List of works - Barrie Kellam

5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.

scientific article published on 25 September 2013

A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-A3 Receptor in Living Cells

scientific article published on 13 December 2017

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

Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes

scientific article

Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells.

scientific article

Alkylation of Staurosporine to Derive a Kinase Probe for Fluorescence Applications.

scientific article published on 23 March 2016

Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization

scientific article published on March 2014

Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery

scientific article published on 3 October 2015

Biosynthesis of carbapenem antibiotics: new carbapenam substrates for carbapenem synthase (CarC).

scientific article

CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans

scientific article published in 2024

Cell-type-specific adhesion onto polymer surfaces from mixed cell populations.

scientific article

Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.

scientific article published in August 2005

Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers.

scientific article published in September 2013

Correction to Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

scientific article published on 24 April 2018

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ)

scientific article published on 27 January 2017

Design and use of fluorescent ligands to study ligand-receptor interactions in single living cells

scientific article published in January 2011

Developing a self-healing supramolecular nucleoside hydrogel.

scientific article

Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells

scientific article

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist.

scientific article published on 30 April 2015

Drug-like Antagonists of P2Y Receptors-From Lead Identification to Drug Development

scientific article

Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization

scientific article published on August 2014

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

scientific article published in January 2018

Fluorophore-tagged GPCR ligands.

scientific article

GPCRs through the keyhole: the role of protein flexibility in ligand binding to β-adrenoceptors.

scientific article published on 17 August 2016

Gelation properties of self-assembling N-acyl modified cytidine derivatives

scientific article published on 29 October 2014

Highly potent and selective fluorescent antagonists of the human adenosine A₃ receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold.

scientific article published on 13 February 2012

Identification of a novel toxicophore in anti-cancer chemotherapeutics that targets mitochondrial respiratory complex I

scientific article published on 20 May 2020

Immunosuppressive but non-LasR-inducing analogues of the Pseudomonas aeruginosa quorum-sensing molecule N-(3-oxododecanoyl)-l-homoserine lactone

scientific article published on 13 April 2011

Insights into low molecular mass organic gelators: a focus on drug delivery and tissue engineering applications

scientific article published on January 2014

Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism

scientific article published on 26 June 2014

Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells

scientific article published on 27 November 2020

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

New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.

scientific article published on 24 January 2007

Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease.

scientific article published on 11 April 2017

Nucleoside Based Self-Assembling Drugs for Localized Drug Delivery

scientific article published on 23 March 2018

Overcoming challenges in developing small molecule inhibitors for GPVI and CLEC-2

scientific article published on 07 January 2021

Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate

scientific article published on 19 November 2014

Recent progress in the design of selectin inhibitors

scientific article published on November 2003

Self-Assembling Benzothiazole-Based Gelators: A Mechanistic Understanding of in Vitro Bioactivation and Gelation.

scientific article published on 5 March 2018

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

scientific article published on 23 October 2019

Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2‐adrenoceptor in CRISPR/Cas9 genome‐edited HEK293T cells at low expression levels

scientific article published on 18 May 2021

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

scientific article published on 09 January 2020

Surface engineering of living myoblasts via selective periodate oxidation.

scientific article published on March 2003

Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

scientific article published on 20 March 2018

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.

scientific article published on 16 September 2011

Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.

scientific article published on 10 May 2013

Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold

scientific article published on 13 January 2015

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

scientific article

The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs

scientific article

List of works by Barrie Kellam

5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.

A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-A3 Receptor in Living Cells

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

Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes

Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells.

Alkylation of Staurosporine to Derive a Kinase Probe for Fluorescence Applications.

Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization

Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery

Biosynthesis of carbapenem antibiotics: new carbapenam substrates for carbapenem synthase (CarC).

CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans

Cell-type-specific adhesion onto polymer surfaces from mixed cell populations.

Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.

Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers.

Correction to Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ)

Design and use of fluorescent ligands to study ligand-receptor interactions in single living cells

Developing a self-healing supramolecular nucleoside hydrogel.

Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist.

Drug-like Antagonists of P2Y Receptors-From Lead Identification to Drug Development

Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

Fluorophore-tagged GPCR ligands.

GPCRs through the keyhole: the role of protein flexibility in ligand binding to β-adrenoceptors.

Gelation properties of self-assembling N-acyl modified cytidine derivatives

Highly potent and selective fluorescent antagonists of the human adenosine A₃ receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold.

Identification of a novel toxicophore in anti-cancer chemotherapeutics that targets mitochondrial respiratory complex I

Immunosuppressive but non-LasR-inducing analogues of the Pseudomonas aeruginosa quorum-sensing molecule N-(3-oxododecanoyl)-l-homoserine lactone

Insights into low molecular mass organic gelators: a focus on drug delivery and tissue engineering applications

Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism

Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells

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

New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.

Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease.

Nucleoside Based Self-Assembling Drugs for Localized Drug Delivery

Overcoming challenges in developing small molecule inhibitors for GPVI and CLEC-2

Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate

Recent progress in the design of selectin inhibitors

Self-Assembling Benzothiazole-Based Gelators: A Mechanistic Understanding of in Vitro Bioactivation and Gelation.

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

Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2‐adrenoceptor in CRISPR/Cas9 genome‐edited HEK293T cells at low expression levels

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

Surface engineering of living myoblasts via selective periodate oxidation.

Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.

Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.

Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold

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

The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs