All Outputs (7)

Rapeseed oleosomes facilitate intestinal lymphatic delivery and oral bioavailability of cannabidiol (2024)
Journal Article
Ji, L., Feng, W., Chen, H., Chu, Y., Wong, A., Zhu, Y., Sinatra, G., Bramante, F., Carrière, F., Stocks, M. J., di Bari, V., Gray, D. A., & Gershkovich, P. (2025). Rapeseed oleosomes facilitate intestinal lymphatic delivery and oral bioavailability of cannabidiol. International Journal of Pharmaceutics, 668, Article 124947. https://doi.org/10.1016/j.ijpharm.2024.124947

Due to high lipophilicity and extensive first-pass metabolic loss, cannabidiol (CBD) has low oral bioavailability. Co-administration of CBD and long-chain lipids facilitates the intestinal lymphatic delivery, resulting in higher systemic bioavailabil... Read More about Rapeseed oleosomes facilitate intestinal lymphatic delivery and oral bioavailability of cannabidiol.

Delivery of imiquimod to intestinal lymph nodes following oral administration (2024)
Journal Article
Chen, H., Ji, L., Wong, A., Chu, Y., Feng, W., Zhu, Y., Wang, J., Comeo, E., Kim, D.-H., Stocks, M. J., & Gershkovich, P. (2024). Delivery of imiquimod to intestinal lymph nodes following oral administration. International Journal of Pharmaceutics, 667, Article 124895. https://doi.org/10.1016/j.ijpharm.2024.124895

Intestinal lymph nodes are involved in the progression of colorectal cancer (CRC). Tumours suppress the activation of dendritic cells (DCs) in draining lymph nodes, diminishing anti-cancer immune response. Imiquimod (IMQ) facilitates DCs activation v... Read More about Delivery of imiquimod to intestinal lymph nodes following oral administration.

Theoretical Study on the Biosynthesis of the Mandapamates: Mechanistic Insights Using Density Functional Theory (2024)
Journal Article
Wang, D., Pattenden, G., Fow, K. L., Stocks, M. J., Hirst, J. D., & Tang, B. (2024). Theoretical Study on the Biosynthesis of the Mandapamates: Mechanistic Insights Using Density Functional Theory. Journal of Organic Chemistry, 89(18), 12946-12956. https://doi.org/10.1021/acs.joc.4c00859

Density functional theory (B3LYP-D3(BJ) and ωB97XD) calculations have been used to assess the stereochemical outcomes of the proposed transannular [4 + 2] cycloaddition pathway for the biosynthesis of mandapamate and isomandapamate from macrocyclic i... Read More about Theoretical Study on the Biosynthesis of the Mandapamates: Mechanistic Insights Using Density Functional Theory.

Design, Synthesis, and Evaluation of a New Chemotype Fluorescent Ligand for the P2Y2 Receptor (2024)
Journal Article
Knight, R., Kilpatrick, L. E., Hill, S. J., & Stocks, M. J. (2024). Design, Synthesis, and Evaluation of a New Chemotype Fluorescent Ligand for the P2Y2 Receptor. ACS Medicinal Chemistry Letters, 15(7), 1127-1135. https://doi.org/10.1021/acsmedchemlett.4c00211

The P2Y2 receptor (P2Y2R) is a target for diseases including cancer, idiopathic pulmonary fibrosis, and atherosclerosis. However, there are insufficient P2Y2R antagonists available for validating P2Y2R function and future drug development. Evaluation... Read More about Design, Synthesis, and Evaluation of a New Chemotype Fluorescent Ligand for the P2Y2 Receptor.

Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein (2024)
Journal Article
Allison, M., Davie, R. L., Mogg, A. J., Hampton, S. L., Emsley, J., & Stocks, M. J. (2024). Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein. ACS Medicinal Chemistry Letters, 15(4), 501–509. https://doi.org/10.1021/acsmedchemlett.3c00572

Hereditary angioedema (HAE), a rare genetic disorder, is associated with uncontrolled plasma kallikrein (PKa) enzyme activity leading to the generation of bradykinin swelling in subcutaneous and submucosal membranes in various locations of the body.... Read More about Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein.

CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans (2024)
Journal Article
White, C. W., Platt, S., Kilpatrick, L. E., Dale, N., Abhayawardana, R. S., Dekkers, S., Kindon, N. D., Kellam, B., Stocks, M. J., Pfleger, K. D. G., & Hill, S. J. (2024). CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans. Science Signaling, 17(828), Article abl3758. https://doi.org/10.1126/scisignal.abl3758

CXCL17 is a chemokine principally expressed by mucosal tissues, where it facilitates chemotaxis of monocytes, dendritic cells, and macrophages and has antimicrobial properties. CXCL17 is also implicated in the pathology of inflammatory disorders and... Read More about CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans.

Design, Synthesis, and Evaluation of New 1H-Benzo[d]imidazole Based PqsR Inhibitors as Adjuvant Therapy for Pseudomonas aeruginosa Infections (2024)
Journal Article
Soukarieh, F., Mashabi, A., Richardson, W., Oton, E. V., Romero, M., Dubern, J.-F., Robertson, S. N., Lucanto, S., Markham-Lee, Z., Sou, T., Kukavica-Ibrulj, I., Levesque, R. C., Bergstrom, C. A., Halliday, N., Kellam, B., Emsley, J., Heeb, S., Williams, P., Stocks, M. J., & Cámara, M. (2024). Design, Synthesis, and Evaluation of New 1H-Benzo[d]imidazole Based PqsR Inhibitors as Adjuvant Therapy for Pseudomonas aeruginosa Infections. Journal of Medicinal Chemistry, 67(2), 1008-1023. https://doi.org/10.1021/acs.jmedchem.3c00973

Pseudomonas aeruginosa is one of the top priority pathogens that requires immediate attention according to the World Health Organisation (WHO). Due to the alarming shortage of novel antimicrobials, targeting quorum sensing (QS), a bacterial cell to c... Read More about Design, Synthesis, and Evaluation of New 1H-Benzo[d]imidazole Based PqsR Inhibitors as Adjuvant Therapy for Pseudomonas aeruginosa Infections.