11β-HSD1 Inhibition Rescues SAMP8 Cognitive Impairment Induced by Metabolic Stress
Sign Up to like & getrecommendations! Published in 2019 at "Molecular Neurobiology"
DOI: 10.1007/s12035-019-01708-4
Abstract: Ageing and obesity have been shown to increase the risk of cognitive decline and Alzheimer’s disease (AD). Besides, elevated glucocorticoid (GCs) levels cause metabolic stress and have been associated with the neurodegenerative process. Direct pieces… read more here.
Keywords: hsd1; metabolic stress; treatment; inhibition ... See more keywords
Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.11.004
Abstract: Current endocrine therapeutics for the estrogen-dependent disease endometriosis often lead to considerable side-effects as they act by reducing estrogen action systemically. A more recent approach takes advantage of the fact that the weak estrogen estrone… read more here.
Keywords: estrogen dependent; hsd1; estrogen; nanomolar ic50 ... See more keywords
A Novel 18F-Labeled Radioligand for Positron Emission Tomography Imaging of 11β-Hydroxysteroid Dehydrogenase (11β-HSD1): Synthesis and Preliminary Evaluation in Nonhuman Primates.
Sign Up to like & getrecommendations! Published in 2019 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.8b00715
Abstract: 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the conversion of cortisone to cortisol and controls a key pathway in the regulation of stress. Studies have implicated 11β-HSD1 in metabolic diseases including type 2 diabetes and obesity,… read more here.
Keywords: 18f labeled; 18f as2471907; hsd1; nonhuman primates ... See more keywords
Identification of 11β-HSD1 inhibitors through enhanced sampling methods.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d1cc06894f
Abstract: Aminoarylbenzosuberene (AAB) molecules were chosen for in silico analysis to develop effective and more competent 11β-hydroxysteroid dehydrogenase (11β-HSD1) protein inhibitors. The AAB4 molecule was shown to have stronger interactions and binding affinity than standard inhibitors… read more here.
Keywords: enhanced sampling; identification hsd1; hsd1; sampling methods ... See more keywords
S100A16-induced adipogenesis is associated with up-regulation of 11 β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
Sign Up to like & getrecommendations! Published in 2019 at "Bioscience Reports"
DOI: 10.1042/bsr20182042
Abstract: The steadily increasing epidemic of obesity continues at alarming rates, is an important public health problem, and expression changes of S100A16 and 11 β-hydroxysteroid dehydrogenase type 1(11β-HSD1) is attributable to the adipocyte differentiation. In our… read more here.
Keywords: expression; hsd1; s100a16 induced; s100a16 ... See more keywords
Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2019.1634064
Abstract: Abstract 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as potential 17β-HSD1… read more here.
Keywords: cofactor dependent; hsd1; substituted alkoxy; synthesis substituted ... See more keywords
Local steroid activation is a critical mediator of the anti-inflammatory actions of therapeutic glucocorticoids
Sign Up to like & getrecommendations! Published in 2020 at "Annals of the Rheumatic Diseases"
DOI: 10.1136/annrheumdis-2020-218493
Abstract: Objectives The enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) plays a well-characterised role in the metabolism and activation of endogenous glucocorticoids (GCs). However, despite its potent upregulation at sites of inflammation, its role in peripheral metabolism… read more here.
Keywords: anti inflammatory; hsd1; inflammation; deletion ... See more keywords
11β-HSD1 determines the extent of muscle atrophy in a model of acute exacerbation of COPD
Sign Up to like & getrecommendations! Published in 2023 at "American Journal of Physiology - Lung Cellular and Molecular Physiology"
DOI: 10.1152/ajplung.00009.2022
Abstract: Muscle atrophy is an extra-pulmonary complication of acute exacerbations (AE) in chronic obstructive pulmonary disease (COPD). The endogenous production and therapeutic application of glucocorticoids (GCs) have been implicated as drivers of muscle loss in AE-COPD.… read more here.
Keywords: hsd1; copd; muscle wasting; muscle ... See more keywords
11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor Development by Lentiviral Screening Based on Computational Modeling
Sign Up to like & getrecommendations! Published in 2018 at "Pharmacology"
DOI: 10.1159/000491397
Abstract: In this study, rat and human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have been cloned by lentiviral transduction and expressed by CHO-K1 cells. The results showed that recombinant plasmids contained R11bhsd1 or H11bhsd1 have been constructed,… read more here.
Keywords: dehydrogenase type; hydroxysteroid dehydrogenase; inhibitor; hsd1 ... See more keywords
OR09-3 11β-HSD1 Mediates a Partial Suppression of Muscle Atrophy in Chronic Inflammatory Disease in Response to Therapeutic Glucocorticoids
Sign Up to like & getrecommendations! Published in 2019 at "Journal of the Endocrine Society"
DOI: 10.1210/js.2019-or09-3
Abstract: Abstract Objective: Therapeutic glucocorticoids (GCs) are routinely used in the treatment of chronic inflammatory disease due to their potent anti-inflammatory effects. Despite their efficacy, chronic exposure to GCs elicits undesirable side effects, including muscle atrophy… read more here.
Keywords: inflammatory; hsd1; gcs; atrophy ... See more keywords
Oral 11β-HSD1 inhibitor AZD4017 improves wound healing and skin integrity in adults with type 2 diabetes mellitus: a pilot randomized controlled trial
Sign Up to like & getrecommendations! Published in 2022 at "European Journal of Endocrinology"
DOI: 10.1530/eje-21-1197
Abstract: Background Chronic wounds (e.g. diabetic foot ulcers) reduce the quality of life, yet treatments remain limited. Glucocorticoids (activated by the enzyme 11β-hydroxysteroid dehydrogenase type 1, 11β-HSD1) impair wound healing. Objectives Efficacy, safety, and feasibility of… read more here.
Keywords: wound healing; hsd1; inhibitor azd4017; type diabetes ... See more keywords