List of works - Robin L. Thurmond

A phase 2a study of toreforant, a histamine H4 receptor antagonist, in eosinophilic asthma

A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties

scientific journal article

Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands

scientific article published on 11 April 2010

Alcaftadine, a new antihistamine with combined antagonist activity at histamine H1, H2, and H4 receptors

article

Antagonism of the histamine H4 receptor reduces LPS-induced TNF production in vivo

scientific article published on 27 March 2013

Antigen Presenting Cells as Drug Targets

Antihistamines and itch

scientific article published on January 2015

Behavioural phenotype of histamine H4 receptor knockout mice: Focus on central neuronal functions

scientific article published on 26 November 2016

Cathepsin S inhibitors as novel immunomodulators

scientific article

Chapter 3 NMR Studies of Membrane Lipid Properties

Clinical Development of Histamine H4 Receptor Antagonists

scientific article

Clinical and preclinical characterization of the histamine H(4) receptor antagonist JNJ-39758979.

scientific article published on 18 February 2014

Cloning and pharmacological characterization of the dog histamine H4 receptor

scientific article

Cloning, expression, purification, and activity of dog (Canis familiaris) and monkey (Saimiri boliviensis) cathepsin S.

scientific article published in March 2003

Conformational energetics of rhodopsin modulated by nonlamellar-forming lipids

scientific article

Curvature, order, and dynamics of lipid hexagonal phases studied by deuterium NMR spectroscopy.

scientific article published on May 1993

Deuterium NMR study of intermolecular interactions in lamellar phases containing palmitoyllysophosphatidylcholine

article

Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors

scientific article

Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists

scientific article published on 21 February 2014

Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.

scientific article

Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors.

scientific article published on March 2005

Elastic deformation of membrane bilayers probed by deuterium NMR relaxation

scientific article published in July 2002

Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist

scientific article

Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators

scientific article published on 20 May 2015

Gene-Expression - Based Responses to Drug Treatment

scientific article

Histamine H 4 receptor antagonists

Histamine H4 receptor activation enhances LPS-induced IL-6 production in mast cells via ERK and PI3K activation

article

Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines

scientific article

Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus

scientific article

Histamine H4 receptor expression is elevated in human nasal polyp tissue

scientific article published on 21 May 2007

Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells

scientific article

Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation

scientific article published on May 2004

Histamine H4 receptor optimizes T regulatory cell frequency and facilitates anti-inflammatory responses within the central nervous system

scientific article published on 5 December 2011

Histamine H4-receptors inhibit mast cell renin release in ischemia/reperfusion via protein kinase C ε-dependent aldehyde dehydrogenase type-2 activation

scientific article

Histamine H4receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation

Histamine Receptors and Signaling

Histamine down-regulates IL-27 production in antigen-presenting cells.

scientific article published on 2 March 2012

Histamine inflammation. Preface

scientific article published on January 1, 2010

Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands

scientific article

Identification of a Potent and Selective Noncovalent Cathepsin S Inhibitor ⬇️

scientific article published on October 17, 2003

Influences of membrane curvature in lipid hexagonal phases studied by deuterium NMR spectroscopy

article

Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.

scientific article

Kinetics of small molecule inhibitor binding to p38 kinase

scientific article published in November 2001

Magnetic alignment and orientational order of dipalmitoylphosphatidylcholine bilayers containing palmitoyllsyophosphatidylcholine

scientific article published on 01 June 1990

Membrane Thickness and Molecular Ordering in Acholeplasma laidlawii Strain A Studied by 2H NMR Spectroscopy

scientific article published on 01 November 1994

Molecular determinants of ligand binding to H4R species variants

scientific article

Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.

scientific article published in September 2004

Organic cation transporter 3 modulates murine basophil functions by controlling intracellular histamine levels

scientific journal article

Peripheral Neuronal Mechanism of Itch

Pharmacological characterization of oxime agonists of the histamine H4 receptor

scholarly article by Robin L. Thurmond published December 2009 in Journal of Receptor, Ligand and Channel Research

Phosphoinositide 3-kinase gamma (PI3Kgamma) inhibitors for the treatment of inflammation and autoimmune disease

scientific article published on January 2010

Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists

scientific article published on December 2005

Proteases as Drug Targets

Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: optimization of cellular potency

scientific article published on 10 September 2009

Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements

scientific article

Pyrazole-based cathepsin S inhibitors with improved cellular potency

scientific article published in 2007

RHAMM, a receptor for hyaluronan-mediated motility, compensates for CD44 in inflamed CD44-knockout mice: a different interpretation of redundancy

scientific article

Recent advances in the design of cathepsin S inhibitors

scientific article published on January 2010

Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy

scientific article published on August 2015

STAT1 phosphorylation and cleavage is regulated by the histamine (H4) receptor in human atopic and non-atopic lymphocytes

Structural requirements for inverse agonism and neutral antagonism of indole-, benzimidazole-, and thienopyrrole-derived histamine H4 receptor ligands

scientific article

Structure and packing of phosphatidylcholines in lamellar and hexagonal liquid-crystalline mixtures with a nonionic detergent: a wide-line deuterium and phosphorus-31 NMR study

Subdomains in the F and G helices of bacteriorhodopsin regulate the conformational transitions of the reprotonation mechanism

scientific article

TLR7/9 antagonists as therapeutics for immune-mediated inflammatory disorders

scientific article published on December 2007

The Histamine H4 Receptor: Drug Discovery in the Post-genomic Era

The Role of Histamine H4 Receptor in Asthma and Atopic Dermatitis

The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors

scientific article published on 3 February 2006

The first potent and selective non-imidazole human histamine H4 receptor antagonists

scientific article published on September 2003

The future antihistamines: histamine H3 and H4 receptor ligands

scientific article published on January 2010

The histamine H(4) receptor: a novel modulator of inflammatory and immune disorders

scientific article published on 28 December 2006

The histamine H4 receptor and potential therapeutic uses for H4 ligands

scientific article

The histamine H4 receptor as a new therapeutic target for inflammation

scientific article

The histamine H4 receptor in autoimmune disease

scientific article published on November 2006

The histamine H4 receptor is a potent inhibitor of adhesion-dependent degranulation in human neutrophils

scientific article published on 5 May 2014

The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells

scientific article published in June 2006

The histamine H4 receptor mediates inflammation and Th17 responses in preclinical models of arthritis

scientific article

The histamine H4 receptor mediates inflammation and pruritus in Th2-dependent dermal inflammation

scientific article published on 12 November 2009

The histamine H4 receptor: from orphan to the clinic

scientific article published on 31 March 2015

The histamine H₄ receptor antagonist, JNJ 39758979, is effective in reducing histamine-induced pruritus in a randomized clinical study in healthy subjects

scientific article published on 9 May 2014

The mechanism of molecular redundancy in autoimmune inflammation in the context of CD44 deficiency

scientific article

The new biology of histamine receptors

scientific article published on March 2008

The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines

scientific article published on January 2008

Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors

scientific article

Toreforant, A Histamine H4 Receptor Antagonist, in Patients with Active Rheumatoid Arthritis Despite Methotrexate Therapy: Results of 2 Phase II Studies

scientific article published on 15 July 2016

Triamino pyrimidines and pyridines as histamine H4 receptor modulators

scientific article published in 2011

List of works by Robin L. Thurmond

A phase 2a study of toreforant, a histamine H4 receptor antagonist, in eosinophilic asthma

A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties

Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands

Alcaftadine, a new antihistamine with combined antagonist activity at histamine H1, H2, and H4 receptors

Antagonism of the histamine H4 receptor reduces LPS-induced TNF production in vivo

Antigen Presenting Cells as Drug Targets

Antihistamines and itch

Behavioural phenotype of histamine H4 receptor knockout mice: Focus on central neuronal functions

Cathepsin S inhibitors as novel immunomodulators

Chapter 3 NMR Studies of Membrane Lipid Properties

Clinical Development of Histamine H4 Receptor Antagonists

Clinical and preclinical characterization of the histamine H(4) receptor antagonist JNJ-39758979.

Cloning and pharmacological characterization of the dog histamine H4 receptor

Cloning, expression, purification, and activity of dog (Canis familiaris) and monkey (Saimiri boliviensis) cathepsin S.

Conformational energetics of rhodopsin modulated by nonlamellar-forming lipids

Curvature, order, and dynamics of lipid hexagonal phases studied by deuterium NMR spectroscopy.

Deuterium NMR study of intermolecular interactions in lamellar phases containing palmitoyllysophosphatidylcholine

Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors

Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists

Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.

Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors.

Elastic deformation of membrane bilayers probed by deuterium NMR relaxation

Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist

Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators

Gene-Expression - Based Responses to Drug Treatment

Histamine H 4 receptor antagonists

Histamine H4 receptor activation enhances LPS-induced IL-6 production in mast cells via ERK and PI3K activation

Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines

Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus

Histamine H4 receptor expression is elevated in human nasal polyp tissue

Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells

Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation

Histamine H4 receptor optimizes T regulatory cell frequency and facilitates anti-inflammatory responses within the central nervous system

Histamine H4-receptors inhibit mast cell renin release in ischemia/reperfusion via protein kinase C ε-dependent aldehyde dehydrogenase type-2 activation

Histamine H4receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation

Histamine Receptors and Signaling

Histamine down-regulates IL-27 production in antigen-presenting cells.

Histamine inflammation. Preface

Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands

Identification of a Potent and Selective Noncovalent Cathepsin S Inhibitor ⬇️

Influences of membrane curvature in lipid hexagonal phases studied by deuterium NMR spectroscopy

Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.

Kinetics of small molecule inhibitor binding to p38 kinase

Magnetic alignment and orientational order of dipalmitoylphosphatidylcholine bilayers containing palmitoyllsyophosphatidylcholine

Membrane Thickness and Molecular Ordering in Acholeplasma laidlawii Strain A Studied by 2H NMR Spectroscopy

Molecular determinants of ligand binding to H4R species variants

Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.

Organic cation transporter 3 modulates murine basophil functions by controlling intracellular histamine levels

Peripheral Neuronal Mechanism of Itch

Pharmacological characterization of oxime agonists of the histamine H4 receptor

Phosphoinositide 3-kinase gamma (PI3Kgamma) inhibitors for the treatment of inflammation and autoimmune disease

Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists

Proteases as Drug Targets

Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: optimization of cellular potency

Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements

Pyrazole-based cathepsin S inhibitors with improved cellular potency

RHAMM, a receptor for hyaluronan-mediated motility, compensates for CD44 in inflamed CD44-knockout mice: a different interpretation of redundancy

Recent advances in the design of cathepsin S inhibitors

Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy

STAT1 phosphorylation and cleavage is regulated by the histamine (H4) receptor in human atopic and non-atopic lymphocytes

Structural requirements for inverse agonism and neutral antagonism of indole-, benzimidazole-, and thienopyrrole-derived histamine H4 receptor ligands

Structure and packing of phosphatidylcholines in lamellar and hexagonal liquid-crystalline mixtures with a nonionic detergent: a wide-line deuterium and phosphorus-31 NMR study

Subdomains in the F and G helices of bacteriorhodopsin regulate the conformational transitions of the reprotonation mechanism

TLR7/9 antagonists as therapeutics for immune-mediated inflammatory disorders

The Histamine H4 Receptor: Drug Discovery in the Post-genomic Era

The Role of Histamine H4 Receptor in Asthma and Atopic Dermatitis

The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors

The first potent and selective non-imidazole human histamine H4 receptor antagonists

The future antihistamines: histamine H3 and H4 receptor ligands

The histamine H(4) receptor: a novel modulator of inflammatory and immune disorders

The histamine H4 receptor and potential therapeutic uses for H4 ligands

The histamine H4 receptor as a new therapeutic target for inflammation

The histamine H4 receptor in autoimmune disease

The histamine H4 receptor is a potent inhibitor of adhesion-dependent degranulation in human neutrophils

The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells

The histamine H4 receptor mediates inflammation and Th17 responses in preclinical models of arthritis

The histamine H4 receptor mediates inflammation and pruritus in Th2-dependent dermal inflammation

The histamine H4 receptor: from orphan to the clinic

The histamine H₄ receptor antagonist, JNJ 39758979, is effective in reducing histamine-induced pruritus in a randomized clinical study in healthy subjects