List of works - Laura H Heitman

A covalent antagonist for the human adenosine A2A receptor

scientific article published on 3 December 2016

A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor

scientific article published in February 2009

Allosteric Modulation of Kv11.1 (hERG) Channels Protects Against Drug-Induced Ventricular Arrhythmias

scientific article published in April 2016

Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist

scientific article published on March 2006

Allosteric modulators of the hERG K(+) channel: radioligand binding assays reveal allosteric characteristics of dofetilide analogs

scientific article published on 5 November 2013

Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor

scientific article

Bias in chemokine receptor signalling

scientific article published on 26 March 2014

Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor

scientific article published on 3 March 2014

Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring

scientific article published on 19 July 2017

Cancer-Associated Mutations of the Adenosine A2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions

scientific article published on 22 July 2022

Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology

scientific article published on 10 June 2022

Cancer‐related somatic mutations alter adenosine A <sub>1</sub> receptor pharmacology—A focus on mutations in the loops and C‐terminus

scientific article published on 23 May 2022

Characterization of 12 GnRH peptide agonists - a kinetic perspective

scientific article published on 23 September 2015

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength

scientific article

Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations

scientific article published on 24 November 2021

Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands

scientific article

Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2.

scientific article

Drug-target residence time--a case for G protein-coupled receptors

scientific article published on 18 February 2014

Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics

scientific article

Equilibrium and kinetic selectivity profiling on the human adenosine receptors

scientific article

Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor.

scientific article published in June 2015

False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase

scientific article published on 23 July 2008

Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A(2A) receptor with novel biological activity

scientific article

From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action

scientific article published on 26 October 2017

Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time

scientific article published on July 2012

G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: a case for Gnrh, LH, FSH, and GPR54 receptor ligands

scientific article

Indanes--Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors

scientific article published on 27 May 2015

Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors

scientific article published on 18 April 2016

Kinetic Profile of Neuropeptide-Receptor Interactions

scientific article published on 25 October 2016

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time

scientific article

Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1

scientific article published on 24 September 2019

Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor.

scientific article published on 12 February 2016

Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor

scientific article published on 5 September 2014

Pan-cancer in silico analysis of somatic mutations in G-protein coupled receptors: The effect of evolutionary conservation and natural variance

Scintillation proximity assay (SPA) as a new approach to determine a ligand's kinetic profile. A case in point for the adenosine A1 receptor

scientific article

Sodium ion binding pocket mutations and adenosine A2A receptor function.

scientific article published on 3 December 2014

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

scientific article

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms

scientific article published in December 2017

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

scientific article published on 07 December 2016

Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists

scientific article published on 7 November 2017

Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists

scientific article published on 14 August 2017

Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists

scientific article published on 27 September 2013

Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor

scientific article

Surface Ig variable domain glycosylation affects autoantigen binding and acts as threshold for human autoreactive B cell activation

scientific article published on 09 February 2022

Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists

scientific article published in August 2021

Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors

scientific article published on January 2004

Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel

scientific article published on 21 October 2015

Synthesis and evaluation of homo-bivalent GnRHR ligands

scientific article published on 6 May 2007

Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core

scientific article

Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists

scientific article published in February 2015

The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery

scientific article published on 19 August 2016

The Role of Target Binding Kinetics in Drug Discovery

scientific article published on 25 August 2015

The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity

scientific article published on 23 September 2015

The role of a sodium ion binding site in the allosteric modulation of the A(2A) adenosine G protein-coupled receptor

scientific article

When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists

scientific article

Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines

scientific article published on 23 June 2015

[3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor

scientific article published on 7 November 2007

List of works by Laura H Heitman

A covalent antagonist for the human adenosine A2A receptor

A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor

Allosteric Modulation of Kv11.1 (hERG) Channels Protects Against Drug-Induced Ventricular Arrhythmias

Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist

Allosteric modulators of the hERG K(+) channel: radioligand binding assays reveal allosteric characteristics of dofetilide analogs

Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor

Bias in chemokine receptor signalling

Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor

Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring

Cancer-Associated Mutations of the Adenosine A2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions

Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology

Cancer‐related somatic mutations alter adenosine A <sub>1</sub> receptor pharmacology—A focus on mutations in the loops and C‐terminus

Characterization of 12 GnRH peptide agonists - a kinetic perspective

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength

Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations

Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands

Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2.

Drug-target residence time--a case for G protein-coupled receptors

Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics

Equilibrium and kinetic selectivity profiling on the human adenosine receptors

Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor.

False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase

Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A(2A) receptor with novel biological activity

From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action

Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time

G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: a case for Gnrh, LH, FSH, and GPR54 receptor ligands

Indanes--Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors

Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors

Kinetic Profile of Neuropeptide-Receptor Interactions

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time

Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1

Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor.

Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor

Pan-cancer in silico analysis of somatic mutations in G-protein coupled receptors: The effect of evolutionary conservation and natural variance

Scintillation proximity assay (SPA) as a new approach to determine a ligand's kinetic profile. A case in point for the adenosine A1 receptor

Sodium ion binding pocket mutations and adenosine A2A receptor function.

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists

Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists

Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists

Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor

Surface Ig variable domain glycosylation affects autoantigen binding and acts as threshold for human autoreactive B cell activation

Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists

Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors

Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel

Synthesis and evaluation of homo-bivalent GnRHR ligands

Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core

Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists

The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery

The Role of Target Binding Kinetics in Drug Discovery

The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity

The role of a sodium ion binding site in the allosteric modulation of the A(2A) adenosine G protein-coupled receptor

When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists

Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines

[3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor