List of works - Scott P Webster

11-Beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors in Type 2 diabetes mellitus and obesity

scientific article published on 25 March 2008

11Beta-hydroxysteroid dehydrogenase-1 deficiency or inhibition enhances hepatic myofibroblast activation in murine liver fibrosis.

scientific article

11β-Hydroxysteroid Dehydrogenase Type 1 Is Expressed in Neutrophils and Restrains an Inflammatory Response in Male Mice.

scientific article published on 4 May 2016

11β-Hydroxysteroid dehydrogenase type 1 contributes to the balance between 7-keto- and 7-hydroxy-oxysterols in vivo

scientific article published on 13 February 2013

A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.

scientific article published in March 2010

A magnetic bead-based ligand binding assay to facilitate human kynurenine 3-monooxygenase drug discovery

scientific article

Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides.

scientific article

Antidiabetic and toxicological evaluations of naringenin in normoglycaemic and NIDDM rat models and its implications on extra-pancreatic glucose regulation.

scientific article

Antihyperglycemic and sub-chronic antidiabetic actions of morolic and moronic acids, in vitro and in silico inhibition of 11β-HSD 1.

scientific article published on 27 February 2013

Bacterial expression of human kynurenine 3-monooxygenase: solubility, activity, purification

scientific article published on 04 December 2013

Characterisation of 8-amino-7-oxononanoate synthase: A bacterial PLP-dependent, acyl CoA condensing enzyme

scientific article published on 01 August 1998

Cognitive and Disease-Modifying Effects of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibition in Male Tg2576 Mice, a Model of Alzheimer's Disease.

scientific article

Corrigendum: Genetic identification of thiosulfate sulfurtransferase as an adipocyte-expressed antidiabetic target in mice selected for leanness

scientific article published on 01 April 2018

Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction

scientific article published on 4 August 2017

Detecting Drug-Target Binding In Cells Using Fluorescence Activated Cell Sorting Coupled With Mass Spectrometry Analysis

Detecting drug-target binding in cells using fluorescence-activated cell sorting coupled with mass spectrometry analysis

scientific article published on 13 September 2017

Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.

scientific article

Diclofenac Identified as a Kynurenine 3-Monooxygenase Binder and Inhibitor by Molecular Similarity Techniques

scientific article published on 02 March 2018

Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors

scientific article published on 25 February 2007

Discovery, synthesis and in combo studies of a tetrazole analogue of clofibric acid as a potent hypoglycemic agent

scientific article published on 05 April 2013

Elevated hepatic 11β-hydroxysteroid dehydrogenase type 1 induces insulin resistance in uremia.

scientific article published on 25 February 2014

Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 Inhibitors.

scientific article

Genetic identification of thiosulfate sulfurtransferase as an adipocyte-expressed antidiabetic target in mice selected for leanness.

scientific article

In search of a small molecule agonist of the relaxin receptor RXFP1 for the treatment of liver fibrosis.

scientific article published on 7 September 2017

Increased levels of 3-hydroxykynurenine parallel disease severity in human acute pancreatitis.

scientific article published on 27 September 2016

Inhibiting 11β-hydroxysteroid dehydrogenase type 1 prevents stress effects on hippocampal synaptic plasticity and impairs contextual fear conditioning.

scientific article published in February 2014

Intrahippocampal glucocorticoids generated by 11β-HSD1 affect memory in aged mice.

scientific article published on 15 July 2014

Kynurenine 3-monooxygenase (KMO) is a critical regulator of renal ischemia-reperfusion injury

Kynurenine 3-monooxygenase is a critical regulator of renal ischemia-reperfusion injury

scientific article published in 2019

Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis

scientific article

Lead discovery for human kynurenine 3-monooxygenase by high-throughput RapidFire mass spectrometry

scientific article published on 31 December 2013

Mass spectrometry imaging for dissecting steroid intracrinology within target tissues

scientific article

Mechanism of 8-amino-7-oxononanoate synthase: spectroscopic, kinetic, and crystallographic studies

scientific article

Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles

scientific article published on 18 April 2010

Novel 11β-HSD1 inhibitors: C-1 versus C-2 substitution and effect of the introduction of an oxygen atom in the adamantane scaffold

scientific article published in October 2015

Optimal elevation of β-cell 11β-hydroxysteroid dehydrogenase type 1 is a compensatory mechanism that prevents high-fat diet-induced β-cell failure.

scientific article published on 7 February 2012

Partial deficiency or short-term inhibition of 11beta-hydroxysteroid dehydrogenase type 1 improves cognitive function in aging mice.

scientific article published on October 2010

Quantification of 11β-hydroxysteroid dehydrogenase 1 kinetics and pharmacodynamic effects of inhibitors in brain using mass spectrometry imaging and stable-isotope tracers in mice

scientific article published on 14 December 2017

Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase

scientific article

Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11β-HSD1 inhibitors

scientific article published in December 2015

Selection and early clinical evaluation of the brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor UE2343 (Xanamem™)

scientific article published on 23 December 2016

Short-term inhibition of 11β-hydroxysteroid dehydrogenase type 1 reversibly improves spatial memory but persistently impairs contextual fear memory in aged mice

scientific article

Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase

scientific article published on 12 June 2017

Suicide inhibition of α-oxamine synthases: structures of the covalent adducts of 8-amino-7-oxononanoate synthase with trifluoroalanine

article

Synthesis of 2-{2-[(α/β-naphthalen-1-ylsulfonyl)amino]-1,3-thiazol-4-yl} acetamides with 11β-hydroxysteroid dehydrogenase inhibition and in combo antidiabetic activities

scientific article published on 08 January 2014

The crystal structure of 8-amino-7-oxononanoate synthase: a bacterial PLP-dependent, acyl-CoA-condensing enzyme

scientific article

The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis

scientific article published on 09 March 2017

The mechanism of 7,8-diaminopelargonate synthase; the role of S-adenosylmethionine as the amino donor

scientific article published in October 2003

UFSRAT: Ultra-fast Shape Recognition with Atom Types--the discovery of novel bioactive small molecular scaffolds for FKBP12 and 11βHSD1

scientific article

β-Cell-Specific Glucocorticoid Reactivation Attenuates Inflammatory β-Cell Destruction.

scientific article published on 14 October 2014

List of works by Scott P Webster

11-Beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors in Type 2 diabetes mellitus and obesity

11Beta-hydroxysteroid dehydrogenase-1 deficiency or inhibition enhances hepatic myofibroblast activation in murine liver fibrosis.

11β-Hydroxysteroid Dehydrogenase Type 1 Is Expressed in Neutrophils and Restrains an Inflammatory Response in Male Mice.

11β-Hydroxysteroid dehydrogenase type 1 contributes to the balance between 7-keto- and 7-hydroxy-oxysterols in vivo

A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.

A magnetic bead-based ligand binding assay to facilitate human kynurenine 3-monooxygenase drug discovery

Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides.

Antidiabetic and toxicological evaluations of naringenin in normoglycaemic and NIDDM rat models and its implications on extra-pancreatic glucose regulation.

Antihyperglycemic and sub-chronic antidiabetic actions of morolic and moronic acids, in vitro and in silico inhibition of 11β-HSD 1.

Bacterial expression of human kynurenine 3-monooxygenase: solubility, activity, purification

Characterisation of 8-amino-7-oxononanoate synthase: A bacterial PLP-dependent, acyl CoA condensing enzyme

Cognitive and Disease-Modifying Effects of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibition in Male Tg2576 Mice, a Model of Alzheimer's Disease.

Corrigendum: Genetic identification of thiosulfate sulfurtransferase as an adipocyte-expressed antidiabetic target in mice selected for leanness

Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction

Detecting Drug-Target Binding In Cells Using Fluorescence Activated Cell Sorting Coupled With Mass Spectrometry Analysis

Detecting drug-target binding in cells using fluorescence-activated cell sorting coupled with mass spectrometry analysis

Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.

Diclofenac Identified as a Kynurenine 3-Monooxygenase Binder and Inhibitor by Molecular Similarity Techniques

Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors

Discovery, synthesis and in combo studies of a tetrazole analogue of clofibric acid as a potent hypoglycemic agent

Elevated hepatic 11β-hydroxysteroid dehydrogenase type 1 induces insulin resistance in uremia.

Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 Inhibitors.

Genetic identification of thiosulfate sulfurtransferase as an adipocyte-expressed antidiabetic target in mice selected for leanness.

In search of a small molecule agonist of the relaxin receptor RXFP1 for the treatment of liver fibrosis.

Increased levels of 3-hydroxykynurenine parallel disease severity in human acute pancreatitis.

Inhibiting 11β-hydroxysteroid dehydrogenase type 1 prevents stress effects on hippocampal synaptic plasticity and impairs contextual fear conditioning.

Intrahippocampal glucocorticoids generated by 11β-HSD1 affect memory in aged mice.

Kynurenine 3-monooxygenase (KMO) is a critical regulator of renal ischemia-reperfusion injury

Kynurenine 3-monooxygenase is a critical regulator of renal ischemia-reperfusion injury

Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis

Lead discovery for human kynurenine 3-monooxygenase by high-throughput RapidFire mass spectrometry

Mass spectrometry imaging for dissecting steroid intracrinology within target tissues

Mechanism of 8-amino-7-oxononanoate synthase: spectroscopic, kinetic, and crystallographic studies

Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles

Novel 11β-HSD1 inhibitors: C-1 versus C-2 substitution and effect of the introduction of an oxygen atom in the adamantane scaffold

Optimal elevation of β-cell 11β-hydroxysteroid dehydrogenase type 1 is a compensatory mechanism that prevents high-fat diet-induced β-cell failure.

Partial deficiency or short-term inhibition of 11beta-hydroxysteroid dehydrogenase type 1 improves cognitive function in aging mice.

Quantification of 11β-hydroxysteroid dehydrogenase 1 kinetics and pharmacodynamic effects of inhibitors in brain using mass spectrometry imaging and stable-isotope tracers in mice

Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase

Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11β-HSD1 inhibitors

Selection and early clinical evaluation of the brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor UE2343 (Xanamem™)

Short-term inhibition of 11β-hydroxysteroid dehydrogenase type 1 reversibly improves spatial memory but persistently impairs contextual fear memory in aged mice

Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase

Suicide inhibition of α-oxamine synthases: structures of the covalent adducts of 8-amino-7-oxononanoate synthase with trifluoroalanine

Synthesis of 2-{2-[(α/β-naphthalen-1-ylsulfonyl)amino]-1,3-thiazol-4-yl} acetamides with 11β-hydroxysteroid dehydrogenase inhibition and in combo antidiabetic activities

The crystal structure of 8-amino-7-oxononanoate synthase: a bacterial PLP-dependent, acyl-CoA-condensing enzyme

The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis

The mechanism of 7,8-diaminopelargonate synthase; the role of S-adenosylmethionine as the amino donor

UFSRAT: Ultra-fast Shape Recognition with Atom Types--the discovery of novel bioactive small molecular scaffolds for FKBP12 and 11βHSD1

β-Cell-Specific Glucocorticoid Reactivation Attenuates Inflammatory β-Cell Destruction.