Holly V. Adcock

Disulfiram metabolite Cu(DDC)2 enhances radionuclide uptake in vivo revealing insights into tumoural ablation resistance

Katie Brookes, Jessica S. Fear, Caitlin E.M. Thornton, Ling Zha et autres

BACKGROUND: Exploitation of the sodium iodide symporter (NIS) has potentially broad clinical application across different tumour ablative settings but often fails in aggressive cancer due to diminished transport activity. We aimed to discover whether enhancing NIS function by modulating proteostasis was targetable …

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Structured Polymers Enable the Sustained Delivery of Glucocorticoids within the Intra‐Articular Space

Ana Crastin, Claire Martin, Shankar Suresh, Scott P Davies et autres

Abstract Intra‐articular glucocorticoid injections are effective in controlling inflammation and pain in arthritides but restricted by short duration of action and risk of joint degeneration. Controlled drug release using biocompatible hydrogels offers a unique solution, but limitations of in situ gelation restrict …

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Exploration of vanoxerine analogues as antibacterial agents

Alexander D. H. Kingdon, Holly V. Adcock, Eleni-Marina Kasimati, Philip G. E. Craven et autres

Mycobacterium tuberculosis is a bacterial pathogen, responsible for approximately 1.3 million deaths in 2022 through tuberculosis infections. The complex treatment regimen required to treat tuberculosis and growing rates of drug resistance, necessitates the development of new anti-mycobacterial agents. One approach is to …

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Tuning the Electronic Properties of Azophosphines as Ligands and Their Application in Base-Free Transfer Hydrogenation Catalysis

Emma J. Jordan, Ethan D. E. Calder, Bethan L. Greene, Holly V. Adcock et autres

High Resolution Image Download MS PowerPoint Slide The design and tuning of new ligands is crucial for unlocking new reactivity at transition metal centers. Azophosphines have recently emerged as a new class of 1,3-P,N ligands in ruthenium piano-stool complexes. This work shows …

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Tuning the Electronic Properties of Azophosphines as Ligands and their Application in Base-Free Transfer Hydrogenation Catalysis

Emma J. Jordan, Ethan D. E. Calder, Bethan L. Greene, Holly V. Adcock et autres

The design and tuning of new ligands is crucial for unlocking new reactivity at transition metal centres. Azophosphines have recently emerged as a new class of 1,3-P,N ligands in ruthenium piano-stool complexes. This work shows that the azophosphine synthesis can tolerate N-aryl …

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Azophosphines: Synthesis, Structure and Coordination Chemistry

Emma J. Jordan, Ethan D. E. Calder, Holly V. Adcock, Louise Male et autres

The conceptual replacement of nitrogen with phosphorus in common organic functional groups unlocks new properties and reactivity. The phosphorus-containing analogues of triazenes are underexplored but offer great potential as flexible and small bite-angle ligands. This manuscript explores the synthesis and characterisation of …

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Dual agonism of sodium iodide symporter function in vivo

Katie Brookes, Caitlin E.M. Thornton, Ling Zha, Jana Kim et autres

Abstract New approaches are urgently needed to enhance the radioiodide (RAI) ablation of aggressive and metastatic thyroid cancer. We recently discovered that valosin-containing protein inhibitors (VCPi) such as clotrimazole and disulfiram transiently block sodium iodide symporter (NIS) proteasomal degradation, hence promoting RAI …

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Azophosphines: Synthesis, Structure and Coordination Chemistry

Emma J. Jordan, Ethan D. E. Calder, Holly V. Adcock, Louise Male et autres

The conceptual replacement of nitrogen with phosphorus in common organic functional groups unlocks new properties and reactivity. The phosphorus-containing analogues of triazenes are underexplored but offer great potential as flexible and small bite-angle ligands. This manuscript explores the synthesis and characterisation of …

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Academic drug discovery: Challenges and opportunities

Angela J. Murray, Liam R. Cox, Holly V. Adcock, Ruth Angela Roberts

There are many different approaches to drug discovery in academia, some of which are based broadly on the industrial model of discovering novel targets and then conducting screening within academic drug discovery centres to identify hit molecules. Here we describe our approach …

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Clinical Implications of Dually Targeting the Sodium Iodide Symporter in Canonical and Non-Canonical Settings

Katie Brookes, Caitlin E.M. Thornton, Ling Zha, Jana Kim et autres

Drug repurposing identifies inhibitors of the proteostasis network to augment radioiodine uptake in combinatorial approaches targeting thyroid cancer

Martin L. Read, Katie Brookes, Alice Fletcher, Caitlin E.M. Thornton et autres

New combinatorial drug strategies are urgently needed to improve radioiodine (RAI) uptake and efficiently ablate thyroid cancer cells, thereby reducing the risk of recurrent disease. Drug repurposing offers the promise of identifying already approved compounds capable of inducing sodium iodide symporter (NIS) …

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OR28-03 Drug Repurposing Identifies Inhibitors of the Proteostasis Network to Augment Radioiodine Uptake in Combinatorial Approaches Targeting Thyroid Cancer

Martin L. Read, Katie Brookes, Alice Fletcher, Caitlin E.M. Thornton et autres

Abstract New combinatorial drug strategies are urgently needed to improve radioiodine (RAI) uptake and efficiently ablate thyroid cancer cells, thereby reducing the risk of recurrent disease. Drug repurposing offers the promise of identifying already approved compounds capable of inducing sodium iodide symporter …

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