List of works - Philip E. Thompson

(+)-Fluorenylethylchloroformate (FLEC)--improved synthesis for application in chiral analysis and peptidomimetic synthesis

scientific article published in April 2013

A Novel Chemical Biology Approach for Mapping of Polymyxin Lipopeptide Antibody Binding Epitopes

scientific article published on 29 March 2016

A Novel Serpin Regulatory Mechanism: SerpinB9 IS REVERSIBLY INHIBITED BY VICINAL DISULFIDE BOND FORMATION IN THE REACTIVE CENTER LOOP

scientific article published on 15 December 2015

A facile, click chemistry-based approach to assembling fluorescent chemosensors for protein tyrosine kinases

scientific article published on 5 November 2010

A potent cyclic peptide targeting SPSB2 protein as a potential anti-infective agent

scientific article published on 06 August 2014

A reversed-phase HPLC-based method for the assay of cyclic nucleotide phosphodiesterase activity

scientific article published on 01 April 2005

A secondary mode of action of polymyxins against Gram-negative bacteria involves the inhibition of NADH-quinone oxidoreductase activity

scientific article published on 30 October 2013

A simple and inexpensive sample-handling method for the semi-preparative RP-HPLC of polypeptides and non-polar peptide derivatives: pre-adsorption of samples

scientific article published on 01 June 1995

A synthetic lipopeptide targeting top-priority multidrug-resistant Gram-negative pathogens

scientific article published on 25 March 2022

Active site similarity between human and Plasmodium falciparum phosphodiesterases: considerations for antimalarial drug design

scientific article published on 16 July 2011

Analysis of anti-PDE3 activity of 2-morpholinochromone derivatives reveals multiple mechanisms of anti-platelet activity.

scientific article

Antimicrobial Activity and Toxicity of the Major Lipopeptide Components of Polymyxin B and Colistin: Last-line Antibiotics against Multidrug-Resistant Gram-negative Bacteria

scientific article published on 04 September 2015

Application of a Sulfoxonium Ylide Electrophile to Generate Cathepsin X-Selective Activity-Based Probes

scientific article published on 14 February 2020

Beta amino acid-modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity.

scientific article published in June 2016

Carbohydrate-mimetic peptides: structural aspects of mimicry and therapeutic implications.

scientific article published on February 2011

Cellular Uptake and Localization of Polymyxins in Renal Tubular Cells Using Rationally Designed Fluorescent Probes

scientific article

Characterization of epitope regions of thyrotropin β-subunit recognized by the monoclonal antibodies mAb279 and mAb299: a chimeric peptide approach

scientific article published on 01 September 1999

Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.

scientific article published on 24 September 2014

Cleavage and activation of proteinase-activated receptor-2 on human neutrophils by gingipain-R from Porphyromonas gingivalis

article

Conformational studies on (+)-anatoxin-a and derivatives

scientific article published on June 1992

Controlled Construction of Cyclic d / l Peptide Nanorods

scientific article published on 05 December 2018

Cyclic Hexapeptide Mimics of the LEDGF Integrase Recognition Loop in Complex with HIV-1 Integrase

article

Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors using in vitro mutagenesis of non-conserved amino acids and kinetic analysis

scientific article

Design and Evaluation of Novel Polymyxin Fluorescent Probes

scientific article published on 11 November 2017

Design, Synthesis, and Characterization of Cyclic Peptidomimetics of the Inducible Nitric Oxide Synthase Binding Epitope That Disrupt the Protein-Protein Interaction Involving SPRY Domain-Containing Suppressor of Cytokine Signaling Box Protein (SPSB

scientific article published on 23 May 2016

Design, synthesis, and evaluation of a new fluorescent probe for measuring polymyxin-lipopolysaccharide binding interactions

scientific article

Development of cognitive enhancers based on inhibition of insulin-regulated aminopeptidase

scientific article

Development of single and mixed isoform selectivity PI3Kδ inhibitors by targeting Asn836 of PI3Kδ.

scientific article published on 11 August 2016

Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).

scientific article

Disrupting the platelet internal membrane via PI3KC2α inhibition impairs thrombosis independently of canonical platelet activation

scientific article published on 01 July 2020

Dissecting isoform selectivity of PI3K inhibitors: the role of non-conserved residues in the catalytic pocket

scientific article published on September 2008

Evidence for the activation of PAR-2 by the sperm protease, acrosin: expression of the receptor on oocytes

scientific article published in November 2000

Functional Characterization of the Unique Terminal Thioesterase Domain from Polymyxin Synthetase.

scientific article published on 10 January 2017

IP3-4 kinase Arg1 regulates cell wall homeostasis and surface architecture to promote clearance of Cryptococcus neoformans infection in a mouse model.

scientific article published on 4 October 2017

Identification and development of specific inhibitors for insulin-regulated aminopeptidase as a new class of cognitive enhancers

scientific article

Identification of a Cyanine-Dye Labeled Peptidic Ligand for Y1R and Y4R, Based upon the Neuropeptide Y C-Terminal Analogue, BVD-15.

scientific article published on 11 August 2016

Identification of a unique filamin A binding region within the cytoplasmic domain of glycoprotein Ibalpha.

scientific article published on May 2005

Identification of potent phosphodiesterase inhibitors that demonstrate cyclic nucleotide-dependent functions in apicomplexan parasites.

scientific article published on 4 February 2015

Identification of preferred carbohydrate binding modes in xenoreactive antibodies by combining conformational filters and binding site maps

scientific article published on 22 February 2010

Imaging the distribution of polymyxins in the kidney

scientific article

Importance of the P4' residue in human granzyme B inhibitors and substrates revealed by scanning mutagenesis of the proteinase inhibitor 9 reactive center loop

scientific article

In silico analysis of antibody-carbohydrate interactions and its application to xenoreactive antibodies

scientific article published on 14 October 2009

Inflammatory twins from PI3K gang brought to justice?

scientific article published in February 2010

Investigating the Interaction of Octapeptin A3 with Model Bacterial Membranes

scientific article

Isoform-selective inhibition of phosphoinositide 3-kinase: identification of a new region of nonconserved amino acids critical for p110α inhibition

scientific article

Measuring polymyxin uptake by renal tubular cells: is BODIPY-polymyxin B an appropriate probe?

scientific article published on October 2014

Mechanisms of PI3Kβ-selective inhibition revealed by reciprocal mutagenesis.

scientific article

Methionine Ameliorates Polymyxin-Induced Nephrotoxicity by Attenuating Cellular Oxidative Stress.

scientific article published on 23 October 2017

Molecular basis for the increased polymyxin susceptibility of Klebsiella pneumoniae strains with under-acylated lipid A.

scientific article

Molecular determinants of the substrate specificity of the complement-initiating protease, C1r.

scientific article

Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y4 Receptor Agonist Derived by an Olefin Metathesis Approach.

scientific article published on 13 June 2016

PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues

scientific article

PI 3-kinase p110beta: a new target for antithrombotic therapy

scientific journal article

Parallel and antiparallel cyclic d/l peptide nanotubes.

scientific article

Peptide inhibitors of xenoreactive antibodies mimic the interaction profile of the native carbohydrate antigens

scientific article published on 01 January 2011

Pharmacokinetics of the Individual Major Components of Polymyxin B and Colistin in Rats.

scientific article published on 12 January 2017

Pharmacology of polymyxins: new insights into an 'old' class of antibiotics

scientific article

Phenylalanine-544 plays a key role in substrate and inhibitor binding by providing a hydrophobic packing point at the active site of insulin-regulated aminopeptidase

scientific article published on 13 July 2010

Polymyxins and analogues bind to ribosomal RNA and interfere with eukaryotic translation in vitro.

scientific article published on 18 September 2013

Polymyxins: a new hope in combating Gram-negative superbugs?

scientific article published on 21 June 2016

Potent inhibitors of phosphatidylinositol 3 (PI3) kinase that have antiproliferative activity only when delivered as prodrug forms.

scientific article published on 8 April 2013

Probing the penetration of antimicrobial polymyxin lipopeptides into gram-negative bacteria

scientific article

Quantitation of Polymyxin-Lipopolysaccharide Interactions Using an Image-Based Fluorescent Probe.

scientific article published on 09 January 2016

Re-discovering PDE3 inhibitors--new opportunities for a long neglected target.

scientific article published on January 2007

Redox-stable cyclic peptide inhibitors of the SPSB2-iNOS interaction

scientific article

Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase

scientific article published in December 2012

RhoA sustains integrin alpha IIbbeta 3 adhesion contacts under high shear.

scientific article published on 5 February 2002

Significant accumulation of polymyxin in single renal tubular cells: a medicinal chemistry and triple correlative microscopy approach

scientific article

Solid-Phase synthesis of a dendritic peptide related to a retinoblastoma protein fragment utilizing a combined boc- and fmoc-chemistry approach

scientific article

Solid-phase synthesis of cyclic analogues related to the hypoglycaemic peptide hGH(6-13): comparison of two i-->i + 4 lactam cyclization procedures

scientific article published in October 2001

Structural Determinants of Isoform Selectivity in PI3K Inhibitors

scientific article published on 26 February 2019

Structural and biochemical characterization of the oxidoreductase NmDsbA3 from Neisseria meningitidis

scientific article

Structural basis of nSH2 regulation and lipid binding in PI3Kα.

scientific article

Structure of granzyme C reveals an unusual mechanism of protease autoinhibition

scientific article

Structure, Function, and Biosynthetic Origin of Octapeptin Antibiotics Active against Extensively Drug-Resistant Gram-Negative Bacteria.

scientific article published on 23 January 2018

Structure--activity relationships of polymyxin antibiotics

scientific article

Structure-Activity Studies of β-Hairpin Peptide Inhibitors of the Plasmodium falciparum AMA1-RON2 Interaction

scientific article

Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate

scientific article published on 29 September 2012

Structure-activity relationships for the binding of polymyxins with human α-1-acid glycoprotein

scientific article

Synthesis and Pharmacological Evaluation of 4-Iminothiazolidinones for Inhibition of PI3 Kinase

scientific article published on January 2012

Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity.

scientific article published on 5 October 2016

Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.

scientific article published on 27 January 2016

Synthesis, structure-activity relationships and brain uptake of a novel series of benzopyran inhibitors of insulin-regulated aminopeptidase.

scientific article published on 7 February 2014

Synthetic routes to the Neuropeptide Y Y1 receptor antagonist 1229U91 and related analogues for SAR studies and cell-based imaging.

scientific article published on 14 April 2014

Teaching 'old' polymyxins new tricks: new-generation lipopeptides targeting gram-negative 'superbugs'.

scientific article

The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

scientific article

The Structure of the Bacterial Oxidoreductase Enzyme DsbA in Complex with a Peptide Reveals a Basis for Substrate Specificity in the Catalytic Cycle of DsbA Enzymes

scientific article

The drug vehicle and solvent N-methylpyrrolidone is an immunomodulator and antimyeloma compound

scientific article

The effects of exosite occupancy on the substrate specificity of thrombin

scientific article published on 26 July 2009

The first total synthesis and solution structure of a polypeptin, PE2, a cyclic lipopeptide with broad spectrum antibiotic activity.

scientific article published in August 2017

The major human and mouse granzymes are structurally and functionally divergent

scientific article

The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.

scientific article

The phytosulfokine (PSK) receptor is capable of guanylate cyclase activity and enabling cyclic GMP-dependent signaling in plants

scientific article

The use of tripeptides for lead discovery of 5-HT4 receptor ligands.

scientific article published in January 2009

Thiazolidinedione-based PI3Kα inhibitors: an analysis of biochemical and virtual screening methods

scientific article

Thiophene inhibitors of PDE4: crystal structures show a second binding mode at the catalytic domain of PDE4D2

scientific article

Transcriptomic Analysis of the Activity of a Novel Polymyxin against Staphylococcus aureus

scientific article published on 27 July 2016

Tropane-based amino acids for peptide structure-function studies: inhibitors of platelet aggregation

scientific article published on 01 October 1998

Use of Kv1.3 blockers for inflammatory skin conditions.

scientific article published in January 2010

List of works by Philip E. Thompson

(+)-Fluorenylethylchloroformate (FLEC)--improved synthesis for application in chiral analysis and peptidomimetic synthesis

A Novel Chemical Biology Approach for Mapping of Polymyxin Lipopeptide Antibody Binding Epitopes

A Novel Serpin Regulatory Mechanism: SerpinB9 IS REVERSIBLY INHIBITED BY VICINAL DISULFIDE BOND FORMATION IN THE REACTIVE CENTER LOOP

A facile, click chemistry-based approach to assembling fluorescent chemosensors for protein tyrosine kinases

A potent cyclic peptide targeting SPSB2 protein as a potential anti-infective agent

A reversed-phase HPLC-based method for the assay of cyclic nucleotide phosphodiesterase activity

A secondary mode of action of polymyxins against Gram-negative bacteria involves the inhibition of NADH-quinone oxidoreductase activity

A simple and inexpensive sample-handling method for the semi-preparative RP-HPLC of polypeptides and non-polar peptide derivatives: pre-adsorption of samples

A synthetic lipopeptide targeting top-priority multidrug-resistant Gram-negative pathogens

Active site similarity between human and Plasmodium falciparum phosphodiesterases: considerations for antimalarial drug design

Analysis of anti-PDE3 activity of 2-morpholinochromone derivatives reveals multiple mechanisms of anti-platelet activity.

Antimicrobial Activity and Toxicity of the Major Lipopeptide Components of Polymyxin B and Colistin: Last-line Antibiotics against Multidrug-Resistant Gram-negative Bacteria

Application of a Sulfoxonium Ylide Electrophile to Generate Cathepsin X-Selective Activity-Based Probes

Beta amino acid-modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity.

Carbohydrate-mimetic peptides: structural aspects of mimicry and therapeutic implications.

Cellular Uptake and Localization of Polymyxins in Renal Tubular Cells Using Rationally Designed Fluorescent Probes

Characterization of epitope regions of thyrotropin β-subunit recognized by the monoclonal antibodies mAb279 and mAb299: a chimeric peptide approach

Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.

Cleavage and activation of proteinase-activated receptor-2 on human neutrophils by gingipain-R from Porphyromonas gingivalis

Conformational studies on (+)-anatoxin-a and derivatives

Controlled Construction of Cyclic d / l Peptide Nanorods

Cyclic Hexapeptide Mimics of the LEDGF Integrase Recognition Loop in Complex with HIV-1 Integrase

Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors using in vitro mutagenesis of non-conserved amino acids and kinetic analysis

Design and Evaluation of Novel Polymyxin Fluorescent Probes

Design, Synthesis, and Characterization of Cyclic Peptidomimetics of the Inducible Nitric Oxide Synthase Binding Epitope That Disrupt the Protein-Protein Interaction Involving SPRY Domain-Containing Suppressor of Cytokine Signaling Box Protein (SPSB

Design, synthesis, and evaluation of a new fluorescent probe for measuring polymyxin-lipopolysaccharide binding interactions

Development of cognitive enhancers based on inhibition of insulin-regulated aminopeptidase

Development of single and mixed isoform selectivity PI3Kδ inhibitors by targeting Asn836 of PI3Kδ.

Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).

Disrupting the platelet internal membrane via PI3KC2α inhibition impairs thrombosis independently of canonical platelet activation

Dissecting isoform selectivity of PI3K inhibitors: the role of non-conserved residues in the catalytic pocket

Evidence for the activation of PAR-2 by the sperm protease, acrosin: expression of the receptor on oocytes

Functional Characterization of the Unique Terminal Thioesterase Domain from Polymyxin Synthetase.

IP3-4 kinase Arg1 regulates cell wall homeostasis and surface architecture to promote clearance of Cryptococcus neoformans infection in a mouse model.

Identification and development of specific inhibitors for insulin-regulated aminopeptidase as a new class of cognitive enhancers

Identification of a Cyanine-Dye Labeled Peptidic Ligand for Y1R and Y4R, Based upon the Neuropeptide Y C-Terminal Analogue, BVD-15.

Identification of a unique filamin A binding region within the cytoplasmic domain of glycoprotein Ibalpha.

Identification of potent phosphodiesterase inhibitors that demonstrate cyclic nucleotide-dependent functions in apicomplexan parasites.

Identification of preferred carbohydrate binding modes in xenoreactive antibodies by combining conformational filters and binding site maps

Imaging the distribution of polymyxins in the kidney

Importance of the P4' residue in human granzyme B inhibitors and substrates revealed by scanning mutagenesis of the proteinase inhibitor 9 reactive center loop

In silico analysis of antibody-carbohydrate interactions and its application to xenoreactive antibodies

Inflammatory twins from PI3K gang brought to justice?

Investigating the Interaction of Octapeptin A3 with Model Bacterial Membranes

Isoform-selective inhibition of phosphoinositide 3-kinase: identification of a new region of nonconserved amino acids critical for p110α inhibition

Measuring polymyxin uptake by renal tubular cells: is BODIPY-polymyxin B an appropriate probe?

Mechanisms of PI3Kβ-selective inhibition revealed by reciprocal mutagenesis.

Methionine Ameliorates Polymyxin-Induced Nephrotoxicity by Attenuating Cellular Oxidative Stress.

Molecular basis for the increased polymyxin susceptibility of Klebsiella pneumoniae strains with under-acylated lipid A.

Molecular determinants of the substrate specificity of the complement-initiating protease, C1r.

Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y4 Receptor Agonist Derived by an Olefin Metathesis Approach.

PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues

PI 3-kinase p110beta: a new target for antithrombotic therapy

Parallel and antiparallel cyclic d/l peptide nanotubes.

Peptide inhibitors of xenoreactive antibodies mimic the interaction profile of the native carbohydrate antigens

Pharmacokinetics of the Individual Major Components of Polymyxin B and Colistin in Rats.

Pharmacology of polymyxins: new insights into an 'old' class of antibiotics

Phenylalanine-544 plays a key role in substrate and inhibitor binding by providing a hydrophobic packing point at the active site of insulin-regulated aminopeptidase

Polymyxins and analogues bind to ribosomal RNA and interfere with eukaryotic translation in vitro.

Polymyxins: a new hope in combating Gram-negative superbugs?

Potent inhibitors of phosphatidylinositol 3 (PI3) kinase that have antiproliferative activity only when delivered as prodrug forms.

Probing the penetration of antimicrobial polymyxin lipopeptides into gram-negative bacteria

Quantitation of Polymyxin-Lipopolysaccharide Interactions Using an Image-Based Fluorescent Probe.

Re-discovering PDE3 inhibitors--new opportunities for a long neglected target.

Redox-stable cyclic peptide inhibitors of the SPSB2-iNOS interaction

Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase

RhoA sustains integrin alpha IIbbeta 3 adhesion contacts under high shear.

Significant accumulation of polymyxin in single renal tubular cells: a medicinal chemistry and triple correlative microscopy approach

Solid-Phase synthesis of a dendritic peptide related to a retinoblastoma protein fragment utilizing a combined boc- and fmoc-chemistry approach

Solid-phase synthesis of cyclic analogues related to the hypoglycaemic peptide hGH(6-13): comparison of two i-->i + 4 lactam cyclization procedures

Structural Determinants of Isoform Selectivity in PI3K Inhibitors

Structural and biochemical characterization of the oxidoreductase NmDsbA3 from Neisseria meningitidis

Structural basis of nSH2 regulation and lipid binding in PI3Kα.

Structure of granzyme C reveals an unusual mechanism of protease autoinhibition

Structure, Function, and Biosynthetic Origin of Octapeptin Antibiotics Active against Extensively Drug-Resistant Gram-Negative Bacteria.

Structure--activity relationships of polymyxin antibiotics

Structure-Activity Studies of β-Hairpin Peptide Inhibitors of the Plasmodium falciparum AMA1-RON2 Interaction

Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate

Structure-activity relationships for the binding of polymyxins with human α-1-acid glycoprotein