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All Outputs (133)

Class 1 PI3K clinical candidates and recent inhibitor design strategies: a medicinal chemistry perspective (2018)
Journal Article
Garces, A. E., & Stocks, M. J. (2019). Class 1 PI3K clinical candidates and recent inhibitor design strategies: a medicinal chemistry perspective. Journal of Medicinal Chemistry, 62(10), 4815-4850. https://doi.org/10.1021/acs.jmedchem.8b01492

Phosphatidylinositol 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylate the 3-OH of the inositol ring of phosphoinositides, and deregulation of this pathway has implications in many diseases. The search for novel PI3K inhibitors has b... Read More about Class 1 PI3K clinical candidates and recent inhibitor design strategies: a medicinal chemistry perspective.

In vitro evaluation of electrospun blends of gelatin and PCL for application as a partial thickness corneal graft (2018)
Journal Article
Rose, J., Sidney, L., Patient, J., White, L., Dua, H., El Haj, A., …Rose, F. (2018). In vitro evaluation of electrospun blends of gelatin and PCL for application as a partial thickness corneal graft. Journal of Biomedical Materials Research Part A, 107(4), 828-838. https://doi.org/10.1002/jbm.a.36598

The advent of innovative surgical procedures utilizing partial thickness corneal grafts has created a need for the development of synthetic implants to recreate corneal stromal tissue. This work evaluates electrospun gelatin and polycaprolactone (PCL... Read More about In vitro evaluation of electrospun blends of gelatin and PCL for application as a partial thickness corneal graft.

Assessing the ex vivo permeation behaviour of functionalised contact lens coatings engineered using an electrohydrodynamic technique (2018)
Journal Article
Mehta, P., Al-Kinani, A. A., Qutachi, O., Arshad, M. S., Alqahtani, A., Chang, M., …Ahmad, Z. (2019). Assessing the ex vivo permeation behaviour of functionalised contact lens coatings engineered using an electrohydrodynamic technique. Journal of Physics: Materials, 2(1), 1-7. https://doi.org/10.1088/2515-7639/aaf263

In vitro testing alone is no longer considered sufficient evidence presented solely with respect to drug release and permeation testing. These studies are thought to be more reliable and representative when using tissue or animal models; as opposed t... Read More about Assessing the ex vivo permeation behaviour of functionalised contact lens coatings engineered using an electrohydrodynamic technique.

Profiling of 54 plasma glycoproteins by label-free targeted LC-MS/MS (2018)
Journal Article
Dahabiyeh, L. A., Tooth, D., & Barrett, D. A. (2019). Profiling of 54 plasma glycoproteins by label-free targeted LC-MS/MS. Analytical Biochemistry, 567, 72-81. https://doi.org/10.1016/j.ab.2018.12.011

Glycoproteins play a central role in diverse biological processes and are linked with many serious human diseases. In this paper we present a simple, reproducible and cost-effective analytical workflow that enables the reliable quantification of clin... Read More about Profiling of 54 plasma glycoproteins by label-free targeted LC-MS/MS.

Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site (2018)
Journal Article
Li, W., Sun, H., Xu, F., Shuai, W., Liu, J., Xu, S., …Xu, J. (2019). Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site. Bioorganic Chemistry, 85, 49-59. https://doi.org/10.1016/j.bioorg.2018.12.015

Twenty-two novel indole-vinyl sulfone derivatives were designed, synthesized and evaluated as tubulin polymerization inhibitors. The physicochemical and drug-likeness properties of all target compounds were predicted by Osiris calculations. All compo... Read More about Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site.

The pharmacy care plan service: Evaluation and estimate of cost-effectiveness (2018)
Journal Article
Twigg, M. J., Wright, D., Barton, G., Kirkdale, C. L., & Thornley, T. (2019). The pharmacy care plan service: Evaluation and estimate of cost-effectiveness. Research in Social and Administrative Pharmacy, 15(1), 84-92. https://doi.org/10.1016/j.sapharm.2018.03.062

Background: The UK Community Pharmacy Future group developed the Pharmacy Care Plan (PCP) service with a focus on patient activation, goal setting and therapy management. Objective: To estimate the effectiveness and cost-effectiveness of the PCP... Read More about The pharmacy care plan service: Evaluation and estimate of cost-effectiveness.

Geometry alone influences stem cell differentiation in a precision 3D printed stem cell niche (2018)
Working Paper
Prina, E., Sidney, L., Tromayer, M., Moore, J., Liska, R., Bertolin, M., …Rose, F. R. Geometry alone influences stem cell differentiation in a precision 3D printed stem cell niche

Stem cells within epithelial tissues reside in anatomical structures known as crypts that are known to contribute to the mechanical and chemical milieu important for function. To date, epithelial stem cell therapies have largely ignored the niche and... Read More about Geometry alone influences stem cell differentiation in a precision 3D printed stem cell niche.

Hydrophobicity of surface-immobilised molecules influences architectures formed via interfacial self-assembly of nucleoside-based gelators (2018)
Journal Article
Angelerou, M. G. F., Yang, B., Arnold, T., Rawle, J., Marlow, M., & Zelzer, M. (2018). Hydrophobicity of surface-immobilised molecules influences architectures formed via interfacial self-assembly of nucleoside-based gelators. Soft Matter, 14(48), 9851-9855. https://doi.org/10.1039/c8sm01868e

Surface-mediated self-assembly has potential in biomaterial development but underlying rules governing surface-gelator interactions are poorly understood. Here, we correlate surface properties with structural characterization data of nucleoside-based... Read More about Hydrophobicity of surface-immobilised molecules influences architectures formed via interfacial self-assembly of nucleoside-based gelators.

Qualitative study using interviews and focus groups to explore the current and potential for antimicrobial stewardship in community pharmacy informed by the Theoretical Domains Framework (2018)
Journal Article
Jones, L. F., Owens, R., Sallis, A., Ashiru-Oredope, D., Thornley, T., Francis, N. A., …McNulty, C. A. (2018). Qualitative study using interviews and focus groups to explore the current and potential for antimicrobial stewardship in community pharmacy informed by the Theoretical Domains Framework. BMJ Open, 8(12), Article e025101. https://doi.org/10.1136/bmjopen-2018-025101

Objectives Community pharmacists and their staff have the potential to contribute to antimicrobial stewardship (AMS). However, their barriers and opportunities are not well understood. The aim was to investigate the experiences and perceptions of com... Read More about Qualitative study using interviews and focus groups to explore the current and potential for antimicrobial stewardship in community pharmacy informed by the Theoretical Domains Framework.

Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site (2018)
Journal Article
Li, W., Shuai, W., Sun, H., Xu, F., Bi, Y., Xu, J., …Xu, S. (2019). Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site. European Journal of Medicinal Chemistry, 163, 428-442. https://doi.org/10.1016/j.ejmech.2018.11.070

A series of novel isocombretastatin A-4 (isoCA-4) analogs were designed and synthesized by replacing 3,4,5-trimethoylphenyl and isovanillin of isoCA-4 with quinoline and indole moieties, respectively. The structure activity relationships (SARs) of th... Read More about Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.

An analysis of endocannabinoid concentrations and mood following singing and exercise in healthy volunteers (2018)
Journal Article
Stone, N. L., Millar, S. A., Herrod, P. J. J., Barrett, D. A., Ortori, C. A., Mellon, V. A., & O’Sullivan, S. E. (2018). An analysis of endocannabinoid concentrations and mood following singing and exercise in healthy volunteers. Frontiers in Behavioral Neuroscience, 12, 1-10. https://doi.org/10.3389/fnbeh.2018.00269

© 2018 Stone, Millar, Herrod, Barrett, Ortori, Mellon and O’Sullivan. The euphoric feeling described after running is, at least in part, due to increased circulating endocannabinoids (eCBs). eCBs are lipid signaling molecules involved in reward, appe... Read More about An analysis of endocannabinoid concentrations and mood following singing and exercise in healthy volunteers.

Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine (2018)
Journal Article
Ali, J., Zgair, A., Hameed, G. S., Garnett, M. C., Roberts, C. J., Burley, J. C., & Gershkovich, P. (2019). Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine. International Journal of Pharmaceutics, 555, 228-236. https://doi.org/10.1016/j.ijpharm.2018.11.051

The oral cavity is of great importance to the performance of orally retained formulations, including: orally disintegrating tablets, taste-masked formulations, and buccal/sublingual delivery systems. With regards to in vitro dissolution assessment of... Read More about Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine.

New perspectives on iron uptake in eukaryotes (2018)
Journal Article
Sherman, H. G., Jovanovic, C., Stolnik, S., Baronian, K., Downard, A. J., & Rawson, F. J. (2018). New perspectives on iron uptake in eukaryotes. Frontiers in Molecular Biosciences, 5(NOV), Article 97. https://doi.org/10.3389/fmolb.2018.00097

All eukaryotic organisms require iron to function. Malfunctions within iron homeostasis have a range of physiological consequences, and can lead to the development of pathological conditions that can result in an excess of non-transferrin bound iron... Read More about New perspectives on iron uptake in eukaryotes.

Changes in chemical and ultrastructural composition of ameroid constrictors following in vitro expansion (2018)
Journal Article
Anderson, T. S., Rance, G. A., Jiang, L., Piggott, M. J., Field, E. J., & Chanoit, G. P. (2018). Changes in chemical and ultrastructural composition of ameroid constrictors following in vitro expansion. PLoS ONE, 13(11), 1-13. https://doi.org/10.1371/journal.pone.0207471

Objective To (1) characterise the chemical and ultra-structural composition of ameroid constrictors, at a native state and during in vitro expansion and (2) determine the presence of irritant compounds at the surface or within the bulk of the constr... Read More about Changes in chemical and ultrastructural composition of ameroid constrictors following in vitro expansion.

Small molecules as inhibitors of PCSK9: current status and future challenges (2018)
Journal Article
Xu, S., Luo, S., Zhu, Z., & Xu, J. (2019). Small molecules as inhibitors of PCSK9: current status and future challenges. European Journal of Medicinal Chemistry, 162, 212-233. https://doi.org/10.1016/j.ejmech.2018.11.011

Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays an important role in regulating lipoprotein metabolism by binding to low-density lipoprotein receptors (LDLRs), leading to their degradation. LDL cholesterol (LDL-C) lowering drugs that oper... Read More about Small molecules as inhibitors of PCSK9: current status and future challenges.

Clean Block Copolymer Microparticles from Supercritical CO 2 : Universal Templates for the Facile and Scalable Fabrication of Hierarchical Mesostructured Metal Oxides (2018)
Journal Article
Bennett, T. M., He, G., Larder, R. R., Fischer, M. G., Rance, G. A., Fay, M. W., …Howdle, S. M. (2018). Clean Block Copolymer Microparticles from Supercritical CO 2 : Universal Templates for the Facile and Scalable Fabrication of Hierarchical Mesostructured Metal Oxides. Nano Letters, 18(12), 7560-7569. https://doi.org/10.1021/acs.nanolett.8b03044

© 2018 American Chemical Society. Metal oxide microparticles with well-defined internal mesostructures are promising materials for a variety of different applications, but practical routes to such materials that allow the constituent structural leng... Read More about Clean Block Copolymer Microparticles from Supercritical CO 2 : Universal Templates for the Facile and Scalable Fabrication of Hierarchical Mesostructured Metal Oxides.

Discovery of peptide ligands targeting a specific ubiquitin-like domain– binding site in the deubiquitinase USP11 (2018)
Journal Article
Spiliotopoulos, A., Ferreras, L. B., Densham, R. M., Caulton, S. G., Maddison, B. C., Morris, J. R., …Dreveny, I. (2019). Discovery of peptide ligands targeting a specific ubiquitin-like domain– binding site in the deubiquitinase USP11. Journal of Biological Chemistry, 294(2), 424-436. https://doi.org/10.1074/jbc.RA118.004469

© 2019 Spiliotopoulos et al. Published by The American Society for Biochemistry and Molecular Biology, Inc. Ubiquitin-specific proteases (USPs) reverse ubiquitination and regulate virtually all cellular processes. Defined noncatalytic domains in USP... Read More about Discovery of peptide ligands targeting a specific ubiquitin-like domain– binding site in the deubiquitinase USP11.

New generation of bioreactors that advance extracellular matrix modelling and tissue engineering (2018)
Journal Article
Ahmed, S., Chauhan, V. M., Ghaemmaghami, A. M., & Aylott, J. W. (2019). New generation of bioreactors that advance extracellular matrix modelling and tissue engineering. Biotechnology Letters, 41(1), 1–25. https://doi.org/10.1007/s10529-018-2611-7

Bioreactors hold a lot of promise for tissue engineering and regenerative medicine applications. They have multiple uses including cell cultivation for therapeutic production and for in vitro organ modelling to provide a more physiologically relevant... Read More about New generation of bioreactors that advance extracellular matrix modelling and tissue engineering.