List of works - Peter J. Scammells

2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers

scientific article published on 28 November 2005

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

scientific article published in December 2015

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

scientific article published on 28 December 2018

7-Selenabicyclo[2.2.1]heptane

scientific article published on 06 August 2012

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

scientific article published on 15 November 2011

A Novel Class of N-Sulfonyl and N-Sulfamoyl Noscapine Derivatives that Promote Mitotic Arrest in Cancer Cells

scientific article published on 12 November 2019

A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists

scientific article published on 15 February 2018

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 critical evaluation of pyrrolo[2,3-d]pyrimidine-4-amines as Plasmodium falciparum apical membrane antigen 1 (AMA1) inhibitors

article

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

scientific article (publication date: September 2014)

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

scientific article published on 8 November 2013

Adenosine receptor ligands with oxygenated N6-substituents

scientific article published on 01 April 1999

Alternating iodonium-mediated reaction cascades giving indole- and quinoline-containing polycycles

scientific article published on 24 April 2008

An allosteric modulator of the adenosine A1 receptor improves cardiac function following ischaemia in murine isolated hearts.

scientific article published on 12 April 2013

An expedient synthesis of N6-substituted-5'-modified adenosines

scientific article published on 21 June 2006

An improved synthesis of 5'-fluoro-5'-deoxyadenosines.

scientific article published in July 2005

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors

scientific article published on 24 April 2018

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

scientific article published on 05 May 2014

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics

scientific article

Design strategies for bivalent ligands targeting GPCRs

scientific article

Design, Synthesis, and Biological Evaluation of Tetra-Substituted Thiophenes as Inhibitors of p38α MAPK.

scientific article

Determination of psilocin and psilocybin using flow injection analysis with acidic potassium permanganate and tris(2,2'-bipyridyl)ruthenium(II) chemiluminescence detection respectively.

scientific article

Development of Inhibitors of Plasmodium falciparum Apical Membrane Antigen 1 Based on Fragment Screening

article

Development of a photoactivatable allosteric ligand for the m1 muscarinic acetylcholine receptor

scientific article published on 9 September 2014

Differential A(1)-adenosine receptor reserve for inhibition of cyclic AMP accumulation and G-protein activation in DDT(1) MF-2 cells

scientific article published in July 2000

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

Effect of linker length and composition on heterobivalent ligand-mediated receptor cross-talk between the A1 adenosine and β2 adrenergic receptors

scientific article published on 18 September 2013

Efficient N-demethylation of opiate alkaloids using a modified nonclassical Polonovski reaction.

scientific article

Electrochemical surface-enhanced Raman spectroscopy (E-SERS) of novel biodegradable ionic liquids

scientific article published in November 2013

Enhancing the Oral Absorption of Kinase Inhibitors Using Lipophilic Salts and Lipid Based Formulations

scientific article published on 13 November 2018

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

scientific article published in January 2018

Further investigation of the N-demethylation of tertiary amine alkaloids using the non-classical Polonovski reaction

scientific article published on 24 March 2006

Further investigations into the N-demethylation of oripavine using iron and stainless steel

scientific article published on 24 December 2010

Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases

scientific article published on 04 January 2019

Identification of the Binding Site of Apical Membrane Antigen 1 (AMA1) Inhibitors Using a Paramagnetic Probe

scientific article published on 13 February 2019

Inter- and intramolecular C-H...pi interactions in morphine bis(1-naphthoate).

scientific article published on 9 August 2003

Investigation of novel ropinirole analogues: synthesis, pharmacological evaluation and computational analysis of dopamine D2 receptor functionalized congeners and homobivalent ligands

scholarly article by Manuela Jörg et al published 2014 in MedChemComm

Ionic Liquid Forms of Weakly Acidic Drugs in Oral Lipid Formulations: Preparation, Characterization, in Vitro Digestion, and in Vivo Absorption Studies.

scientific article published on 27 September 2017

Ionic liquids provide unique opportunities for oral drug delivery: structure optimization and in vivo evidence of utility

scientific article published on 01 February 2014

Ligand-induced conformational change of Plasmodium falciparum AMA1 detected using 19F NMR.

scientific article published on 5 August 2014

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 mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

scientific article

N-demethylation of N-methyl alkaloids with ferrocene.

scientific article published on 10 June 2010

N6-(5,6-epoxynorbornyl)adenosine analogs as A1 adenosine agonists

scientific article published on 01 December 1998

NMR case study of ropinirole: concentration-dependent effects of nonexchangeable proton resonances

scientific article published on 07 August 2014

New irreversible adenosine A(1) antagonists based on FSCPX.

scientific article published in November 2002

New potent and selective A1 adenosine receptor agonists.

scientific article published in September 2004

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

scientific article published on 18 February 2016

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions

scientific article published on 18 July 2019

Novel Irreversible Agonists Acting at the A1 Adenosine Receptor

scientific article

Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space

scientific article published on 2 April 2013

Overcoming P-Glycoprotein-Mediated Drug Resistance with Noscapine Derivatives

scientific article published on 26 November 2018

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

Positive allosteric mechanisms of adenosine A<sub>1</sub> receptor-mediated analgesia

scientific article published on 08 September 2021

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions

scientific article

Probe dependence of allosteric enhancers on the binding affinity of adenosine A -receptor agonists at rat and human A -receptors measured using NanoBRET

scientific article published on 06 March 2019

Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents.

scientific article

Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.

scientific article published on 16 January 2015

Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.

scientific article

Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

scientific article published on 28 September 2016

Screening the Medicines for Malaria Venture "Malaria Box" against the Plasmodium falciparum aminopeptidases, M1, M17 and M18.

scientific article published on 20 February 2015

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

scientific article published on 11 March 2014

Solution NMR characterization of apical membrane antigen 1 and small molecule interactions as a basis for designing new antimalarials

scientific article published on 24 January 2016

Structure and dynamics of apical membrane antigen 1 from Plasmodium falciparum FVO

scientific article

Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum

scientific article

Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity

scientific article published in February 2017

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

scientific article published on 23 October 2019

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

Structure-based optimization and biological evaluation of human 20α-hydroxysteroid dehydrogenase (AKR1C1) salicylic acid-based inhibitors.

scientific article published on 17 September 2010

Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1).

scientific article published in May 2009

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

Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor

scientific article published on 09 January 2020

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles

scientific article published on 23 March 2018

Synthesis and Pharmacological Evaluation of Noscapine-Inspired 5-Substituted Tetrahydroisoquinolines as Cytotoxic Agents

scientific article published on 14 September 2018

Synthesis and biological evaluation of N-substituted noscapine analogues

scientific article

Synthesis and biological evaluation of adenosines with heterobicyclic and polycyclic N(6)-substituents as adenosine A(1) receptor agonists.

scientific article

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor.

scientific article published on 17 February 2012

Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists.

scientific article published on 27 March 2010

Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.

scientific article published on 5 June 2014

Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease

scientific article published on 24 December 2014

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.

scientific article published on 17 June 2013

Synthesis and structure-activity relationships of phosphonic arginine mimetics as inhibitors of the M1 and M17 aminopeptidases from Plasmodium falciparum

scientific article

Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.

scientific article

Synthesis, molecular structure, NMR spectroscopic and computational analysis of a selective adenosine A2A antagonist, ZM 241385

article published in 2012

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 dopamine D2 and adenosine A2A receptors: past, present and future trends for the treatment of Parkinson's disease

scientific article published on January 2014

The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling

scientific article published on 9 August 2016

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 synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor.

scientific article published on 4 May 2011

The synthesis and biological evaluation of multifunctionalised derivatives of noscapine as cytotoxic agents

scientific article published on 11 December 2013

Transformation of Biopharmaceutical Classification System Class I and III Drugs Into Ionic Liquids and Lipophilic Salts for Enhanced Developability Using Lipid Formulations.

scientific article

Transformation of poorly water-soluble drugs into lipophilic ionic liquids enhances oral drug exposure from lipid based formulations

scientific article

Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors

scientific article

VCP746, a novel A1 adenosine receptor biased agonist, reduces hypertrophy in a rat neonatal cardiac myocyte model.

scientific article published on 5 July 2016

Virtual screening using a conformationally flexible target protein: models for ligand binding to p38α MAPK ⬇️

scientific article published on April 20, 2012

XH-14 analogues as adenosine antagonists ⬇️

scientific article published on September 1, 1998

List of works by Peter J. Scammells

2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers

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

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

7-Selenabicyclo[2.2.1]heptane

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

A Novel Class of N-Sulfonyl and N-Sulfamoyl Noscapine Derivatives that Promote Mitotic Arrest in Cancer Cells

A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists

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

A critical evaluation of pyrrolo[2,3-d]pyrimidine-4-amines as Plasmodium falciparum apical membrane antigen 1 (AMA1) inhibitors

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

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

Adenosine receptor ligands with oxygenated N6-substituents

Alternating iodonium-mediated reaction cascades giving indole- and quinoline-containing polycycles

An allosteric modulator of the adenosine A1 receptor improves cardiac function following ischaemia in murine isolated hearts.

An expedient synthesis of N6-substituted-5'-modified adenosines

An improved synthesis of 5'-fluoro-5'-deoxyadenosines.

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors

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

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics

Design strategies for bivalent ligands targeting GPCRs

Design, Synthesis, and Biological Evaluation of Tetra-Substituted Thiophenes as Inhibitors of p38α MAPK.

Determination of psilocin and psilocybin using flow injection analysis with acidic potassium permanganate and tris(2,2'-bipyridyl)ruthenium(II) chemiluminescence detection respectively.

Development of Inhibitors of Plasmodium falciparum Apical Membrane Antigen 1 Based on Fragment Screening

Development of a photoactivatable allosteric ligand for the m1 muscarinic acetylcholine receptor

Differential A(1)-adenosine receptor reserve for inhibition of cyclic AMP accumulation and G-protein activation in DDT(1) MF-2 cells

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

Effect of linker length and composition on heterobivalent ligand-mediated receptor cross-talk between the A1 adenosine and β2 adrenergic receptors

Efficient N-demethylation of opiate alkaloids using a modified nonclassical Polonovski reaction.

Electrochemical surface-enhanced Raman spectroscopy (E-SERS) of novel biodegradable ionic liquids

Enhancing the Oral Absorption of Kinase Inhibitors Using Lipophilic Salts and Lipid Based Formulations

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

Further investigation of the N-demethylation of tertiary amine alkaloids using the non-classical Polonovski reaction

Further investigations into the N-demethylation of oripavine using iron and stainless steel

Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases

Identification of the Binding Site of Apical Membrane Antigen 1 (AMA1) Inhibitors Using a Paramagnetic Probe

Inter- and intramolecular C-H...pi interactions in morphine bis(1-naphthoate).

Investigation of novel ropinirole analogues: synthesis, pharmacological evaluation and computational analysis of dopamine D2 receptor functionalized congeners and homobivalent ligands

Ionic Liquid Forms of Weakly Acidic Drugs in Oral Lipid Formulations: Preparation, Characterization, in Vitro Digestion, and in Vivo Absorption Studies.

Ionic liquids provide unique opportunities for oral drug delivery: structure optimization and in vivo evidence of utility

Ligand-induced conformational change of Plasmodium falciparum AMA1 detected using 19F NMR.

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

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole

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

N-demethylation of N-methyl alkaloids with ferrocene.

N6-(5,6-epoxynorbornyl)adenosine analogs as A1 adenosine agonists

NMR case study of ropinirole: concentration-dependent effects of nonexchangeable proton resonances

New irreversible adenosine A(1) antagonists based on FSCPX.

New potent and selective A1 adenosine receptor agonists.

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

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions

Novel Irreversible Agonists Acting at the A1 Adenosine Receptor

Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space

Overcoming P-Glycoprotein-Mediated Drug Resistance with Noscapine Derivatives

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

Positive allosteric mechanisms of adenosine A<sub>1</sub> receptor-mediated analgesia

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions

Probe dependence of allosteric enhancers on the binding affinity of adenosine A -receptor agonists at rat and human A -receptors measured using NanoBRET

Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents.

Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.

Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.

Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Screening the Medicines for Malaria Venture "Malaria Box" against the Plasmodium falciparum aminopeptidases, M1, M17 and M18.

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

Solution NMR characterization of apical membrane antigen 1 and small molecule interactions as a basis for designing new antimalarials

Structure and dynamics of apical membrane antigen 1 from Plasmodium falciparum FVO

Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum

Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity

Structure-Kinetic Profiling of Haloperidol Analogues at the Human 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.

Structure-based optimization and biological evaluation of human 20α-hydroxysteroid dehydrogenase (AKR1C1) salicylic acid-based inhibitors.

Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1).

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

Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles

Synthesis and Pharmacological Evaluation of Noscapine-Inspired 5-Substituted Tetrahydroisoquinolines as Cytotoxic Agents

Synthesis and biological evaluation of N-substituted noscapine analogues

Synthesis and biological evaluation of adenosines with heterobicyclic and polycyclic N(6)-substituents as adenosine A(1) receptor agonists.

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor.

Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists.