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List of works by Laura H Heitman

A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies

scientific article published on 26 July 2017

A binding kinetics study of human adenosine A3 receptor agonists.

scientific article

A covalent antagonist for the human adenosine A2A receptor

scientific article published on 3 December 2016

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor

scientific article published on 27 March 2019

A multiple classifier system identifies novel cannabinoid CB2 receptor ligands

scientific article published on 7 November 2019

A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy

scientific article

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

A two-state model for the kinetics of competitive radioligand binding

scientific article published on 27 February 2018

Affinity, binding kinetics and functional characterization of draflazine analogues for human equilibrative nucleoside transporter 1 (SLC29A1)

scientific article published on 10 December 2019

Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines

scientific article published on 3 April 2014

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

An Affinity-Based Probe for the Human Adenosine A Receptor

article

An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters

scientific article published in 2021

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

Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.

scientific article published on 03 January 2017

Characterization of 12 GnRH peptide agonists - a kinetic perspective

scientific article published on 23 September 2015

Characterization of cancer-related somatic mutations in the adenosine A2B receptor

scientific article published on 26 April 2020

Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor.

scientific article published on 29 March 2018

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

scientific article

Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization.

scientific article published in March 2018

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

scientific article published on 24 November 2021

Design and Pharmacological Profile of a Novel Covalent Partial Agonist for the Adenosine A1 Receptor

scientific article published on 09 July 2020

Design, Synthesis and Pharmacological Profile of LUF7746, a Novel Covalent Partial Agonist for the Adenosine A1 Receptor

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

scientific article

Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A Receptor

scientific article published on 28 March 2019

Development of a Cannabinoid-Based Photoaffinity Probe to Determine the Δ8/9-Tetrahydrocannabinol Protein Interaction Landscape in Neuroblastoma Cells.

scientific article published in July 2018

Development of an Affinity-Based Probe to Profile Endogenous Human Adenosine A<sub>3</sub> Receptor Expression

scientific article published on 2 August 2023

Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2.

scientific article published on 13 July 2017

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

scientific article

Discovery of selective luteinizing hormone receptor agonists using the bivalent ligand method.

scientific article published in July 2009

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 expressed and studied in yeast. The adenosine receptor as a prime example

scientific article published on 15 December 2020

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

scientific article

Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition

scientific article published on 8 July 2021

Impact of allosteric modulation: Exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2

scientific article published on 17 July 2018

Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters

scientific article published in 2022

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

scientific article published on 27 May 2015

Intracellular Receptor Modulation: Novel Approach to Target GPCRs.

scientific article published on 10 April 2018

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

Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure-kinetics relationships (SKR) and implications for insurmountable antagonism.

scientific article published in November 2017

LUF7244, an allosteric modulator/activator of Kv 11.1 channels, counteracts dofetilide-induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model

scientific article published on 30 August 2019

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

Label-free technology and patient cells: from early drug development to precision medicine

scientific article published on August 2017

Long residence time adenosine A1 receptor agonists produce sustained wash-resistant antilipolytic effect in rat adipocytes

scientific article published on 21 March 2019

Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients

scientific article

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

Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.

scientific article published on 21 November 2015

Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2.

scientific article published on 22 July 2013

Oncological drug discovery: AI meets structure-based computational research

scientific article published in June 2022

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

Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype

scientific article published on 31 January 2017

Proteochemometric Modeling Identifies Chemically Diverse Norepinephrine Transporter Inhibitors

scientific article published on 16 March 2023

Protocol to Study β-Arrestin Recruitment by CB1 and CB2 Cannabinoid Receptors

scientific article published in January 2016

Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2

scientific article published on 11 October 2018

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

Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells.

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 relationship studies of cannabinoid CB 2 receptor agonists reveal substituent-specific lipophilic effects on residence time

scientific article published on 21 March 2018

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

Structure-kinetics relationships of Capadenoson derivatives as adenosine A 1 receptor agonists

scientific article published on 15 July 2015

Structure–Affinity Relationships (SARs) and Structure–Kinetics Relationships (SKRs) of Kv11.1 Blockers

scientific article published on 17 July 2015

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 Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5

scientific article published on 13 December 2019

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

Targeting the CCL2–CCR2 axis for atheroprotection

scientific article published on 7 March 2022

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

scientific article published on 19 August 2016

The RESOLUTE consortium: unlocking SLC transporters for drug discovery

scientific article published on 07 April 2020

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

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