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Outputs (6)

Synthesis and vectorial functionalisation of pyrazolo[3,4- c ]pyridines (2023)
Journal Article
Bedwell, E. V., da Silva Emery, F., Clososki, G. C., & Steel, P. G. (2023). Synthesis and vectorial functionalisation of pyrazolo[3,4- c ]pyridines. RSC Advances, 13(49), 34391-34399. https://doi.org/10.1039/d3ra07458g

Heterocycles are a cornerstone of fragment-based drug discovery (FBDD) due to their prevalence in biologically active compounds. However, novel heterocyclic fragments are only valuable if they can be suitably elaborated to compliment a chosen target... Read More about Synthesis and vectorial functionalisation of pyrazolo[3,4- c ]pyridines.

Inhibition of HSP90 distinctively modulates the global phosphoproteome of Leishmania mexicana developmental stages (2023)
Journal Article
Porta, E. O., Gao, L., Denny, P. W., Steel, P. G., & Kalesh, K. (2023). Inhibition of HSP90 distinctively modulates the global phosphoproteome of Leishmania mexicana developmental stages. Microbiology Spectrum, https://doi.org/10.1128/spectrum.02960-23

Heat shock protein 90 (HSP90) is an evolutionarily conserved chaperone protein that plays a central role in the folding and maturation of a large array of client proteins. In the unicellular parasite Leishmania, the etiological agent of the neglected... Read More about Inhibition of HSP90 distinctively modulates the global phosphoproteome of Leishmania mexicana developmental stages.

Assessing Dose-Exposure-Response Relationships of Miltefosine in Adults and Children using Physiologically-Based Pharmacokinetic Modeling Approach. (2023)
Journal Article
Madu, S. J., Wang, K., Chirumamilla, S. K., Turner, D. B., Steel, P. G., & Li, M. (2023). Assessing Dose-Exposure-Response Relationships of Miltefosine in Adults and Children using Physiologically-Based Pharmacokinetic Modeling Approach. Pharmaceutical Research, 40, 2983-3000. https://doi.org/10.1007/s11095-023-03610-0

Miltefosine is the first and only oral medication to be successfully utilized as an antileishmanial agent. However, the drug is associated with differences in exposure patterns and cure rates among different population groups e.g. ethnicity and age (... Read More about Assessing Dose-Exposure-Response Relationships of Miltefosine in Adults and Children using Physiologically-Based Pharmacokinetic Modeling Approach..

Disruption of the inositol phosphorylceramide synthase gene affects Trypanosoma cruzi differentiation and infection capacity (2023)
Journal Article
Dos Santos, N. S. A., Estevez-Castro, C. F., Macedo, J. P., Chame, D. F., Castro-Gomes, T., Santos-Cardoso, M., …Teixeira, S. M. R. (2023). Disruption of the inositol phosphorylceramide synthase gene affects Trypanosoma cruzi differentiation and infection capacity. PLoS Neglected Tropical Diseases, 17(9), Article e0011646. https://doi.org/10.1371/journal.pntd.0011646

Sphingolipids (SLs) are essential components of all eukaryotic cellular membranes. In fungi, plants and many protozoa, the primary SL is inositol-phosphorylceramide (IPC). Trypanosoma cruzi is a protozoan parasite that causes Chagas disease (CD), a c... Read More about Disruption of the inositol phosphorylceramide synthase gene affects Trypanosoma cruzi differentiation and infection capacity.

Navigating drug repurposing for Chagas disease: advances, challenges, and opportunities (2023)
Journal Article
Porta, E. O. J., Kalesh, K., & Steel, P. G. (2023). Navigating drug repurposing for Chagas disease: advances, challenges, and opportunities. Frontiers in Pharmacology, 14(2023), https://doi.org/10.3389/fphar.2023.1233253

Chagas disease is a vector-borne illness caused by the protozoan parasite Trypanosoma cruzi (T. cruzi). It poses a significant public health burden, particularly in the poorest regions of Latin America. Currently, there is no available vaccine, and c... Read More about Navigating drug repurposing for Chagas disease: advances, challenges, and opportunities.