Lista de obras - Laura H Heitman - Dominio Público Uruguay

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

artículo científico publicado en 2017

A binding kinetics study of human adenosine A3 receptor agonists.

artículo científico publicado en 2018

A covalent antagonist for the human adenosine A2A receptor

artículo científico publicado en 2016

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

artículo científico publicado en 2019

A multiple classifier system identifies novel cannabinoid CB2 receptor ligands

artículo científico publicado en 2019

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

artículo científico publicado en 2017

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

artículo científico publicado en 2009

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

artículo científico publicado en 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

artículo científico publicado en 2014

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

artículo científico publicado en 2016

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

artículo científico publicado en 2006

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

artículo científico publicado en 2013

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

artículo científico publicado en 2008

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

artículo científico publicado en 2021

Bias in chemokine receptor signalling

artículo científico

Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor

artículo científico publicado en 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

artículo científico publicado en 2022

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

artículo científico publicado en 2022

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

artículo científico publicado en 2022

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

artículo científico publicado en 2017

Characterization of 12 GnRH peptide agonists - a kinetic perspective

artículo científico publicado en 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.

artículo científico publicado en 2018

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

artículo científico publicado en 2016

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

artículo científico publicado en 2018

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

artículo científico publicado en 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

artículo científico publicado en 2012

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

artículo científico publicado en 2019

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

artículo científico publicado en 2018

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

artículo científico publicado en 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.

artículo científico publicado en 2017

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

artículo científico publicado en 2014

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

artículo científico publicado en 2009

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

artículo científico publicado en 2014

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

artículo científico publicado en 2012

Equilibrium and kinetic selectivity profiling on the human adenosine receptors

artículo científico publicado en 2016

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

artículo científico publicado en 2015

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

artículo científico publicado en 2008

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

artículo científico publicado en 2012

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

artículo científico publicado en 2017

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

artículo científico publicado en 2012

G protein-coupled receptors expressed and studied in yeast. The adenosine receptor as a prime example

artículo científico publicado en 2020

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

artículo científico publicado en 2008

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

artículo científico publicado en 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

artículo científico publicado en 2022

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

artículo científico

Intracellular Receptor Modulation: Novel Approach to Target GPCRs.

artículo científico publicado en 2018

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

artículo científico publicado en 2016

Kinetic Profile of Neuropeptide-Receptor Interactions

artículo científico publicado en 2016

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

artículo científico publicado en 2017

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

artículo científico publicado en 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

artículo científico publicado en 2019

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

artículo científico

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

artículo científico publicado en 2019

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

artículo científico publicado en 2015

Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor

artículo científico publicado en 2016

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

artículo científico publicado en 2014

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

artículo científico publicado en 2015

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

artículo científico publicado en 2013

Oncological drug discovery: AI meets structure-based computational research

artículo científico publicado en 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

artículo científico publicado en 2017

Proteochemometric Modeling Identifies Chemically Diverse Norepinephrine Transporter Inhibitors

artículo científico publicado en 2023

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

artículo científico publicado en 2016

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

artículo científico publicado en 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

artículo científico publicado en 2015

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

artículo científico publicado en 2018

Sodium ion binding pocket mutations and adenosine A2A receptor function.

artículo científico publicado en 2014

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

artículo científico publicado en 2012

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

artículo científico publicado en 2017

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

artículo científico publicado en 2016

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

artículo científico publicado en 2017

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

artículo científico publicado en 2017

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

artículo científico publicado en 2018

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

artículo científico publicado en 2013

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

artículo científico publicado en 2015

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

artículo científico publicado en 2015

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

artículo científico publicado en 2009

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

artículo científico publicado en 2022

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

artículo científico publicado en 2019

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

artículo científico publicado en 2021

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

artículo científico publicado en 2004

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

artículo científico publicado en 2015

Synthesis and evaluation of homo-bivalent GnRHR ligands

artículo científico publicado en 2007

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

artículo científico publicado en 2008

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

artículo científico publicado en 2015

Targeting the CCL2–CCR2 axis for atheroprotection

artículo científico publicado en 2022

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

artículo científico publicado en 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

artículo científico publicado en 2015

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

artículo científico publicado en 2015

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

artículo científico publicado en 2013

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

artículo científico publicado en 2015

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

artículo científico publicado en 2015

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

artículo científico publicado en 2007

Lista de obras de Laura H Heitman

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

A binding kinetics study of human adenosine A3 receptor agonists.

A covalent antagonist for the human adenosine A2A receptor

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

A multiple classifier system identifies novel cannabinoid CB2 receptor ligands

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

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

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

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

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

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

An Affinity-Based Probe for the Human Adenosine A Receptor

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

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

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

Characterization of 12 GnRH peptide agonists - a kinetic perspective

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Intracellular Receptor Modulation: Novel Approach to Target GPCRs.

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

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

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

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

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

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

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

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

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

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

Oncological drug discovery: AI meets structure-based computational research

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

Proteochemometric Modeling Identifies Chemically Diverse Norepinephrine Transporter Inhibitors

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

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

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

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

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