List of works - Iain Uings

A pharmacological approach to enhancing the therapeutic index of corticosteroids in airway inflammatory disease

scientific article

Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists

scientific article published on 5 November 2008

Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes

scientific article published on 22 August 2019

CDK12 inhibition reduces abnormalities in cells from patients with myotonic dystrophy and in a mouse model

scientific article published on 01 April 2020

Cyclic peptide interleukin 5 antagonists mimic CD turn recognition epitope for receptor alpha.

scientific article published in April 2004

Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an "agreement docking" method

scientific article published on July 2005

Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor

scientific article

Designing corticosteroid drugs for pulmonary selectivity

scientific article

Development of IL-5 receptor antagonists

scientific article

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

scientific article

Discovery and characterization of small molecule inhibitors of the BET family bromodomains

scientific article

Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity

scientific article published on 31 December 2010

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains

scientific article

Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series

scientific article published on July 2006

Effects of dexamethasone on TNF-alpha-induced release of cytokines from purified human blood eosinophils

scientific article

Functional analysis of the interleukin-5 receptor antagonist peptide, AF18748.

scientific article published on June 2004

Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists

scientific article

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

scientific article published on 27 September 2016

Inhibition of nuclear factor-kappaB activation un-masks the ability of TNF-alpha to induce human eosinophil apoptosis

scientific article published in February 2002

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

Molecular Patterns in Acute Pancreatitis Reflect Generalizable Endotypes of the Host Response to Systemic Injury in Humans

scientific article published on 02 June 2020

Multiomic definition of generalizable endotypes in human acute pancreatitis

Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics

scientific article published on 26 June 2007

Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity

scientific article

Pharmacological disruption of the MID1/α4 interaction reduces mutant Huntingtin levels in primary neuronal cultures

scientific article published on 27 February 2018

Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease

scientific article

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

scientific article published on 12 June 2017

Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists

scientific article published in June 2010

Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation

scientific article published on 09 March 2020

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

scientific article published on 09 March 2017

The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist

scientific article

The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.

scientific article

List of works by Iain Uings

A pharmacological approach to enhancing the therapeutic index of corticosteroids in airway inflammatory disease

Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists

Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes

CDK12 inhibition reduces abnormalities in cells from patients with myotonic dystrophy and in a mouse model

Cyclic peptide interleukin 5 antagonists mimic CD turn recognition epitope for receptor alpha.

Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an "agreement docking" method

Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor

Designing corticosteroid drugs for pulmonary selectivity

Development of IL-5 receptor antagonists

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

Discovery and characterization of small molecule inhibitors of the BET family bromodomains

Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains

Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series

Effects of dexamethasone on TNF-alpha-induced release of cytokines from purified human blood eosinophils

Functional analysis of the interleukin-5 receptor antagonist peptide, AF18748.

Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists

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

Inhibition of nuclear factor-kappaB activation un-masks the ability of TNF-alpha to induce human eosinophil apoptosis

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

Molecular Patterns in Acute Pancreatitis Reflect Generalizable Endotypes of the Host Response to Systemic Injury in Humans

Multiomic definition of generalizable endotypes in human acute pancreatitis

Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics

Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity

Pharmacological disruption of the MID1/α4 interaction reduces mutant Huntingtin levels in primary neuronal cultures

Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease

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

Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists

Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation

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

The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist

The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.