On-column ligand exchange for structure-based drug design: a case study with human 11[beta]-hydroxysteroid dehydrogenase type 1...
Resource Type:. Journal Article. Resource Relation:. Journal Name: Acta Crystallogr. F; Journal Volume: 68; Journal Issue: (5 ... Qin, Wenying ; Judge, Russell A. ; Longenecker, Kenton L. ; Solomon, Larry R. ; Harlan, John E.  + Show Author Affiliations ... beta]-hydroxysteroid dehydrogenase type 1 ... a case study with human 11[beta]-hydroxysteroid dehydrogenase ... Title: On-column ligand exchange for structure-based drug design: a case study with human 11[ ...https://www.osti.gov/scitech/biblio/1090101-column-ligand-exchange-structure-based-drug-design-case-study-human-beta-hydroxysteroid-dehydrogenase-type
Research programme: 11-beta hydroxysteroid dehydrogenase type 1 inhibitors - Poxel - AdisInsight
... is developing 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors for the ... Research Type 2 diabetes mellitus Most Recent Events * 21 Oct 2016 11-beta hydroxysteroid dehydrogenase type 1 inhibitors are ... 16 Jul 2016 No recent reports of development identified for research development in Type-2-diabetes-mellitus in France ... 28 May 2009 Early research in Type-2 diabetes mellitus in France (unspecified route) ...https://adisinsight.springer.com/drugs/800032548?error=cookies_not_supported&code=480e00d9-928e-41cc-abbe-2c66721cc61d
11-Beta-Hydroxysteroid Dehydrogenase Type 1 (Hsd11b1) Antibody -Abbexa
11-Beta-Hydroxysteroid Dehydrogenase Type 1 (Hsd11b1) Antibody 由Abbexa供应，该产品简介:11-Beta-Hydroxysteroid Dehydrogenase Type 1 ( ... 注：1.可以使用快捷键Alt+S或Ctrl+Enter发送信息!. 2.如有必要,请您留下您的详细联系方式! ... 产品名称：11-Beta-Hydroxysteroid Dehydrogenase Type 1 (Hsd11b1) Antibody ... 地址：上海市闵http://abbexa.bioleaf.com/Product_2061238823.html
Tissue-specific dysregulation of 11 beta-hydroxysteroid dehydrogenase type 1 and pathogenesis of the metabolic syndrome |...
Elevenbeta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1), a key intracellular enzyme which catalyses the conversion of ... If confirmed, these results would prompt the development of selective and tissue-specific 11beta-HSD-1 inhibitors to decrease ... 11β-hydroxysteroid dehydrogenase type 1; Cortisol; Cortisone; Metabolic syndrome. Settore Scientifico Disciplinare: Settore MED ... are less convincing with several case control and cross-sectional studies showing an association between with 11beta-HSD-1 ...https://air.unimi.it/handle/2434/200905
11beta-hydroxysteroid dehydrogenase type 1 regulates glucocorticoid-induced insulin resistance in skeletal muscle.
... ... 11beta-hydroxysteroid dehydrogenase type 1 regulates glucocorticoid-induced insulin resistance in skeletal muscle. 2009, 58 (11 ... 11beta-Hydroxysteroid dehydrogenase type 1 regulates insulin and glucagon secretion in pancreatic islets. ... Within skeletal muscle, 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) converts cortisone (11-dehydrocorticosterone ...https://www.lenus.ie/handle/10147/254113
11beta-hydroxysteroid dehydrogenase type 1 regulates glucocorticoid-induced insulin resistance in skeletal muscle. - Radcliffe...
Within skeletal muscle, 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) converts cortisone (11-dehydrocorticosterone ... A1 (selective 11beta-HSD1 inhibitor) abolished enzyme activity and blocked the increase in pSer(307) IRS1 and reduction in ... Selective 11beta-HSD1 inhibition decreases pSer(307) IRS1, increases pThr(308) Akt/PKB, and decreases lipogenic and lipolytic ... In C57Bl6/J mice, the selective 11beta-HSD1 inhibitor, A2, decreased fasting blood glucose levels and improved insulin ...https://www.rdm.ox.ac.uk/publications/482083
High-level production and optimization of monodispersity of 11beta-hydroxysteroid dehydrogenase type 1.
Heterologous production of 11beta-HSD1, devoid of its N-terminal transmembrane segment, is possible but yields only small ... Here we show that the soluble portion of recombinant 11beta-HSD1 produced in E. coli is found mainly as multimeric aggregates ... Moreover, active site titration of human 11beta-HSD1 revealed that at least 75% of the protein in a typical preparation ... By co-overexpressing GroEL/ES and adding an 11beta-HSD1 inhibitor during protein synthesis, we have increased the accumulation ...https://oacentre.kennedy.ox.ac.uk/publications/108418
Type 1 11beta-hydroxysteroid dehydrogenase as universal drug target in metabolic diseases?
The latter effect is accomplished by two different 11beta-hydroxysteroid dehydrogenase isozymes, constituting a shuttle system ... The type 2 enzyme is an exclusive NAD+ dependent dehydrogenase of glucocorticoids, thus 'protecting' the mineralocorticoid ... Whereas the type 1 enzyme (11beta-HSD1) is in vitro a NADP(H)- dependent bidirectional enzyme, it reduces in most instances in ... Importantly, 11beta-HSD1 activity appears to be intrinsically linked to all features of the metabolic syndrome, which could at ...https://oacentre.kennedy.ox.ac.uk/publications/108459
Benzothiazole derivatives as novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1. - Department of Pharmacology
11beta-HSD1) have considerable potential as treatments for metabolic diseases, such as diabetes mellitus type 2 or obesity. ... inhibition for 11beta-HSD1 at 10 microM and exhibited IC50 values in the low micromolar range. The preliminary SAR study ... the discovery and synthesis of a series of novel benzothiazole derivatives and their inhibitory activities against 11beta-HSD1 ... Docking studies with the benzothiazole derivative 1 into the crystal structure of human 11beta-HSD1 revealed how the molecule ...https://pharm.ox.ac.uk/publications/640377
Effects of peroxisome proliferator-activated receptor-alpha and -gamma agonists on 11beta-hydroxysteroid dehydrogenase type 1...
Reduced adipose 11beta-HSD1 expression and increased plasma cortisol during longer therapy with rosiglitazone probably reflect ... In 12 healthy men, 4-5 wk of rosiglitazone increased insulin sensitivity during insulin infusion but did not change 11beta-HSD1 ... OBJECTIVE: Our objective was to test whether PPAR agonists alter cortisol secretion and peripheral regeneration by 11beta-HSD1 ... In 12 men with type 2 diabetes 12 wk of rosiglitazone reduced arteriovenous cortisone extraction across abdominal sc adipose ...https://www.rdm.ox.ac.uk/publications/17985
11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response. - Radcliffe Department of...
Therapeutic inhibition of 11beta-HSD1 reductase activity in patients with obesity and the metabolic syndrome, as well as in ... In this review, we discuss both the genetic and enzymatic characterization of 11beta-HSD1, as well as describing its role in ... The molecular basis of cortisone reductase deficiency, the putative '11beta-HSD1 knockout state' in humans, has been defined ... We speculate that hexose-6-phosphate dehydrogenase activity and therefore reduced nicotinamide-adenine dinucleotide phosphate ...https://www.rdm.ox.ac.uk/publications/125554
HSD11B1 ELISA Kits from Abbexa Ltd | Biocompare.com
Rat 11-Beta-Hydroxysteroid Dehydrogenase Type 1 (HSD11B1) ELISA Kit Abbexa Ltd ...https://www.biocompare.com/pfu/110627/soids/2-22505/Assay_Kit/ELISA_HSD11B1?vids=105293
Type 1 11beta -hydroxysteroid dehydrogenase mediates glucocorticoid activation and insulin release in pancreatic islets. - The...
Incubation of beta-cells in the presence of 11-dehydrocorticosterone leads to a dose-dependent inhibition of insulin release, ... carried out by 11beta-hydroxysteroid dehydrogenases (11beta-HSDs). In this study, we determined the role of glucocorticoid ... Inhibition of 11beta-HSD activity by carbenoxolone reverses inhibition of insulin release. The presence of 11beta-HSD in islets ... Expression of type 1 11beta-HSD mRNA was detected by reverse transcriptase-polymerase chain reaction in islets isolated from ob ...https://www.kennedy.ox.ac.uk/publications/108556
Optimal Elevation of β-Cell 11β-Hydroxysteroid Dehydrogenase Type 1 Is a Compensatory Mechanism That Prevents High-Fat Diet...
Beta-cell deficit and increased beta-cell apoptosis in humans with type 2 diabetes. Diabetes 2003;52:102-110pmid:12502499. ... 11Beta-hydroxysteroid dehydrogenase type 1 and obesity. Front Horm Res 2008;36:146-164pmid:18230901. ... 11Beta-hydroxysteroid dehydrogenase type 1 regulates insulin and glucagon secretion in pancreatic islets. Diabetologia 2008;51: ... Preadipocyte 11beta-hydroxysteroid dehydrogenase type 1 is a keto-reductase and contributes to diet-induced visceral obesity in ...http://diabetes.diabetesjournals.org/content/61/3/642
11beta-hydroxysteroid dehydrogenase type 1 mRNA is increased in both visceral and subcutaneous adipose tissue of obese patients ... 11beta-hydroxysteroid dehydrogenase and the pre-receptor regulation of corticosteroid hormone action. J Endocrinol 2005;186:251 ... Overexpression of 11beta-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of ... Type 2 (non-insulin-dependent) diabetes mellitus: the thrifty phenotype hypothesis. Diabetologia 1992;35:595-601 ...http://diabetes.diabetesjournals.org/content/59/1/98
Drug CategoriesBrowse DrugBank Categories - DrugBank
3-Hydroxysteroid Dehydrogenases, antagonists & inhibitors. Not Available. 1. 4. Details. 3-Oxoacyl-(Acyl-Carrier-Protein) ... Adrenergic beta-2 Receptor Agonists. Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.. 14. 39. Details. ... 1. 15. Details. ADP Ribose Transferases. Enzymes that transfer the ADP-RIBOSE group of NAD or NADP to proteins or other small ... 1. Details. Acyltransferases. Enzymes from the transferase class that catalyze the transfer of acyl groups from donor... more. ...https://www.drugbank.ca/categories
Methods for treatment of inflammatory diseases using CT-3 or analogs thereof - BAKER DAVID
Betaseron, a modified beta interferon, has recently been approved for use in MS patients. Although Betaseron treatment showed ... For example, a majority of MS patients have HLA-type DR2a and DR2b. The MS patients having genetic dispositions to MS who are ... First are patients with early disease of the relapsing remitting type. Entry criteria would include disease duration of more ... dependent on the type of noniception being studied.32,33 This is consistent with high levels of CB1 receptors on primary ...http://www.freepatentsonline.com/y2005/0070596.html
11 beta hydroxysteroid dehydrogenase and the syndrome of apparent mineralocorticoid excess | 11β-Hydroxysteroid dehydrogenase...
Their findings showed that the D-bifunctional protein plays an essential role in the peroxisomal beta-oxidation pathway that ... Biochemical analysis showed that the 3-hydroxyacyl-CoA dehydrogenase activity of the D-bifunctional protein was completely ... 11 beta hydroxysteroid dehydrogenase and the syndrome of apparent mineralocorticoid excess. Media:. ... 11 beta hydroxysteroid dehydrogenase and the syndrome of apparent mineralocorticoid excess. In 2 unrelated patients, Ulick et ...http://oiu.steroids-australia.net/11-beta-hydroxysteroid-dehydrogenase-and-the-syndrome-of-apparent-mineralocorticoid-excess.html
3 beta-hydroxysteroid dehydrogenase-1, cholesterol side-chain cleavage cytochrome P450, and steroid-11 beta-hydroxylase) were ... publication type. *Refereed Article (2). * access. *digital, restricted acccess (1). *digital, open acccess (1) ... We will mail you new results for this query: keywords==11-beta-hydroxysteroid dehydrogenase type-1 ... 11-beta-hydroxysteroid dehydrogenase type-1 - protein-coupled receptor - cannabinoid cb1 receptor - brown adipose-tissue - ...http://library.wur.nl/WebQuery/wurpubs?A320==11-beta-hydroxysteroid%20dehydrogenase%20type-1
Chronic Maternal Dietary Chromium Restriction Modulates Visceral Adiposity
Desbriere R, Vuaroqueaux V, Achard V, Boullu-Ciocca S, Labuhn M, Dutour A, Grino M.: 11beta-hydroxysteroid dehydrogenase type 1 ... Draper N, Stewart PM.: 11beta-hydroxysteroid dehydrogenase and the pre-receptor regulation of corticosteroid hormone action. J ... Overexpression of 11beta-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of ... Type 2 (non-insulin-dependent) diabetes mellitus: the thrifty phenotype hypothesis. Diabetologia 1992;35:595-601 [PubMed] ...http://pubmedcentralcanada.ca/pmcc/articles/PMC2797950/
Frontiers | Tissue-Specific Effects of Loss of Estrogen during Menopause and Aging | Endocrinology
... and glucose tolerance in 11beta-hydroxysteroid dehydrogenase type 1 null mice. J. Biol. Chem. 276, 41293-41300. ... Specific regulation of lipocalin-type prostaglandin D synthase in mouse heart by estrogen receptor beta. Mol. Endocrinol. 17, ... 11Beta-hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist ... Sex steroids and leptin regulate 11beta-hydroxysteroid dehydrogenase I and P450 aromatase expressions in human preadipocytes: ...https://www.frontiersin.org/articles/10.3389/fendo.2012.00019/full
11β-Hydroxysteroid dehydrogenase type 1 - Wikipedia
... beta-hydroxysteroid dehydrogenase isoforms using reverse-transcriptase-polymerase chain reaction and localization of the type 2 ... Wake DJ, Walker BR (February 2006). "Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 in obesity". Endocrine. 29 (1): ... Agarwal AK (November 2003). "Cortisol metabolism and visceral obesity: role of 11beta-hydroxysteroid dehydrogenase type I ... "11beta-Hydroxysteroid dehydrogenase types 1 and 2 are up- and downregulated in cortisol-secreting adrenal adenomas". Journal of ...https://en.wikipedia.org/wiki/11%CE%B2-Hydroxysteroid_dehydrogenase_type_1
Begum R[au] - PubMed - NCBI
Genetic variants of tumor necrosis factor-α and its levels: A correlation with dyslipidemia and type 2 diabetes susceptibility. ... A case-control study on association of proteasome subunit beta 8 (PSMB8) and transporter associated with antigen processing 1 ( ... Association of glucose 6-phosphate dehydrogenase (G6PD) 3'UTR polymorphism with vitiligo and in vitro studies on G6PD ... Genetic variants of resistin and its plasma levels: Association with obesity and dyslipidemia related to type 2 diabetes ...https://www.ncbi.nlm.nih.gov/pubmed?cmd=search&term=Begum+R%5Bau%5D&dispmax=50
Browsing by Title
All of DSpaceCommunities & CollectionsIssue DateAuthorsTitlesSubjectsPublication TypeSponsor ... Docherty, Pamela Jane (The University of Edinburgh, 2012-11-28) A current group GX is an infinite-dimensional Lie group of ... Khogeer, Asim Abdulaziz Omar (The University of Edinburgh, 2016-11-29) Bone metastases are a major cause of morbidity in ... Cellular regulation of cortisol in vivo by 11-beta hydroxysteroid dehydrogenase type 1 Anderson, Anna Jane Claire (The ...https://www.era.lib.ed.ac.uk/browse?type=title&sort_by=1&order=ASC&rpp=20&etal=-1&null=&offset=2949
Anthony P. Coll - Semantic Scholar
11beta-Hydroxysteroid dehydrogenase type 1 (11beta-HSD1) converts inert 11keto-glucocorticoids to active 11beta-hydroxy forms, ... Glucocorticoid regulation of the promoter of 11beta-hydroxysteroid dehydrogenase type 1 is indirect and requires CCAAT/enhancer ... protein-beta.. *Shuji Sai, Cristina L. Esteves, +7 authors Karen E. Chapman ...https://www.semanticscholar.org/author/Anthony-P.-Coll/5011191