping and MD-simulation. The most potent compound showed stable binding and good affinity with the active site pocket of the enzyme. The developed pharmacophore can be helpful in designing novel indole-based molecules for the treatment of androgenic disorders.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Nicole Petersen, Andrea J. Rapkin, Kyoji Okita, Kaitlin R. Kinney, Tomi Mizuno, Mark A. Mandelkern, Edythe D. London
Summary: Research on 16 women aged 23-45 found no significant difference in dopamine D-2-type receptor availability in the striatum subregions during high-estrogen vs. low-estrogen phases of the menstrual cycle, suggesting that circulating estrogen levels do not affect dopamine D-2-type receptor availability in the human striatum.
MOLECULAR PSYCHIATRY
(2021)
Article
Nutrition & Dietetics
Yuki Nouchi, Eiji Munetsuna, Hiroya Yamada, Mirai Yamazaki, Yoshitaka Ando, Genki Mizuno, Miyuki Ikeya, Itsuki Kageyama, Takuya Wakasugi, Atsushi Teshigawara, Yuji Hattori, Yoshiki Tsuboi, Hiroaki Ishikawa, Koji Suzuki, Koji Ohashi
Summary: This study aimed to elucidate the molecular mechanism by which maternal high-fructose corn syrup (HFCS) intake increases circulating GC levels in rat offspring. By giving female Sprague Dawley rats HFCS solution, it was found that HFCS led to a decrease in activity of GC-metabolizing enzyme 11 beta-Hsd2 and an increase in renal miR-27a expression. These findings suggest that the elevation of circulating GC levels in offspring induced by maternal HFCS consumption may be explained by a decrease in 11 beta-Hsd2 activity via renal miR-27a expression.
Article
Multidisciplinary Sciences
Panu K. Luukkonen, Ikki Sakuma, Rafael C. Gaspar, Meghan Mooring, Ali Nasiri, Mario Kahn, Xian-Man Zhang, Dongyan Zhang, Henna Sammalkorpi, Anne K. Penttilae, Marju Orho-Melander, Johanna Arola, Anne Juuti, Xuchen Zhang, Dean Yimlamai, Hannele Yki-Jaervinen, Kitt Falk Petersen, Gerald I. Shulman
Summary: The HSD17B13 rs72613567-A variant is associated with a reduced risk of liver fibrosis in nonalcoholic fatty liver disease (NAFLD). The protective effect is related to decreased pyrimidine catabolism mediated by dihydropyrimidine dehydrogenase. Inhibition of pyrimidine catabolism could mimic the protective effect of HSD17B13, suggesting it as a potential therapeutic target against liver fibrosis in NAFLD.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Toxicology
Zdenek Fisar, Kamil Musilek, Ondrej Benek, Lukas Hroch, Lucie Vinklarova, Monika Schmidt, Jana Hroudova, Jiri Raboch
Summary: Novel potential AD drugs were screened in vitro for their effects on mitochondrial enzymes, with six compounds showing minimal impact on mitochondrial respiratory rate and enzyme activity. Among them, AG18051 and one new compound demonstrated inhibition of MAO-B with minimal effects on mitochondrial respiration, making them promising candidates for further testing.
TOXICOLOGY LETTERS
(2021)
Article
Chemistry, Multidisciplinary
Alfinda Novi Kristanti, Nanik Siti Aminah, Imam Siswanto, Yosephine Sri Wulan Manuhara, Muhammad Ikhlas Abdjan, Andika Pramudya Wardana, Ei Ei Aung, Yoshiaki Takaya
Summary: This study identified two inhibitor candidates that interact with the HSD17B1 enzyme through molecular simulation methods and pharmacokinetic studies, and provided information on key residues involved in the inhibition mechanism.
Article
Endocrinology & Metabolism
Eva Kathrin Lamade, Ferdinand Hendlmeier, Stefan A. Wudy, Stephanie H. Witt, Marcella Rietschel, Michaela Coenen, Maria Gilles, Michael Deuschle
Summary: The study revealed time-specific alteration of fetoplacental 11 beta-HSD2 activity, peaking in the morning to protect fetus from maternal glucocorticoids. Acute affective or anxiety disorders were found to impact fetoplacental 11 beta-HSD2 activity.
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
(2021)
Article
Chemistry, Medicinal
Emanuele M. Gargano, Abdelrahman Mohamed, Ahmed S. Abdelsamie, Giuseppe F. Mangiatordi, Hanna Drzewiecka, Pawel P. Jagodzinski, Arcangela Mazzini, Chris J. van Koppen, Matthias W. Laschke, Orazio Nicolotti, Angelo Carotti, Sandrine Marchais-Oberwinkler, Rolf W. Hartmann, Martin Frotscher
Summary: Facing the clinical challenge of NSCLC, there is a genuine need for new therapeutic approaches. The discovery of 17 beta-HSD1 inhibitor 1 through rational design of compound libraries and biological screening shows promise in fighting NSCLC with high selectivity. Further in vivo studies can be pursued based on its pharmacological profile.
ACS MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Environmental Sciences
Kaisheng Gong, Yuanqiong Lin, Pan Wu, Xiaoying Jin, Gary Owens, Zuliang Chen
Summary: This study successfully utilized carbonized-Fe/Ni NPs to remove 17 beta-estradiol (E2) from water, showing excellent adsorption capacity and removal efficiency, with applications in domestic sewage and livestock wastewater treatment, providing an effective means for environmental protection.
Article
Chemistry, Analytical
Yuanyuan Qin, Shuda Liu, Shuyun Meng, Dong Liu, Tianyan You
Summary: The study developed a split aptamer-based sandwich-type ratiometric biosensor for the detection of 17 beta-estradiol (E2) using photoelectrochemical and electrochemical assays. The biosensor utilized split aptamer fragments to recognize E2 and trigger a hybridization chain reaction, resulting in the production of double-stranded DNA labeled with CdTe quantum dots. This DNA complex was able to sensitize CdTe quantum dots and generate response signals for E2 detection. The developed biosensor demonstrated high sensitivity and accuracy with two linear ranges and low detection limits.
ANALYTICA CHIMICA ACTA
(2024)
Article
Pharmacology & Pharmacy
Cristina Gomez, Zerin Alimajstorovic, Nantia Othonos, Denise V. Winter, Sarah White, Gareth G. Lavery, Jeremy W. Tomlinson, Alexandra J. Sinclair, Alex Odermatt
Summary: This study compares the abilities of GUDCA/G7oxoLCA ratio and urinary (5α-THF+THF)/THE ratio to detect pharmacological 11 beta-HSD1 inhibition in humans. Results suggest that GUDCA/G7oxoLCA ratio is a more reliable biomarker for 11 beta-HSD1 inhibition.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Chemistry, Analytical
Lei Wu, Jiayi Dong, Longshan Zhao
Summary: A photoelectrochemical sensor using Ag2S-sensitized BiOBr photoanode material was designed for high-sensitivity analysis of 17 beta-estradiol (E2). The sensor exhibited a wide linear range, low detection limit, and remarkable specificity and stability. A visualization device for E2 detection was also constructed, providing a promising approach for the development of practical PEC sensors.
SENSORS AND ACTUATORS B-CHEMICAL
(2023)
Article
Engineering, Biomedical
Afonso Malheiro, Abhishek Harichandan, Joyce Bernardi, Adrian Seijas-Gamardo, Gonda F. Konings, Paul G. A. Volders, Andrea Romano, Carlos Mota, Paul Wieringa, Lorenzo Moroni
Summary: In this study, a functional humanized in vitro nerve model using induced pluripotent stem cells-derived nociceptors was developed. The model demonstrated realistic responses to stimuli and had enhanced tissue development and stability using a scaffold. Additionally, the model showed potential for integrating other organ cells for more comprehensive studies.
Article
Reproductive Biology
Ying Feng, Zhixiang Wang, Ran Cui, Meizhu Xiao, Huiqiao Gao, Huimin Bai, Bert Delvoux, Zhen Zhang, Andre Dekker, Andrea Romano, Shuzhen Wang, Alberto Traverso, Chongdong Liu, Zhenyu Zhang
Summary: Preoperative circulating leukocytes in patients with serous ovarian carcinoma show significant differences compared to the normal control group, especially the MO/LY ratio. A decision tree model was built using factors like CA125 level, WBC count, lymph node metastasis, MO count, MO/LY ratio, and other parameters to predict patient survival.
JOURNAL OF OVARIAN RESEARCH
(2022)
Article
Oncology
Ying Feng, Zhixiang Wang, Meizhu Xiao, Jinfeng Li, Yuan Su, Bert Delvoux, Zhen Zhang, Andre Dekker, Sofia Xanthoulea, Zhiqiang Zhang, Alberto Traverso, Andrea Romano, Zhenyu Zhang, Chongdong Liu, Huiqiao Gao, Shuzhen Wang, Linxue Qian
Summary: This study developed a machine learning model to predict the histology, stage, and grade of endometrial carcinoma, assisting doctors in making accurate diagnoses and predictions.
FRONTIERS IN ONCOLOGY
(2022)
Article
Immunology
Ying Feng, Meizhu Xiao, Guangming Cao, Hao Liu, Yanfang Li, Shuzhen Wang, Stan Zijtveld, Bert Delvoux, Sofia Xanthoulea, Andrea Romano, Chongdong Liu, Zhenyu Zhang
Summary: This study found that human monocytes can differentiate into tumor-associated macrophages (TAMs) in the microenvironment of serous ovarian carcinoma. The induced TAMs promote the growth and invasion of ovarian cancer cells, and the IL-6sR and JAK-STAT signaling pathway play an important role in this differentiation process.
JOURNAL OF INFLAMMATION-LONDON
(2022)
Article
Medicine, General & Internal
Linda Stevens Brentjens, Denise Habets, Janneke Den Hartog, Salwan Al-Nasiry, Lotte Wieten, Servaas Morre, Aafke Van Montfoort, Andrea Romano, Ron van Golde
Summary: This study aims to investigate the differences in endometrial receptivity parameters between women aged 18-38 with reproductive failure (RIF and RM) and fertile controls, focusing on steroid metabolism, uNK cells, and the microbiome.
Review
Obstetrics & Gynecology
Willem Jan van Weelden, Philine B. Birkendahl, Roy I. Lalisang, Joanna IntHout, Roy F. P. M. Kruitwagen, Andrea Romano, Johanna M. A. Pijnenborg
Summary: This study reviewed the response and toxicity of progestin therapy in patients with advanced stage and recurrent endometrial cancer (EC), and stratified the response based on progesterone receptor (PR) expression and tumour grade. The results showed that progestin therapy is a viable treatment option for advanced stage and recurrent EC, with low toxicity and high overall response rate (ORR) in PR-positive disease. However, the role of PR expression in relation to progression-free survival and overall survival is still unclear.
BJOG-AN INTERNATIONAL JOURNAL OF OBSTETRICS AND GYNAECOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Donald Poirier, Atunga Nyachieo, Andrea Romano, Jenny Roy, Rene Maltais, Daniel Chai, Bert Delvoux, Carla Tomassetti, Arne Vanhie
Summary: The targeted covalent inhibitor PBRM against 178-HSD1 shows promising potential for the treatment of endometriosis, reducing the number and area of lesions and adhesions without adverse effects.
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2022)
Article
Multidisciplinary Sciences
A. A. S. van den Bosch, J. M. A. Pijnenborg, A. Romano, I. S. Haldorsen, H. M. J. Werner
Summary: This study aims to compare hormone levels and inflammatory markers after bilateral salpingo-oophorectomy (BSO) in obese and non-obese patients. The study also examines the impact of fat distribution and diagnosis on these changes, as well as the effect of BSO on menopausal complaints.
Review
Endocrinology & Metabolism
Antonio Mercorio, Pierluigi Giampaolino, Andrea Romano, Patrick Dallenbach, Nicola Pluchino
Summary: This article reviews the endocrine issues and related enzymatic pathways in endometriosis. The clinical role of these enzymes is still controversial and lacks sufficient clinical data. Research on new drug targets is ongoing, but there are challenges, such as evaluating enzyme expression.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Review
Pharmacology & Pharmacy
Tea Lanisnik Rizner, Andrea Romano
Summary: Drugs targeting local estrogen formation have been successfully used for the treatment of hormone dependent cancers and endometriosis. Inhibitors of aromatase and sulfatase have shown clinical effects, while inhibitors of 17beta-hydroxysteroid dehydrogenase 1 are still in preclinical studies.
FRONTIERS IN PHARMACOLOGY
(2023)
Review
Oncology
Anouk A. S. van den Bosch, Johanna M. A. Pijnenborg, Andrea Romano, Bjorn Winkens, Louis J. M. van der Putten, Roy F. P. M. Kruitwagen, Henrica M. J. Werner
Summary: This systematic review found that adipose tissue (AT) distribution plays a significant role in the development and prognosis of endometrial cancer (EC), correlating with obesity measures, histological subtypes, lymph node metastasis, and sex steroid levels. Further well-designed prospective studies are needed to explore these differences more specifically and understand how it can contribute to the prediction and therapy of EC.
FRONTIERS IN ONCOLOGY
(2023)
Review
Oncology
Andrea Romano, Tea Lanisnik Rizner, Henrica Maria Johanna Werner, Andrzej Semczuk, Camille Lowy, Christoph Schroeder, Anne Griesbeck, Jerzy Adamski, Dmytro Fishman, Janina Tokarz
Summary: Endometrial cancer, the most common gynaecological malignancy, has a high incidence and mortality rate in developed countries. There is a need for non/minimally invasive tools for diagnosis and prognosis to manage the increasing number of women at risk. Biomarkers from proteomics and metabolomics can be used to develop such tools, and this review explores the current research in this field. A systematic review of published studies using proteomics and/or metabolomics for biomarker discovery in endometrial cancer is provided, along with recommendations for future studies.
FRONTIERS IN ONCOLOGY
(2023)
Letter
Obstetrics & Gynecology
Willem Jan van Weelden, Philine B. Birkendahl, Roy I. Lalisang, Joanna Inthout, Roy F. P. M. Kruitwagen, Andrea Romano, Johanna M. A. Pijnenborg
BJOG-AN INTERNATIONAL JOURNAL OF OBSTETRICS AND GYNAECOLOGY
(2023)
Article
Reproductive Biology
L. B. P. M. Stevens Brentjens, D. Obukhova, B. Delvoux, J. E. den Hartog, B. N. Bui, F. Mol, J. P. de Bruin, D. Besselink, G. Teklenburg, F. Morgan, M. Baker, F. J. M. Broekmans, R. J. T. van Golde, M. Zamani Esteki, A. Romano
Summary: This pilot study examined the formation and inactivation of 170-oestradiol in endometrial tissue of women undergoing IVF/ICSI treatment. The study found that inhibition of HSD17B1 activity was significantly higher in the non-pregnant group of primary infertile women. Further investigation in larger patient groups is needed to understand the relationship between steroid-metabolising enzyme activity, expression, and implantation outcome.
REPRODUCTION AND FERTILITY
(2023)
Article
Reproductive Biology
Andrea Romano, Sun-Wei Guo, Jan Brosens, Asgerally Fazlebas, Caroline E. Gargett, Stefan Giselbrecht, Martin Gotte, Linda Griffith, Hugh S. Taylor, Robert N. Taylor, Hugo Vankelecom, Charles Chapron, Xiao-Hong Chang, Khaleque N. Khan, Paola Vigano
Summary: This article presents the protocol for a Delphi process to develop a consensus on in vitro methodologies using endometrial cells. By selecting critical methodologies, topics, and items, and conducting surveys and ratings, unbiased guidance for research methods is promoted to increase confidence in the reliability of in vitro models.
REPRODUCTION AND FERTILITY
(2022)