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Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2 (2023)
Journal Article
Casella, B. M., Farmer, J. P., Nesheva, D. N., Williams, H. E., Charlton, S. J., Holliday, N. D., …Mistry, S. N. (2023). Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2. Journal of Medicinal Chemistry, https://doi.org/10.1021/acs.jmedchem.3c00849

The inhibition of CXC chemokine receptor 2 (CXCR2), a key inflammatory mediator, is a potential strategy in the treatment of several pulmonary diseases and cancers. The complexity of endogenous chemokine interaction with the orthosteric binding site... Read More about Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2.

Discovery of new imidazotetrazinones with potential to overcome tumor resistance (2023)
Journal Article
Summers, H. S., Lewis, W., Williams, H. E. L., Bradshaw, T. D., Moody, C. J., & Stevens, M. F. G. (2023). Discovery of new imidazotetrazinones with potential to overcome tumor resistance. European Journal of Medicinal Chemistry, 257, Article 115507. https://doi.org/10.1016/j.ejmech.2023.115507

We describe the design, organic synthesis, and characterization, including X-ray crystallography, of a series of novel analogues of the clinically used antitumor agent temozolomide, together with their in vitro biological evaluation. The work has res... Read More about Discovery of new imidazotetrazinones with potential to overcome tumor resistance.

Effect of sweeteners and carbonation on aroma partitioning and release in beverage systems (2022)
Journal Article
Yeo, H., Linforth, R., MacNaughtan, W., Williams, H., Hewson, L., & Fisk, I. D. (2023). Effect of sweeteners and carbonation on aroma partitioning and release in beverage systems. Food Research International, 164, Article 112373. https://doi.org/10.1016/j.foodres.2022.112373

The effect of monosaccharides (glucose, fructose and galactose) and disaccharides (sucrose and lactose) at 10, 20 and 30 % w/v on the in-vitro aroma partitioning of C - C aldehydes and ethyl esters, as well as limonene (concentration of aroma compo... Read More about Effect of sweeteners and carbonation on aroma partitioning and release in beverage systems.

Direct routes to functional RAFT agents from substituted N-alkyl maleimides (2022)
Journal Article
Catania, R., Foralosso, R., Spanos, L., Russo, E., Mastrotto, F., Gurnani, P., …Mantovani, G. (2022). Direct routes to functional RAFT agents from substituted N-alkyl maleimides. Polymer Chemistry, 13(45), 6261-6267. https://doi.org/10.1039/d1py01565f

N-substituted maleimides have become an indispensable tool for the synthesis of bioconjugates and functional materials. Herein, we present three strategies for the incorporation of N-alkyl substituted maleimides into RAFT agents and show that these m... Read More about Direct routes to functional RAFT agents from substituted N-alkyl maleimides.

Relative Abundance of Lipid Metabolites in Spermatozoa across Three Compartments (2022)
Journal Article
Furse, S., Kusinski, L. C., Ray, A., Glenn-Sansum, C., Williams, H., Koulman, A., & Meek, C. L. (2022). Relative Abundance of Lipid Metabolites in Spermatozoa across Three Compartments. International Journal of Molecular Sciences, 23(19), Article 11655. https://doi.org/10.3390/ijms231911655

Male fertility, as manifest by the quantity and progressive motility of spermatozoa, is negatively impacted by obesity, dyslipidaemia and metabolic disease. However, the relative distribution of lipids in spermatozoa and the two compartments which su... Read More about Relative Abundance of Lipid Metabolites in Spermatozoa across Three Compartments.

Paternal nutritional programming of lipid metabolism is propagated through sperm and seminal plasma (2022)
Journal Article
Furse, S., Watkins, A. J., Williams, H. E., Snowden, S. G., Chiarugi, D., & Koulman, A. (2022). Paternal nutritional programming of lipid metabolism is propagated through sperm and seminal plasma. Metabolomics, 18(2), Article 13. https://doi.org/10.1007/s11306-022-01869-9

Background: The paternal diet affects lipid metabolism in offspring for at least two generations through nutritional programming. However, we do not know how this is propagated to the offspring. Objectives: We tested the hypothesis that the changes i... Read More about Paternal nutritional programming of lipid metabolism is propagated through sperm and seminal plasma.

An ALS-associated variant of the autophagy receptor SQSTM1/p62 reprograms binding selectivity toward the autophagy-related hATG8 proteins (2021)
Journal Article
Brennan, A., Layfield, R., Long, J., Williams, H. E., Oldham, N. J., Scott, D., & Searle, M. S. (2022). An ALS-associated variant of the autophagy receptor SQSTM1/p62 reprograms binding selectivity toward the autophagy-related hATG8 proteins. Journal of Biological Chemistry, 298(2), Article 101514. https://doi.org/10.1016/j.jbc.2021.101514

Recognition of human autophagy-related 8 (hATG8) proteins by autophagy receptors represents a critical step within this cellular quality control system. Autophagy impairment is known to be a pathogenic mechanism in the motor neuron disorder amyotroph... Read More about An ALS-associated variant of the autophagy receptor SQSTM1/p62 reprograms binding selectivity toward the autophagy-related hATG8 proteins.

Site-Selective Installation of Nϵ-Modified Sidechains into Peptide and Protein Scaffolds via Visible-Light-Mediated Desulfurative C–C Bond Formation (2021)
Journal Article
Griffiths, R. C., Smith, F. R., Long, J. E., Scott, D., Williams, H. E., Oldham, N. J., …Mitchell, N. J. (2022). Site-Selective Installation of Nϵ-Modified Sidechains into Peptide and Protein Scaffolds via Visible-Light-Mediated Desulfurative C–C Bond Formation. Angewandte Chemie International Edition, 61(2), Article e202110223. https://doi.org/10.1002/anie.202110223

Post-translational modifications (PTMs) enhance the repertoire of protein function and mediate or influence the activity of many cellular processes. The preparation of site-specifically and homogeneously modified proteins, to apply as tools to unders... Read More about Site-Selective Installation of Nϵ-Modified Sidechains into Peptide and Protein Scaffolds via Visible-Light-Mediated Desulfurative C–C Bond Formation.

Site‐Selective Installation of Nϵ ‐Modified Sidechains into Peptide and Protein Scaffolds via Visible‐Light‐Mediated Desulfurative C–C Bond Formation (2021)
Journal Article
Griffiths, R. C., Smith, F. R., Long, J. E., Scott, D., Williams, H. E. L., Oldham, N. J., …Mitchell, N. J. (2022). Site‐Selective Installation of Nϵ ‐Modified Sidechains into Peptide and Protein Scaffolds via Visible‐Light‐Mediated Desulfurative C–C Bond Formation. Angewandte Chemie, 134(2), Article e202110223. https://doi.org/10.1002/ange.202110223

Post-translational modifications (PTMs) enhance the repertoire of protein function and mediate or influence the activity of many cellular processes. The preparation of site-specifically and homogeneously modified proteins, to apply as tools to unders... Read More about Site‐Selective Installation of Nϵ ‐Modified Sidechains into Peptide and Protein Scaffolds via Visible‐Light‐Mediated Desulfurative C–C Bond Formation.

A pipeline for making 31P NMR accessible for small- and large-scale lipidomics studies (2021)
Journal Article
Furse, S., Williams, H. E. L., Watkins, A. J., Virtue, S., Vidal-Puig, A., Amarsi, R., …Koulman, A. (2021). A pipeline for making 31P NMR accessible for small- and large-scale lipidomics studies. Analytical and Bioanalytical Chemistry, 413(19), 4763-4773. https://doi.org/10.1007/s00216-021-03430-4

Detailed molecular analysis is of increasing importance in research into the regulation of biochemical pathways, organismal growth and disease. Lipidomics in particular is increasingly sought after as it provides insight into molecular species involv... Read More about A pipeline for making 31P NMR accessible for small- and large-scale lipidomics studies.

Lipid traffic analysis reveals the impact of high paternal carbohydrate intake on offsprings’ lipid metabolism (2021)
Journal Article
Furse, S., Watkins, A., Hojat, N., Smith, J., Williams, H., Chiarugi, D., & Koulman, A. (2021). Lipid traffic analysis reveals the impact of high paternal carbohydrate intake on offsprings’ lipid metabolism. Communications Biology, 4, Article 163. https://doi.org/10.1038/s42003-021-01686-1

In this paper we present an investigation of parental-diet-driven metabolic programming in offspring using a novel computational network analysis tool. The impact of high paternal carbohydrate intake on offsprings’ phospholipid and triglyceride metab... Read More about Lipid traffic analysis reveals the impact of high paternal carbohydrate intake on offsprings’ lipid metabolism.

Structural and electronic studies of substituted m-terphenyl lithium complexes (2020)
Journal Article
Valentine, A. J., Geer, A. M., Taylor, L. J., Teale, A. M., Wood, K. E., Williams, H. E. L., …Kays, D. L. (2021). Structural and electronic studies of substituted m-terphenyl lithium complexes. Dalton Transactions, 50(2), 722-728. https://doi.org/10.1039/d0dt03972a

The effect of para-substitution upon the structural and electronic properties of a series of m-terphenyl lithium complexes [R-Ar#-Li]2 (R = t-Bu 1, SiMe32, H 3, Cl 4, CF35; where R-Ar# = 2,6-{2,6-Xyl}2-4-R-C6H2 and 2,6-Xyl = 2,6-Me2C6H3) has been inv... Read More about Structural and electronic studies of substituted m-terphenyl lithium complexes.

Incidence, nature and causes of avoidable significant harm in primary care in England: retrospective case note review (2020)
Journal Article
Avery, A. J., Sheehan, C. L., Bell, B. G., Armstrong, S. J., Ashcroft, D. M., Boyd, M. J., …Carson-Stevens, A. (2021). Incidence, nature and causes of avoidable significant harm in primary care in England: retrospective case note review. BMJ Quality and Safety, 30(12), 961-976. https://doi.org/10.1136/bmjqs-2020-011405

Objective To estimate the incidence of avoidable significant harm in primary care in England; describe and classify the associated patient safety incidents and generate suggestions to mitigate risks of ameliorable factors contributing to the incident... Read More about Incidence, nature and causes of avoidable significant harm in primary care in England: retrospective case note review.

Site‐Selective Modification of Peptides and Proteins via Interception of Free‐Radical‐Mediated Dechalcogenation (2020)
Journal Article
Griffiths, R. C., Smith, F. R., Long, J. E., Williams, H. E. L., Layfield, R., & Mitchell, N. J. (2020). Site‐Selective Modification of Peptides and Proteins via Interception of Free‐Radical‐Mediated Dechalcogenation. Angewandte Chemie, 132(52), 23867-23875. https://doi.org/10.1002/ange.202006260

The development of site-selective chemistry targeting the canonical amino acids enables the controlled installation of desired functionalities into native peptides and proteins. Such techniques facilitate the development of polypeptide conjugates to... Read More about Site‐Selective Modification of Peptides and Proteins via Interception of Free‐Radical‐Mediated Dechalcogenation.

Selection of potential molecular markers for cheese ripening and quality prediction by NMR spectroscopy (2020)
Journal Article
Chen, Y., MacNaughtan, W., Jones, P., Yang, Q., Williams, H., & Foster, T. (2021). Selection of potential molecular markers for cheese ripening and quality prediction by NMR spectroscopy. LWT - Food Science and Technology, 136, Article 110306. https://doi.org/10.1016/j.lwt.2020.110306

© 2020 Elsevier Ltd Predicting cheese quality as early as possible after ripening is important for quality control in the cheese industry. The main aim of this study was to investigate potential metabolites for predictive models of Cheddar cheese qua... Read More about Selection of potential molecular markers for cheese ripening and quality prediction by NMR spectroscopy.

Site-Selective Modification of Peptides and Proteins via Interception of Free-Radical-Mediated Dechalcogenation (2020)
Journal Article
Griffiths, R. C., Smith, F. R., Long, J. E., Williams, H. E. L., Layfield, R., & Mitchell, N. J. (2020). Site-Selective Modification of Peptides and Proteins via Interception of Free-Radical-Mediated Dechalcogenation. Angewandte Chemie International Edition, 59(52), 23659-23667. https://doi.org/10.1002/anie.202006260

© 2020 The Authors. Published by Wiley-VCH GmbH The development of site-selective chemistry targeting the canonical amino acids enables the controlled installation of desired functionalities into native peptides and proteins. Such techniques facilita... Read More about Site-Selective Modification of Peptides and Proteins via Interception of Free-Radical-Mediated Dechalcogenation.

Structural, functional, and metabolic alterations in human cerebrovascular endothelial cells during toxoplasma gondii infection and amelioration by verapamil in vitro (2020)
Journal Article
Al-Sandaqchi, A. T., Marsh, V., Williams, H. E. L., Stevenson, C. W., & Elsheikha, H. M. (2020). Structural, functional, and metabolic alterations in human cerebrovascular endothelial cells during toxoplasma gondii infection and amelioration by verapamil in vitro. Microorganisms, 8(9), Article 1386. https://doi.org/10.3390/microorganisms8091386

© 2020 by the authors. Licensee MDPI, Basel, Switzerland. Toxoplasma gondii (T. gondii), the causative agent of toxoplasmosis, is a frequent cause of brain infection. Despite its known ability to invade the brain, there is still a dire need to better... Read More about Structural, functional, and metabolic alterations in human cerebrovascular endothelial cells during toxoplasma gondii infection and amelioration by verapamil in vitro.

Corrigendum: A Highly Active Bidentate Magnesium Catalyst for Amine‐Borane Dehydrocoupling: Kinetic and Mechanistic Studies (2020)
Journal Article
Ried, A. C. A., Taylor, L. J., Geer, A. M., Williams, H. E. L., Lewis, W., Blake, A. J., & Kays, D. L. (2020). Corrigendum: A Highly Active Bidentate Magnesium Catalyst for Amine‐Borane Dehydrocoupling: Kinetic and Mechanistic Studies. Chemistry - A European Journal, 26(7), 1692-1692. https://doi.org/10.1002/chem.202000050

In the published paper, we described the attempted synthesis of Me2NH⋅BD3, according to the method published by Webster et al., which in our hands afforded a mixture of Me2NH⋅BH3 and Me2NH⋅BD3. We would like to clarify that in the paper Webster et al... Read More about Corrigendum: A Highly Active Bidentate Magnesium Catalyst for Amine‐Borane Dehydrocoupling: Kinetic and Mechanistic Studies.

Targeted PEG-poly(glutamic acid) complexes for inhalation protein delivery to the lung (2019)
Journal Article
Nieto-Orellana, A., Li, H., Rosiere, R., Wauthoz, N., Williams, H., Monteiro, C., …Stolnik, S. (2019). Targeted PEG-poly(glutamic acid) complexes for inhalation protein delivery to the lung. Journal of Controlled Release, 316, 250-262. https://doi.org/10.1016/j.jconrel.2019.10.012

Pulmonary delivery is increasingly seen as an attractive, non-invasive route for the delivery of forthcoming protein therapeutics. In this context, here we describe protein complexes with a new ‘complexing excipient’ - vitamin B12-targeted poly(ethyl... Read More about Targeted PEG-poly(glutamic acid) complexes for inhalation protein delivery to the lung.

Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells (2019)
Journal Article
Liu, Z., Turyanska, L., Zamberlan, F., Pacifico, S., Bradshaw, T. D., Moro, F., …Thomas, N. R. (2019). Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells. Nanotechnology, 30(50), Article 505102. https://doi.org/10.1088/1361-6528/ab437c

We report on the synthesis of water-soluble gold nanoclusters capped with polyethylene glycol (PEG)-based ligands and further functionalized with folic acid for specific cellular uptake. The dihydrolipoic acid-PEG-based ligands terminated with -OMe,... Read More about Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells.