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Browsing School of Chemistry by subject "0304 Medicinal and Biomolecular Chemistry"

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    • Aryl urea substituted fatty acids: a new class of protonophoric mitochondrial uncoupler that utilises a synthetic anion transporter 

      Rawling, Tristan; MacDermott-Opeskin, Hugh; Roseblade, Ariane; Pazderka, Curtis; Clarke, Callum; Bourget, Kirsi; Wu, Xin; Lewis, William; Noble, Benjamin; Gale, Philip A.; O'Mara, Megan L.; Cranfield, Charles; Murray, Michael
      Published 2020
      Respiring mitochondria establish a proton gradient across the mitochondrial inner membrane (MIM) that is used to generate ATP. Protein-independent mitochondrial uncouplers collapse the proton gradient and disrupt ATP ...
      Open Access
      Article
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    • Cubanes in Medicinal Chemistry 

      Reekie, Tristan A.; Williams, Craig M.; Rendina, Louis M.; Kassiou, Michael
      Published 2019
      Cubane is a highly strained saturated hydrocarbon system that has historically been of interest in theoretical organic chemistry. More recently it has become a molecule of interest for biological applications due to its ...
      Open Access
      Article
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    • Cyclisation strategies for stabilising peptides with irregular conformations 

      Vu, Quynh Ngoc; Young, Reginald; Sudhakar, Haritha Krishna; Gao, Tianyi; Huang, Tiancheng; Tan, Yaw Sing
      Published 2021
      Cyclisation is a common synthetic strategy for enhancing the therapeutic potential of peptide-based molecules. While there are extensive studies on peptide cyclisation for reinforcing regular secondary structures such as ...
      Open Access
      Article
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    • Dual-functionalisation of fluorophores for the preparation of targeted and selective probes 

      Trinh, Natalie; Jolliffe, Katrina A; New, Elizabeth J
      Published 2020
      A key current challenge in biological research is the elucidation of the roles that chemicals and chemical reactions play in cellular function and dysfunction. Of the available cellular imaging techniques, ...
      Open Access
      Article
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    • Duale Funktionalisierung von Fluorophoren für die Konstruktion zielgerichteter und selektiver Fluoreszenz-Sensoren 

      Trinh, Natalie; Jolliffe, Katrina A; New, Elizabeth J
      Published 2020
      Eine Schlüsselfrage in der gegenwärtigen biologischen Forschung ist, welche Rolle gewisse Chemikalien und chemische Reaktionen im Zusammenhang mit dem regulären zellulären Betrieb, als auch mit zellulären Störungen spielen. ...
      Open Access
      Article
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    • The effect of charge on the uptake and resistance to reduction of platinum(IV) complexes in human serum and whole blood models 

      Hambley, Trevor; Chen, Catherine; Gui, Xiao; Kappen, Peter; Renfrew, Anna
      Published 2020
      cis- and trans-Platinum(IV) complexes with diaminetetracarboxylate coordination spheres possess the highly desirable property of exhibiting unusual resistance to reduction by blood serum components and endogenous reductants ...
      Open Access
      Article
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    • Element 5 – Boron 

      Rendina, Louis M.
      Published 2019
      2019 is the International Year of the Periodic Table of Chemical Elements (IYPT 2019), as declared by the United Nations General Assembly. This invited paper on boron is one in a series of essays about the chemical elements.
      Open Access
      Article
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    • Elucidating the Roles of Fenton Reactants in Drug-Treated Cells using a Selective Rhodamine-Thiophenol Fluorogenic Sensor 

      Wang, Zhanlong; Yeo, Jia Hao; New, Elizabeth J
      Published 2021
      While Fenton chemistry has long been known to play a role in inducing cellular stress, there has been recent renewed interest in understanding its roles in health and disease. Here we describe a fluorogenic probe, RTFt1, ...
      Open Access
      Article
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    • Encapsulin Nanocompartments for Biomanufacturing Applications 

      Szyszka, Taylor; Adamson, Lachlan; Lau, Yu Heng
      Published 2022
      Enzyme scaffolding is an emerging technique for enhancing yield and efficiency of biomanufacturing processes for generating high-value products. Of the many scaffolds available for in vivo and cell-free applications, ...
      Open Access
      Book chapter
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    • Gadolinium theranostics for the diagnosis and treatment of cancer 

      Robertson, Amy G.; Rendina, Louis M.
      Published 2021
      According to the World Health Organization (WHO), there were 18.1 million new cancer cases and 9.6 million cancer deaths reported worldwide in 2018. These numbers are expected to rise over the next decade, and the ...
      Open Access
      Article
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    • Histone Deacetylase 2 (HDAC2) Inhibitors Containing Boron 

      Kavianpour, Poya; Gemmell, Madeleine C. M.; Kahlert, Jan U.; Rendina, Louis M.
      Published 2020
      Histone deacetylase enzymes (HDACs) are responsible for the global silencing of tumour‐suppressor genes. Treatment with a histone deacetylase inhibitor (HDACi) can reverse this process and restore normal cell function. ...
      Open Access
      Article
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    • How Pore Architecture Regulates the Function of Nanoscale Protein Compartments 

      Tasneem, Nuren; Szyszka, Taylor; Jenner, Eric; Lau, Yu Heng
      Published 2022
      Self-assembling proteins can form porous compartments that adopt well-defined architectures at the nanoscale. In nature, protein compartments act as semipermeable barriers to enable spatial separation and organization of ...
      Open Access
      Article
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    • The impact of highly electron withdrawing carboxylato ligands on the stability and activity of platinum(IV) pro-drugs 

      Hambley, Trevor; Chen, Catherine
      Published 2019
      Recent developments in the design of platinum(IV) pro-drug candidates have demonstrated the importance of the coordination sphere of the complex in determining the resistance to reduction by endogenous reductants and the ...
      Open Access
      Article
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    • Nicotinamide-appended fluorophores as fluorescent redox sensors 

      Leslie, Kathryn G; Kolanowski, Jacek L; Trinh, Natalie; Carrara, Serena; Anscomb, Matthew D; Yang, Kylie; Hogan, Conor F; Jolliffe, Katrina A; New, Elizabeth J
      Published 2019
      Fluorescent sensors have proved invaluable in elucidating the regulation and dysregulation of redox processes in biology, but understanding of the breadth of biological redox reactions requires development of new sensors ...
      Open Access
      Article
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    • Nonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials 

      Tse, Edwin G.; Houston, Sevan D.; Williams, Craig M.; Savage, G. Paul; Rendina, Louis M.; Hallyburton, Irene; Anderson, Mark; Sharma, Raman; Walker, Gregory S.; Obach, R. Scott; Todd, Matthew H.
      Published 2020
      The replacement of one chemical motif with another that is broadly similar is a common method in medicinal chemistry to modulate the physical and biological properties of a molecule (i.e., bioisosterism). In recent years, ...
      Open Access
      Article
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    • Order-disorder transitions of cytoplasmic N-termini in the mechanisms of P-type ATPases 

      Hossain, Khondker Rufaka; Clayton, Daniel; Goodchild, Sophia C; Rodger, Alison; Payne, Richard James; Cornelius, Flemming; Ronald, James Clarke
      Published 2020-01-01
      Membrane protein structure and function are modulated via interactions with their lipid environment. This is particularly true for the integral membrane pumps, the P-type ATPases. These ATPases play vital roles in cell ...
      Article
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    • Strategies for organelle targeting of fluorescent probes 

      Lin, Jiarun; Yang, Kylie; New, Elizabeth J
      Published 2021
      Fluorescent tools have emerged as an important tool for studying the distinct chemical microenvironments of organelles, due to their high specificity and ability to be used in non-destructive, live cellular ...
      Open Access
      Article
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    • Studies of the labile lead pool using a rhodamine-based fluorescent probe 

      Zhu, Jianping; Yeo, Jia Hao; Bower, Amy A; Proschogo, Nicholas; New, Elizabeth J
      Published 2020
      Lead is a heavy metal which has long been known to have toxic effects on the body. However, much remains to be learnt about the labile lead pool and cellular uptake of lead. We report here RPb1 that undergoes a 100-fold ...
      Open Access
      Article
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    • Synthesis and tumour cell uptake studies of gadolinium(III)–phosphonium complexes 

      Hall, Andrew J.; Robertson, Amy G.; Hill, Leila R.; Rendina, Louis M.
      Published 2021
      The synthesis of a new series of Gd(III)-arylphosphonium complexes is described and the solution stability of selected compounds is reported. Their lipophilicity and uptake in human glial (SVG p12) and human glioblastoma ...
      Open Access
      Article
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    • Synthesis of nitro-aryl functionalised 4-amino-1,8-naphthalimides and their evaluation as fluorescent hypoxia sensors 

      Adair, Liam D; Trinh, Natalie; Vérité, Pauline M; Jacquemin, Denis; Jolliffe, Katrina A; New, Elizabeth J
      Published 2020
      Fluorescent sensors are a vital research tool, enabling the study of intricate cellular processes in a sensitive manner. The design and synthesis of responsive and targeted probes is necessary to allow such processes to ...
      Open Access
      Article
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