All Outputs (133)

In Silico and in Vitro-Guided Identification of Inhibitors of Alkylquinolone-Dependent Quorum Sensing in Pseudomonas aeruginosa (2018)
Journal Article
Soukarieh, F., Vico Oton, E., Dubern, J.-F., Gomes, J., Halliday, N., de Pilar Crespo, M., Ramírez-Prada, J., Insuasty, B., Abonia, R., Quiroga, J., Heeb, S., Williams, P., Stocks, M., & Cámara, M. (2018). In Silico and in Vitro-Guided Identification of Inhibitors of Alkylquinolone-Dependent Quorum Sensing in Pseudomonas aeruginosa. Molecules, 23(2), 1-15. https://doi.org/10.3390/molecules23020257

Pseudomonas aeruginosa is a major opportunistic pathogen in cystic fibrosis, wound and nosocomial infections, posing a serious burden to public health, due to its antibiotic resistance. The P. aeruginosa Pseudomonas Quinolone System (pqs) quorum sens... Read More about In Silico and in Vitro-Guided Identification of Inhibitors of Alkylquinolone-Dependent Quorum Sensing in Pseudomonas aeruginosa.

Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells (2018)
Journal Article
Stoddart, L. A., Vernall, A. J., Bouzo-Lorenzo, M., Bosma, R., Kooistra, A. J., de Graaf, C., Vischer, H. F., Leurs, R., Briddon, S. J., Kellam, B., & Hill, S. J. (2018). Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells. Scientific Reports, 8, Article 1572. https://doi.org/10.1038/s41598-018-19714-2

The histamine H1-receptor (H1R) is an important mediator of allergy and inflammation. H1R antagonists have particular clinical utility in allergic rhinitis and urticaria. Here we have developed six novel fluorescent probes for this receptor that are... Read More about Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells.

Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position (2018)
Journal Article
Cousin, D., Hummersone, M., Bradshaw, T. D., Zhang, J., Moody, C. J., Foreiter, M., Summers, H., Lewis, W., Wheelhouse, R., & Stevens, M. F. (in press). Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position. MedChemComm, https://doi.org/10.1039/C7MD00554G

A series of 3-(benzyl-substituted)-imidazo[5,1-d]-1,2,3,5-tetrazines (13) and related derivatives with 3-heteromethyl groups has been synthesised and screened for growth-inhibitory activity in vitro against two pairs of glioma cell lines with temozol... Read More about Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position.

3D extrusion printing of high drug loading immediate release paracetamol tablets (2018)
Journal Article
Khaled, S. A., Alexander, M. R., Wildman, R. D., Wallace, M. J., Sharpe, S., Yoo, J., & Roberts, C. J. (2018). 3D extrusion printing of high drug loading immediate release paracetamol tablets. International Journal of Pharmaceutics, 538(1-2), 223-230. https://doi.org/10.1016/j.ijpharm.2018.01.024

The manufacture of immediate release high drug loading paracetamol oral tablets was achieved using an extrusion based 3D printer from a premixed water based paste formulation. The 3D printed tablets demonstrate that a very high drug (paracetamol) loa... Read More about 3D extrusion printing of high drug loading immediate release paracetamol tablets.

Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway (2018)
Journal Article
Khaled bin Break, M., Hossan, M. S., Khooa, Y., Emad Qazzaz, M., Al-Hayali, M., Chow, S. C., Wiart, C., Bradshaw, T. D., Collins, H., & Khoo, T.-J. (2018). Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway. Fitoterapia, 125, https://doi.org/10.1016/j.fitote.2018.01.006

Nineteen analogues of cardamonin were semi-synthesized and tested against A549 and HK1 cell lines. The analogues were fully characterized via IR and NMR analyses, while compound 19 (a Cu (II) complex of cardamonin) was further characterized via HRMS,... Read More about Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway.

Synthetic glycopolymers as modulators of protein aggregation: influence of chemical composition, topology and concentration (2018)
Journal Article
Madeira do Ó, J., Mastrotto, F., Francini, N., Allen, S., van der Walle, C., Stolnik, S., & Mantovani, G. (in press). Synthetic glycopolymers as modulators of protein aggregation: influence of chemical composition, topology and concentration. Journal of Materials Chemistry B, 7(6), https://doi.org/10.1039/c7tb02720f

Novel drug excipients are required to achieve stable formulations of protein drug candidates. Synthetic glycopolymers have been shown in some cases to improve protein formulation stability, although their structure function relationship remains unkno... Read More about Synthetic glycopolymers as modulators of protein aggregation: influence of chemical composition, topology and concentration.

An electrochemical system for the study of trans-plasma membrane electron transport in whole eukaryotic cells (2018)
Journal Article
Sherman, H. G., Jovanovic, C., Stolnik, S., & Rawson, F. J. (in press). An electrochemical system for the study of trans-plasma membrane electron transport in whole eukaryotic cells. Analytical Chemistry, 90(4), https://doi.org/10.1021/acs.analchem.7b04853

The development of new assays to study trans-plasma membrane electron transport (tPMET) in eukaryotic systems is paramount for a number reasons, which include the further understanding of the underlying biology which can then potentially be applied t... Read More about An electrochemical system for the study of trans-plasma membrane electron transport in whole eukaryotic cells.

Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells (2018)
Journal Article
Yang, Z., Wei, D., Liu, F., Liu, J., Wu, X., Stevens, M. F. G., Bradshaw, T. D., Luo, Y., & Zhang, J. (in press). Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells. Journal of Cellular Biochemistry, https://doi.org/10.1002/jcb.26674

The efficacy of temozolomide (TMZ) treatment for cancers is currently limited by inherent or the development of resistance, particularly, but not exclusively, due to the expression of the DNA repair enzyme O6-methylguanine-DNA methyltransferase (MGMT... Read More about Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells.

Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging (2018)
Journal Article
Zamberlan, F., Turyanska, L., Patanè, A., Liu, Z., Williams, H., Fay, M., Clarke, P., Imamura, Y., Jin, T., Bradshaw, T., Thomas, N., & Grabowska, A. (in press). Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging. Journal of Materials Chemistry B, 6, https://doi.org/10.1039/c7tb02912h

The short shelf-life of water-soluble quantum dots (QDs) due to colloidal instability represents a major drawback to their exploitation. This work examines the colloidal stability of PbS nanoparticles capped with dihydrolipoic acid–polyethylene glyco... Read More about Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging.

Identification of novel ‘inks’ for 3D printing using high throughput screening: bioresorbable photocurable polymers for controlled drug delivery (2018)
Journal Article
Louzao, I., Koch, B., Taresco, V., Ruiz Cantu, L., Irvine, D. J., Roberts, C. J., Tuck, C. J., Alexander, C., Hague, R. J., Wildman, R. D., & Alexander, M. R. (in press). Identification of novel ‘inks’ for 3D printing using high throughput screening: bioresorbable photocurable polymers for controlled drug delivery. ACS Applied Materials and Interfaces, 10(8), https://doi.org/10.1021/acsami.7b15677

A robust discovery methodology is presented to identify novel biomaterials suitable for 3D printing. Currently the application of Additive Manufacturing is limited by the availability of functional inks, especially in the area of biomaterials-this me... Read More about Identification of novel ‘inks’ for 3D printing using high throughput screening: bioresorbable photocurable polymers for controlled drug delivery.

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies (2018)
Journal Article
Lam, R., Gondin, A. B., Canals, M., Kellam, B., Briddon, S. J., Graham, B., & Scammells, P. J. (2018). Fluorescently Labeled Morphine Derivatives for Bioimaging Studies. Journal of Medicinal Chemistry, 61(3), 1316-1329. https://doi.org/10.1021/acs.jmedchem.7b01811

Opioids, like morphine, are the mainstay analgesics for the treatment and control of pain. Despite this, they often exhibit severe side effects that limit dose; patients often become tolerant and dependent on these drugs, which remains a major health... Read More about Fluorescently Labeled Morphine Derivatives for Bioimaging Studies.

Post-modified polypeptides with UCST-type behavior for control of cell attachment in physiological conditions (2018)
Journal Article
Xue, X., Thiagarajan, L., Dixon, J. E., Saunders, B. R., Shakesheff, K. M., & Alexander, C. (2018). Post-modified polypeptides with UCST-type behavior for control of cell attachment in physiological conditions. Materials, 11(1), Article 95. https://doi.org/10.3390/ma11010095

Upper Critical Solution Temperature (UCST)-type thermally responsive polypeptides (TRPs) with phase transition temperatures around 37 ◦C in phosphate-buffered saline (PBS) buffer (pH 7.4, 100 mM) were prepared from poly(L-ornithine) hydrobromide and... Read More about Post-modified polypeptides with UCST-type behavior for control of cell attachment in physiological conditions.

Prediction of Broad-Spectrum Pathogen Attachment to Coating Materials for Biomedical Devices (2018)
Journal Article
Dundas, A. A., Mikulskis, P., Hook, A., Dundas, A., Irvine, D., Sanni, O., Anderson, D., Langer, R., Alexander, M. R., Williams, P., & Winkler, D. A. (2018). Prediction of Broad-Spectrum Pathogen Attachment to Coating Materials for Biomedical Devices. ACS Applied Materials and Interfaces, 10(1), 139-149. https://doi.org/10.1021/acsami.7b14197

© 2017 American Chemical Society. Bacterial infections in healthcare settings are a frequent accompaniment to both routine procedures such as catheterization and surgical site interventions. Their impact is becoming even more marked as the numbers of... Read More about Prediction of Broad-Spectrum Pathogen Attachment to Coating Materials for Biomedical Devices.