List of works - J. Robert Lane

4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.

scientific article published in December 2015

A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

scientific article published on 15 November 2011

A Thieno[2,3-d]pyrimidine Scaffold is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor.

scientific article published on 23 April 2018

A kinetic view of GPCR allostery and biased agonism

scientific article published in August 2017

A new mechanism of allostery in a G protein-coupled receptor dimer

scientific article (publication date: September 2014)

A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization

scientific article

A novel nonribose agonist, LUF5834, engages residues that are distinct from those of adenosine-like ligands to activate the adenosine A(2a) receptor.

scientific article

A structure-activity analysis of biased agonism at the dopamine D2 receptor

scientific article published on 8 November 2013

Allosteric approaches to GPCR drug discovery

scientific article published on 01 January 2013

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

scientific article

Allosteric modulation of a chemogenetically modified G protein-coupled receptor.

scientific article published on 29 November 2012

Antibodies that identify only the active conformation of G(i) family G protein alpha subunits.

scientific article

Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation

scientific article published on 17 August 2018

Biased Agonism of Endogenous Opioid Peptides at the μ-Opioid Receptor.

scientific article published on 26 May 2015

Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective.

scientific article published on 05 May 2014

Bridging the gap: bitopic ligands of G-protein-coupled receptors.

scientific article

Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand

scientific article published on 10 August 2015

Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1

scientific article published on 19 December 2018

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors

scientific article published on 2 October 2017

G protein coupling and ligand selectivity of the D2L and D3 dopamine receptors.

scientific article published on 24 January 2008

GRKs as Key Modulators of Opioid Receptor Function

scientific article published on 02 November 2020

Identification of Positive Allosteric Modulators of the D Dopamine Receptor That Act at Diverse Binding Sites

scientific article published on 01 August 2018

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2.

scientific article published on 23 May 2017

Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues.

scientific article

Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

scientific article published on 31 March 2020

Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor ⬇️

scientific article published on April 1, 2012

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor.

scientific article

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole

scientific article published on 05 August 2019

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor.

scientific article published on 17 January 2014

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

scientific article

Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.

scientific article published on 30 June 2016

Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A).

scientific article published on 27 March 2012

Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor.

scientific article published on 18 February 2016

Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior

scientific article published on 14 September 2016

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors

scientific article published on 30 January 2015

Protean agonism at the dopamine D2 receptor: (S)-3-(3-hydroxyphenyl)-N-propylpiperidine is an agonist for activation of Go1 but an antagonist/inverse agonist for Gi1,Gi2, and Gi3.

scientific article published on 7 February 2007

Regulation of G protein-coupled receptors by allosteric ligands

scientific article

Reply to 'Antipsychotics with similar association kinetics at dopamine D receptors differ in extrapyramidal side-effects'

scientific article published in Nature Communications

Sequential Conformational Rearrangements Dictate the Dynamics of Class C GPCR Activation

article

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.

scientific article published on 13 October 2013

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor

scientific article published on 23 October 2019

Structure-activity relationships of privileged structures lead to the discovery of novel biased ligands at the dopamine D₂ receptor.

scientific article published on 30 May 2014

Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor.

scientific article published on 24 June 2015

Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Ac

scientific article published on 02 July 2018

Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).

scientific article published on 10 February 2017

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor.

scientific article

The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors

scientific article published on 16 January 2018

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions

scientific article published on 19 January 2018

The differential actions of clozapine and other antipsychotic drugs on the translocation of dopamine D2 receptors to the cell surface

scientific article published on 22 January 2019

The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor.

scientific article

The role of kinetic context in apparent biased agonism at GPCRs

scientific article published on 24 February 2016

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor

scientific article published on 8 January 2018

The structure of the adenosine receptors: implications for drug discovery.

scientific article published on January 2011

The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion.

scientific article published on 17 November 2015

β2-Adrenoceptors on tumor cells play a critical role in stress-enhanced metastasis in a mouse model of breast cancer.

scientific article published on 16 June 2016

β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.

scientific article

List of works by J. Robert Lane

4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.

A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

A Thieno[2,3-d]pyrimidine Scaffold is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor.

A kinetic view of GPCR allostery and biased agonism

A new mechanism of allostery in a G protein-coupled receptor dimer

A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization

A novel nonribose agonist, LUF5834, engages residues that are distinct from those of adenosine-like ligands to activate the adenosine A(2a) receptor.

A structure-activity analysis of biased agonism at the dopamine D2 receptor

Allosteric approaches to GPCR drug discovery

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

Allosteric modulation of a chemogenetically modified G protein-coupled receptor.

Antibodies that identify only the active conformation of G(i) family G protein alpha subunits.

Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation

Biased Agonism of Endogenous Opioid Peptides at the μ-Opioid Receptor.

Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective.

Bridging the gap: bitopic ligands of G-protein-coupled receptors.

Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand

Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors

G protein coupling and ligand selectivity of the D2L and D3 dopamine receptors.

GRKs as Key Modulators of Opioid Receptor Function

Identification of Positive Allosteric Modulators of the D Dopamine Receptor That Act at Diverse Binding Sites

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2.

Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues.

Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor ⬇️

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor.

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor.

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.

Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A).

Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor.

Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors

Protean agonism at the dopamine D2 receptor: (S)-3-(3-hydroxyphenyl)-N-propylpiperidine is an agonist for activation of Go1 but an antagonist/inverse agonist for Gi1,Gi2, and Gi3.

Regulation of G protein-coupled receptors by allosteric ligands

Reply to 'Antipsychotics with similar association kinetics at dopamine D receptors differ in extrapyramidal side-effects'

Sequential Conformational Rearrangements Dictate the Dynamics of Class C GPCR Activation

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor

Structure-activity relationships of privileged structures lead to the discovery of novel biased ligands at the dopamine D₂ receptor.

Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor.

Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Ac

Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor.

The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions

The differential actions of clozapine and other antipsychotic drugs on the translocation of dopamine D2 receptors to the cell surface

The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor.

The role of kinetic context in apparent biased agonism at GPCRs

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor

The structure of the adenosine receptors: implications for drug discovery.

The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion.

β2-Adrenoceptors on tumor cells play a critical role in stress-enhanced metastasis in a mouse model of breast cancer.

β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.