Lista de obras - Laura H Heitman - Dominio Público Uruguay

A covalent antagonist for the human adenosine A2A receptor

artículo científico publicado en 2016

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

artículo científico publicado en 2009

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

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

Characterization of 12 GnRH peptide agonists - a kinetic perspective

artículo científico publicado en 2015

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

artículo científico publicado en 2016

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

artículo científico publicado en 2021

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

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

artículo científico publicado en 2014

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

artículo científico publicado en 2008

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

artículo científico

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

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

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

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

artículo científico publicado en 2015

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

artículo científico publicado en 2013

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 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

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

artículo científico publicado en 2016

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 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