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)
Review
Medicine, General & Internal
Daria Kupczyk, Renata Studzinska, Renata Kolodziejska, Szymon Baumgart, Martyna Modrzejewska, Alina Wozniak
Summary: This paper discusses the role of glucocorticoids in the human body, their relationship with obesity, metabolic syndrome, and cardiovascular complications, and emphasizes the importance of selective inhibition of 11 beta-HSD1 in the treatment of these diseases.
JOURNAL OF CLINICAL MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Beom Jun Kim, Noo Ri Lee, Chung Hyeok Lee, Young Bin Lee, Sung Jay Choe, Solam Lee, Hyun Jee Hwang, Eunjung Kim, Gareth G. Lavery, Kyong-Oh Shin, Kyungho Park, Eung Ho Choi
Summary: Increased expression of 11 beta-HSD1 in aged skin leads to elevated levels of active glucocorticoids, suppressing sebaceous lipid biosynthesis and causing impaired epidermal permeability barrier.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Rahul Singh, Vijay Kumar Bhardwaj, Pralay Das, Rituraj Purohit
Summary: Aminoarylbenzosuberene (AAB) molecules were analyzed in silico to develop potent inhibitors for 11 beta-Hydroxysteroid dehydrogenase (11 beta-HSD1) protein. AAB4 molecule showed stronger interactions and binding affinity compared to the standard inhibitors.
CHEMICAL COMMUNICATIONS
(2022)
Article
Biochemistry & Molecular Biology
Chloe G. Fenton, Ana Crastin, Claire S. Martin, Saicharan Suresh, Isabella Montagna, Bismah Hussain, Amy J. Naylor, Simon W. Jones, Morten S. Hansen, Caroline M. Gorvin, Maria Price, Andrew Filer, Mark S. Cooper, Gareth G. Lavery, Karim Raza, Rowan S. Hardy
Summary: This study reveals the critical role of 11 beta-HSD1 in inflammatory bone loss and its involvement in the anti-inflammatory effects of therapeutic glucocorticoids (GCs) in chronic inflammatory disease.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
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
Pharmacology & Pharmacy
Michael Weingartner, Simon Stucheli, Denise Kratschmar, Julia Birk, Petra Klusonova, Karen E. Chapman, Gareth G. Lavery, Alex Odermatt
Summary: The study found that the plasma ratio of UDC-Tau to 7oxoLC-Tau can serve as a biomarker for decreased 11 beta-HSD1 oxoreduction activity in different mouse models. Enzyme product to substrate ratios were more reliable markers of 11 beta-HSD1 activity than absolute levels due to large inter-individual variations in bile acid concentrations. The persistence of oxoreduction activity in the face of cofactor loss indicates the existence of an alternative NADPH source in the endoplasmic reticulum.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Article
Immunology
Rahul Y. Mahida, Sian Lax, Christopher R. Bassford, Aaron Scott, Dhruv Parekh, Rowan S. Hardy, Babu Naidu, Michael A. Matthay, Paul M. Stewart, Mark C. Cooper, Gavin D. Perkins, David R. Thickett
Summary: Acute Respiratory Distress Syndrome (ARDS) is a severe inflammatory lung disease commonly caused by sepsis. Glucocorticoids are immune-modulating steroids that can suppress inflammation. Impaired activity of 11 beta-hydroxysteroid dehydrogenase type-1 (HSD-1) and glucocorticoid activation in alveolar macrophages (AMs) may lead to greater inflammatory injury and worse outcomes in sepsis-related ARDS.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Endocrinology & Metabolism
Xinyu Li, Shuanggang Hu, Qinling Zhu, Guangxin Yao, Jufang Yao, Jiaxing Li, Yuan Wang, Ying Ding, Jia Qi, Rui Xu, Hanting Zhao, Zhenyi Zhu, Yanzhi Du, Kang Sun, Yun Sun
Summary: Elevated 11 beta-HSD1 levels in the ovaries are involved in the pathogenesis of PCOS by impairing insulin signaling pathway and ECM remodeling. Selective inhibition of 11 beta-HSD1 ameliorates a cluster of PCOS phenotypes, indicating its potential role as a novel and promising strategy for the treatment of PCOS.
METABOLISM-CLINICAL AND EXPERIMENTAL
(2021)
Article
Chemistry, Medicinal
Jurica Novak, Vadim E. Tseilikman, Olga B. Tseilikman, Svetlana S. Lazuko, Lyudmila E. Belyeva, Azam Rahmani, Julia Fedotova
Summary: This study investigated the binding possibility of resveratrol to 11 beta-HSD-1 using molecular docking and molecular dynamics simulations. The results showed that the 11 beta-HSD-1:resveratrol complex was stable on the microsecond time scale, and binding was achieved through hydrogen bonds and hydrophobic interactions. In vivo studies demonstrated the ability of resveratrol to reduce 11 beta-HSD-1 activity in the liver, accompanied by changes in corticosterone levels and anxiety levels.
Article
Pharmacology & Pharmacy
Eun-Nam Kim, Gil-Saeng Jeong
Summary: This study evaluated the effectiveness of the compound betulin in inhibiting periodontitis. The results showed that betulin inhibited the production of pro-inflammatory mediators and regulated the expression of osteogenic markers. Furthermore, betulin administration alleviated alveolar bone loss and periodontal inflammation in an animal model. Therefore, betulin has the potential to be a new treatment for periodontitis.
Article
Biotechnology & Applied Microbiology
Yang Yue, Fu Xu, JiaRong Zhang, Miao Zhao, FangFang Zhou
Summary: This study found that Sufentanil (SUF) enhances HTR8/SVneo cell proliferation by inhibiting miR-24-3p and promoting HSD11B2 expression. In patients with pre-eclampsia, miR-24-3p is increased while HSD1162 is inhibited, and miR-24-3p targets HSD11B2. Additionally, SUF restrains the progression of pre-eclampsia in vivo and in vitro by mediating the miR-24-3p/HSD11B2 axis.
Review
Medicine, General & Internal
Jonathan Seckl
Summary: 11 beta-HSDs are enzymes that convert active 11-hydroxy glucocorticoids to their inert 11-keto forms. 11 beta-HSD2 inactivates glucocorticoids and has important roles in the kidney and developing foetal brain. In contrast, 11 beta-HSD1 amplifies active glucocorticoid levels in the brain and is associated with age-related cognitive decline.
JOURNAL OF INTERNAL MEDICINE
(2023)
Article
Endocrinology & Metabolism
Nicola Wheelan, Jonathan R. Seckl, Joyce L. W. Yau
Summary: This study investigates how a deficiency of 11β-HSD1 and aging modulates fear conditioning and PTSD-like memory in mice. The results indicate that a deficiency of 11β-HSD1 protects young adult mice against amnesia for the conditioning context and hypermnesia for a salient tone, but only prevents contextual amnesia in aged mice.
PSYCHONEUROENDOCRINOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Mohamad Hafizi Abu Bakar, Mohamad Shamil Faris Mohamad Khalid, Nor Shafiqah Nor Shahril, Khairul Anuar Shariff, Thiruventhan Karunakaran
Summary: Celastrol improves glucose tolerance, lipid profiles, and insulin sensitivity, reduces hepatic glucose production, attenuates inflammation, mitigates oxidative stress, and inhibits 11 beta-HSD1 activity in adipose tissues, highlighting its potential in combating metabolic syndrome induced by high fructose consumption.
Meeting Abstract
Cardiac & Cardiovascular Systems
E. J. Batchen, R. V. Richardson, A. J. W. Thomson, C. M. Moran, G. A. Gray, K. E. Chapman
Meeting Abstract
Cardiac & Cardiovascular Systems
Kathryn Wilson, James Baily, Carl Tucker, Sharron Vass, Carmel Moran, Karen Chapman, John Mullins, Chris Kenyon, Patrick Hadoke, Martin Denvir
Article
Developmental Biology
Usua Laresgoiti, Marko Z. Nikolic, Chandrika Rao, Jane L. Brady, Rachel V. Richardson, Emma J. Batchen, Karen E. Chapman, Emma L. Rawlins
Article
Endocrinology & Metabolism
Christopher I. White, Maurits A. Jansen, Kieran McGregor, Katie J. Mylonas, Rachel V. Richardson, Adrian Thomson, Carmel M. Moran, Jonathan R. Seckl, Brian R. Walker, Karen E. Chapman, Gillian A. Gray
Article
Endocrinology & Metabolism
Agnes E. Coutinho, Tiina M. J. Kipari, Zhenguang Zhang, Cristina L. Esteves, Christopher D. Lucas, James S. Gilmour, Scott P. Webster, Brian R. Walker, Jeremy Hughes, John S. Savill, Jonathan R. Seckl, Adriano G. Rossi, Karen E. Chapman
Review
Endocrinology & Metabolism
Gillian A. Gray, Christopher I. White, Raphael F. P. Castellan, Sara J. McSweeney, Karen E. Chapman
JOURNAL OF MOLECULAR ENDOCRINOLOGY
(2017)
Article
Endocrinology & Metabolism
J. Qiu, D. R. Dunbar, J. Noble, C. Cairns, R. Carter, V. Kelly, K. E. Chapman, J. R. Seckl, J. L. W. Yau
JOURNAL OF NEUROENDOCRINOLOGY
(2016)
Article
Pediatrics
Shuji Sai, Masaki Yamamoto, Rie Yamaguchi, Karen E. Chapman, Teruaki Hongo
Article
Multidisciplinary Sciences
Caitlin S. Wyrwoll, June Noble, Adrian Thomson, Dijana Tesic, Mark R. Miller, Eva A. Rog-Zielinska, Carmel M. Moran, Jonathan R. Seckl, Karen E. Chapman, Megan C. Holmes
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2016)
Review
Immunology
Maria Emilia Solano, Megan C. Holmes, Paul R. Mittelstadt, Karen E. Chapman, Eva Tolosa
SEMINARS IN IMMUNOPATHOLOGY
(2016)
Review
Endocrinology & Metabolism
Rachel V. Richardson, Emma J. Batchen, Martin A. Denvir, Gillian A. Gray, Karen E. Chapman
TRENDS IN ENDOCRINOLOGY AND METABOLISM
(2016)
Article
Pharmacology & Pharmacy
Dongxing Zhu, Nabil A. Rashdan, Karen E. Chapman, Patrick W. F. Hadoke, Vicky E. MacRae
VASCULAR PHARMACOLOGY
(2016)
Article
Multidisciplinary Sciences
Leen Vandermosten, Thao-Thy Pham, Sofie Knoops, Charlotte De Geest, Natacha Lays, Kristof Van der Molen, Christopher J. Kenyon, Manu Verma, Karen E. Chapman, Frans Schuit, Karolien De Bosscher, Ghislain Opdenakker, Philippe E. Van den Steen
NATURE COMMUNICATIONS
(2018)
Editorial Material
Biochemistry & Molecular Biology
Karen E. Chapman
Article
Neurosciences
Jessica R. Ivy, Roderic N. Carter, Jin-Feng Zhao, Charlotte Buckley, Helena Urquijo, Eva A. Rog-Zielinska, Emma Panting, Lenka Hrabalkova, Cara Nicholson, Emma J. Agnew, Matthew W. Kemp, Nicholson N. Morton, Sarah J. Stock, Caitlin Wyrwoll, Ian G. Ganley, Karen E. Chapman
Summary: The late gestational increase in glucocorticoids helps in the maturation of the fetal heart, particularly in the switch from carbohydrate to fatty acid oxidation. Excessive use of exogenous glucocorticoids may interfere with normal fetal heart development and pose potential clinical risks.
JOURNAL OF PHYSIOLOGY-LONDON
(2021)