List of works - Lyn H. Jones

A Concise Synthesis of Trifluoromethyl-Substituted 4-Aryloxy Pyrazoles

A Concise and Selective Synthesis of Novel 5-Aryloxyimidazole NNRTIs

scientific article published on 01 April 2006

A flow cytometry-based screen identifies MBNL1 modulators that rescue splicing defects in myotonic dystrophy type I.

scientific article

A library approach to rapidly discover photoaffinity probes of the mRNA decapping scavenger enzyme DcpS.

scientific article published on 11 May 2015

A mild synthesis of N-functionalised bromomaleimides, thiomaleimides and bromopyridazinediones

scientific article published on July 2013

Active immunization with a glycolipid transition state analogue protects against endotoxic shock.

scientific article

An industry perspective on drug target validation

scientific article published on 09 May 2016

Antibody catalysis of the oxidation of water

scientific article

Applications of chemogenomic library screening in drug discovery

scientific article

Aryloxymaleimides for cysteine modification, disulfide bridging and the dual functionalization of disulfide bonds

scientific article published on 01 July 2014

Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

scientific article published on 16 August 2016

Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes.

scientific article published on 4 January 2017

Cell permeable affinity- and activity-based probes

scientific article published on 29 October 2015

Cellular thermal shift and clickable chemical probe assays for the determination of drug-target engagement in live cells

article

Chemical biology & drug discovery

scientific article published on 08 October 2014

Chemistry and biology of biomolecule nitration

scientific article published on September 2012

Chemoselective Preparation of Clickable Aryl Sulfonyl Fluoride Monomers: A Toolbox of Highly Functionalized Intermediates for Chemical Biology Probe Synthesis.

scientific article

Cleavage of the cyclohexyl-subunit of rapamycin results in loss of immunosuppressive activity

scientific article published on 01 February 1999

Click chemistry patents and their impact on drug discovery and chemical biology

scientific article published on January 2015

Click-enabled heterotrifunctional template for sequential bioconjugations

article

Clinical chemoproteomics-Opportunities and obstacles.

scientific article

Comparison of the non-nucleoside reverse transcriptase inhibitor lersivirine with its pyrazole and imidazole isomers.

scientific article

Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane

scientific article published on 25 April 2017

Conformation and stereodynamics of 2,2'-disubstituted N,N'-diaryl ureas

scientific article published on 16 June 2008

Conversion of enediynes into quinones by antibody catalysis and in aqueous buffers: implications for an alternative enediyne therapeutic mechanism

scientific article published in April 2001

Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue

scientific article published on 18 July 2017

Design and development of histone deacetylase (HDAC) chemical probes for cell-based profiling.

scientific article

Design and synthesis of a fluorescent muscarinic antagonist

scientific article published on 17 November 2007

Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).

scientific article

Development of a cell viability assay to assess drug metabolite structure-toxicity relationships

scientific article published on 30 June 2016

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

scientific article published on 28 October 2016

Dual-pharmacology muscarinic antagonist and β₂ agonist molecules for the treatment of chronic obstructive pulmonary disease

scientific article published on October 2011

Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-β₂-agonist for the treatment of chronic obstructive pulmonary disease

scientific article published on 2 September 2011

Emerging Utility of Fluorosulfate Chemical Probes

scientific article published on 27 June 2018

Expanding chemogenomic space using chemoproteomics

scientific article published on 13 June 2019

Helix persistence and breakdown in oligoureas of metaphenylenediamine: apparent diastereotopicity as a spectroscopic marker of helix length in solution

scientific article

Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes

scientific article

Identification of novel macrolides with antibacterial, anti-inflammatory and type I and III IFN-augmenting activity in airway epithelium

scientific article published on 25 July 2016

In vitro and in vivo effects of 2,4 diaminoquinazoline inhibitors of the decapping scavenger enzyme DcpS: Context-specific modulation of SMN transcript levels.

scientific article published on 25 September 2017

In-cell click labelling of small molecules to determine subcellular localisation

scientific article

Inhalation by design.

scientific article published in October 2011

Know your target, know your molecule

scientific article

Medicinal chemistry of glucagon-like peptide receptor agonists

scientific article published on January 2013

Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells

scientific article published on 31 October 2017

Modern advances in heterocyclic chemistry in drug discovery

scientific article

Molecular hybridization yields triazole bronchodilators for the treatment of COPD.

scientific article published on 8 October 2015

Molecular scaffolds using multiple orthogonal conjugations: applications in chemical biology and drug discovery

scientific article published on 19 April 2012

Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays

scientific article

Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.

scientific article published on 6 October 2006

Optimization of 5-aryloxyimidazole non-nucleoside reverse transcriptase inhibitors

scientific article published on November 2008

Oxaziridine-mediated amination of primary amines: scope and application to a one-pot pyrazole synthesis.

scientific article published in February 2005

PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease

scientific article published on 24 December 2020

Pharmacological Correction of Proteinopathies via Lysosomal Degradation

scientific article published on 30 January 2020

Physicochemical drug properties associated with in vivo toxicological outcomes: a review

scientific article

Precision Retargeting: A Selective Covalent Inhibitor Illuminates CDK7 Biology

scientific article published on 01 June 2019

Protein labelling

scientific article published on 01 May 2016

Pyrazole NNRTIs 3: optimisation of physicochemical properties

scientific article published on 14 August 2009

Quantifying drug-target engagement in live cells using sulfonyl fluoride chemical probes

scientific article published on 09 March 2019

Quantitative measurement of intracellular HDAC1/2 drug occupancy using a -cyclooctene largazole thiol probe

scientific article published on 09 January 2017

Rare diseases. Foreword

scientific article published in June 2014

Rational Targeting of Active-Site Tyrosine Residues Using Sulfonyl Fluoride Probes

article

Reactive Chemical Probes: Beyond the Kinase Cysteinome.

scientific article published on 12 April 2018

Recent advances in the molecular design of synthetic vaccines

scientific article

Relaying stereochemistry through aromatic ureas: 1,9 and 1,15 remote stereocontrol

scientific article published on 26 November 2008

Selection of a novel anti-nicotine vaccine: influence of antigen design on antibody function in mice

scientific article

Selective Downregulation of JAK2 and JAK3 by an ATP-Competitive pan-JAK Inhibitor

scientific article

Selectivity Determination of a Small Molecule Chemical Probe Using Protein Microarray and Affinity Capture Techniques

scientific article published on 5 August 2016

Small molecules targeting hepatitis C virus-encoded NS5A cause subcellular redistribution of their target: insights into compound modes of action

scientific article

Small-Molecule Kinase Downregulators

scientific article published on 8 November 2017

Squaramides: physical properties, synthesis and applications

scientific article published on 14 March 2011

Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain

scientific article published on 4 April 2017

Sulfonyl fluorides as privileged warheads in chemical biology

scientific article

Synthetic chemistry-led creation of a difluorinated biaryl ether non-nucleoside reverse transcriptase inhibitor

scientific article published on 02 October 2007

Synthetic phosphorylation of p38α recapitulates protein kinase activity

scientific article published on 27 January 2014

TAK1 inhibition in the DFG-out conformation

scientific article published in November 2013

TAK1 selective inhibition: state of the art and future opportunities

scientific article published on January 2015

Target Validation Using PROTACs: Applying the Four Pillars Framework

scientific article published on 17 December 2020

Target validation using chemical probes

scientific article

Thermodynamic optimisation in drug discovery: a case study using carbonic anhydrase inhibitors

scientific article

Total Synthesis of (+)-Zaragozic Acid C

scientific article published on 01 October 2000

Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities

scientific article

Understanding and applying tyrosine biochemical diversity

scientific article published on May 2014

Understanding the chemically-reactive proteome

scientific article published on 01 May 2016

Uptake, efficacy, and systemic distribution of naked, inhaled short interfering RNA (siRNA) and locked nucleic acid (LNA) antisense

scientific article

Welcome to Pharmaceutical Patent Analyst. Foreword.

scientific article

List of works by Lyn H. Jones

A Concise Synthesis of Trifluoromethyl-Substituted 4-Aryloxy Pyrazoles

A Concise and Selective Synthesis of Novel 5-Aryloxyimidazole NNRTIs

A flow cytometry-based screen identifies MBNL1 modulators that rescue splicing defects in myotonic dystrophy type I.

A library approach to rapidly discover photoaffinity probes of the mRNA decapping scavenger enzyme DcpS.

A mild synthesis of N-functionalised bromomaleimides, thiomaleimides and bromopyridazinediones

Active immunization with a glycolipid transition state analogue protects against endotoxic shock.

An industry perspective on drug target validation

Antibody catalysis of the oxidation of water

Applications of chemogenomic library screening in drug discovery

Aryloxymaleimides for cysteine modification, disulfide bridging and the dual functionalization of disulfide bonds

Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes.

Cell permeable affinity- and activity-based probes

Cellular thermal shift and clickable chemical probe assays for the determination of drug-target engagement in live cells

Chemical biology & drug discovery

Chemistry and biology of biomolecule nitration

Chemoselective Preparation of Clickable Aryl Sulfonyl Fluoride Monomers: A Toolbox of Highly Functionalized Intermediates for Chemical Biology Probe Synthesis.

Cleavage of the cyclohexyl-subunit of rapamycin results in loss of immunosuppressive activity

Click chemistry patents and their impact on drug discovery and chemical biology

Click-enabled heterotrifunctional template for sequential bioconjugations

Clinical chemoproteomics-Opportunities and obstacles.

Comparison of the non-nucleoside reverse transcriptase inhibitor lersivirine with its pyrazole and imidazole isomers.

Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane

Conformation and stereodynamics of 2,2'-disubstituted N,N'-diaryl ureas

Conversion of enediynes into quinones by antibody catalysis and in aqueous buffers: implications for an alternative enediyne therapeutic mechanism

Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue

Design and development of histone deacetylase (HDAC) chemical probes for cell-based profiling.

Design and synthesis of a fluorescent muscarinic antagonist

Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).

Development of a cell viability assay to assess drug metabolite structure-toxicity relationships

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

Dual-pharmacology muscarinic antagonist and β₂ agonist molecules for the treatment of chronic obstructive pulmonary disease

Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-β₂-agonist for the treatment of chronic obstructive pulmonary disease

Emerging Utility of Fluorosulfate Chemical Probes

Expanding chemogenomic space using chemoproteomics

Helix persistence and breakdown in oligoureas of metaphenylenediamine: apparent diastereotopicity as a spectroscopic marker of helix length in solution

Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes

Identification of novel macrolides with antibacterial, anti-inflammatory and type I and III IFN-augmenting activity in airway epithelium

In vitro and in vivo effects of 2,4 diaminoquinazoline inhibitors of the decapping scavenger enzyme DcpS: Context-specific modulation of SMN transcript levels.

In-cell click labelling of small molecules to determine subcellular localisation

Inhalation by design.

Know your target, know your molecule

Medicinal chemistry of glucagon-like peptide receptor agonists

Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells

Modern advances in heterocyclic chemistry in drug discovery

Molecular hybridization yields triazole bronchodilators for the treatment of COPD.

Molecular scaffolds using multiple orthogonal conjugations: applications in chemical biology and drug discovery

Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays

Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.

Optimization of 5-aryloxyimidazole non-nucleoside reverse transcriptase inhibitors

Oxaziridine-mediated amination of primary amines: scope and application to a one-pot pyrazole synthesis.

PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease

Pharmacological Correction of Proteinopathies via Lysosomal Degradation

Physicochemical drug properties associated with in vivo toxicological outcomes: a review

Precision Retargeting: A Selective Covalent Inhibitor Illuminates CDK7 Biology

Protein labelling

Pyrazole NNRTIs 3: optimisation of physicochemical properties

Quantifying drug-target engagement in live cells using sulfonyl fluoride chemical probes

Quantitative measurement of intracellular HDAC1/2 drug occupancy using a -cyclooctene largazole thiol probe

Rare diseases. Foreword

Rational Targeting of Active-Site Tyrosine Residues Using Sulfonyl Fluoride Probes

Reactive Chemical Probes: Beyond the Kinase Cysteinome.

Recent advances in the molecular design of synthetic vaccines

Relaying stereochemistry through aromatic ureas: 1,9 and 1,15 remote stereocontrol

Selection of a novel anti-nicotine vaccine: influence of antigen design on antibody function in mice

Selective Downregulation of JAK2 and JAK3 by an ATP-Competitive pan-JAK Inhibitor

Selectivity Determination of a Small Molecule Chemical Probe Using Protein Microarray and Affinity Capture Techniques

Small molecules targeting hepatitis C virus-encoded NS5A cause subcellular redistribution of their target: insights into compound modes of action

Small-Molecule Kinase Downregulators

Squaramides: physical properties, synthesis and applications

Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain

Sulfonyl fluorides as privileged warheads in chemical biology

Synthetic chemistry-led creation of a difluorinated biaryl ether non-nucleoside reverse transcriptase inhibitor

Synthetic phosphorylation of p38α recapitulates protein kinase activity

TAK1 inhibition in the DFG-out conformation

TAK1 selective inhibition: state of the art and future opportunities

Target Validation Using PROTACs: Applying the Four Pillars Framework

Target validation using chemical probes

Thermodynamic optimisation in drug discovery: a case study using carbonic anhydrase inhibitors