Louis Allott

Louis Allott
University of Hull · Department of Biomedical Sciences

PhD

About

29
Publications
2,598
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253
Citations
Introduction
Establishing a research group at The University of Hull to develop new radiochemistry and automated synthesis methods for translating radiopharmaceuticals into the clinic.

Publications

Publications (29)
Article
The automation of positron emission tomography (PET) radiochemistry using cassette-based automated radiosynthesis platforms is an essential component of clinical translation for the vast majority of 18F-based radiopharmaceuticals. The technology is widely adopted by good manufacturing practice (GMP) compliant radiopharmaceutical production faciliti...
Article
The production of 18F-labelled microbubbles (MBs) via the aluminium-[18F]fluoride ([18F]AlF) radiolabelling method and facile inverse-electron-demand Diels-Alder (IEDDA) 'click' chemistry is reported. An [18F]AlF-NODA-labelled tetrazine was synthesised in excellent radiochemical yield (>95% RCY) and efficiently conjugated to a trans-cyclooctene (TC...
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Full-text available
The aluminium-[¹⁸F]fluoride ([¹⁸F]AlF) radiolabelling method combines the favourable decay characteristics of fluorine-18 with the convenience and familiarity of metal-based radiochemistry and has been used to parallel gallium-68 radiopharmaceutical developments. As such, the [¹⁸F]AlF method is popular and widely implemented in the development of r...
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Hypoxia is a complex microenvironmental condition known to regulate choline kinase α (CHKA) activity and choline transport through transcription factor hypoxia-inducible factor-1α (HIF-1α) and, therefore, may confound the uptake of choline radiotracer [18F]fluoromethyl-[1,2-2H4]-choline ([18F]-D4-FCH). The aim of this study was to investigate how h...
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Choline kinase alpha (CHKA) is a promising target for the development of cancer therapeutics. We have previously reported ICL-CCIC-0019, a potent CHKA inhibitor with high cellular activity but with some unfavorable pharmacological properties. In this work, we present an active analogue of ICL-CCIC-0019 bearing a piperazine handle (CK146) to facilit...
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Full-text available
Background: Reprogrammed cellular metabolism is a cancer hallmark. In addition to increased glycolysis, the oxidation of acetate in the citric acid cycle is another common metabolic phenotype. We have recently developed a novel fluorine-18-labelled trimethylacetate-based radiotracer, [18F]fluoro-pivalic acid ([18F]FPIA), for imaging the transcellu...
Article
We have exemplified a pretargeted approach to interrogate hypoxia in live cells using radioactive bioorthogonal inverse electron demand Diels–Alder (IEDDA) “click” chemistry. Our novel 18F-tetrazine probe ([18F]FB-Tz) and 2-nitroimidazole-based TCO targeting molecule (8) showed statistically significant (P < 0.0001) uptake in hypoxic cells (ca. 90...
Article
The use of biologics in positron emission tomography (PET) imaging is an important area of radiopharmaceutical development and new automated methods are required to facilitate their production. We report an automated radiosynthesis method to produce a radiolabelled biologic via facile inverse electron demand Diels-Alder (IEDDA) "click" chemistry on...
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The squaryl moiety has emerged as an important phosphate bioisostere with reportedly greater cell permeability. It has been used in the synthesis of several therapeutic drug molecules including nucleoside and nucleotide analogues but is yet to be evaluated in the context of positron emission tomography (PET) imaging. We have designed, synthesised a...
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Background Fatty acids derived de novo or taken up from the extracellular space are an essential source of nutrient for cell growth and proliferation. Radiopharmaceuticals including 11C-acetate, and 18F-FAC (2-18F-fluoroacetate), have previously been used to study short-chain fatty acid (SCFA) metabolism. We developed 18F-fluoropivalate (18F-FPIA;...
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Background: Glycogen is a multibranched polysaccharide of glucose produced by cells to store energy and plays a key role in cancer. A previously reported fluorescent probe (CDg4) was shown to selectively bind glycogen in mouse embryonic stem cells, however the molecule was not evaluated in cancer cells. We report the synthesis and biological evalu...
Article
Positron emission tomography (PET) has proven to be an invaluable tool in the staging and management of disease in oncology; however, [¹⁸F]fluorodeoxyglucose ([¹⁸F]FDG) remains the most widely used PET radiopharmaceutical despite large financial investment in novel radiotracer development. We report our perspective and experience of translating rad...
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The success of Lutathera™ ([177Lu]Lu-DOTA-TATE) in the NETTER-1 clinical trial as a peptide receptor radionuclide therapy (PRRT) for somatostatin receptor expressing (SSTR) neuroendocrine tumours (NET) is likely to increase the demand for patient stratification by positron emission tomography (PET). The current gold standard of gallium-68 radiolabe...
Article
A solid-supported cyanoborohydride cartridge was designed to facilitate the automated production of positron emission tomography (PET) radiotracers synthesised via reductive amination chemistry. Two model compounds ([¹⁸F]1 and [¹⁸F]2) were radiolabelled efficiently using the GE FASTLab™ platform, accessed in >98% RCP in a total synthesis time of 75...
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Full-text available
Background. The histological evaluation of estrogen receptor (ER) and progesterone receptor (PR) expression in breast cancer lesions from biopsy tissue can stratify patients to receive endocrine therapy. Furthermore, PR expression can predict response to selective estrogen receptor modulators (SERMs). Current immunohistochemical approaches to PR de...
Article
The fluorine-18 radiolabelled octreotide derivative [18F]FET-βAG-TOCA targeting somatostatin receptor type 2, has been evaluated clinically for positron emission tomography (PET) imaging of neuroendocrine tumours (NETs). We report an improved automated radiosynthesis of [18F]FET-βAG-TOCA with several advantages over the current automated GMP synthe...
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In head and neck squamous cell carcinoma (HNSCC), the human epidermal growth factor receptor 1 (EGFR) is the dominant signaling molecule among all members of the family. So far, cetuximab is the only approved anti-EGFR mAb used for the treatment of HNSCC, but despite the benefits of adding it to standard treatment regimens, attempts to define a pre...
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Purpose: Recent studies have highlighted a role of human epidermal growth factor receptor 3 (HER3) in HER2-driven cancers (e.g. breast cancer) implicating the up-regulation of the receptor in resistance to HER-targeted therapies and Hsp90 inhibitors (e.g. AUY922). Therefore, we have developed an affibody-based PET radioconjugate that quantitativel...
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The future of 89Zr-based immuno-PET is reliant upon the development of new chelators with improved stability compared to the currently used deferoxamine (DFO). Herein, we report the evaluation of the octadentate molecule DFO-HOPO (3) as a suitable chelator for 89Zr and a more stable alternative to DFO. The molecule showed good potential for the fut...
Article
The aluminium fluoride-18 ([18F]AlF) radiolabelling procedure has generated great interest because it is a simple, one-pot method that can be used to directly radiolabel small molecules, peptides and proteins without the requirement for a [18F]fluoride drying step. Reported here is the development of an automated [18F]AlF radiolabelling procedure o...
Article
The human epidermal growth factor receptor 3 (HER3) is over-expressed in several cancers, being linked to a more resistant phenotype and hence poor patient prognosis. Imaging HER3 is challenging owing to the modest receptor number (<50000 receptors/cell) in overexpressing cancer cells. Therefore, to image HER3 in vivo, high target affinity PET prob...
Article
The estrogen receptor (ER) and progesterone receptor (PR) are over-expressed in ∼50% of breast cancer lesions, and used as biomarkers to stratify patients for endocrine therapy. Currently, immunohistochemical (IHC) assessment of these lesions from a core-needle biopsy in deep-sited metastases has limitations associated with sampling error and lack...
Article
Synthesis of the first water soluble porphyrin radiolabeled with fluorine-18 is described. This new molecular theranostic agent is designed to integrate the therapeutic modality of photodynamic therapy (PDT) with the imaging modality of positron emission tomography (PET). The procedure involves the conjugation of a cationic water-soluble porphyrin...
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Full-text available
Steroid hormone receptor (SHR) expression and changes in SHR expression compared to basal levels, whether upregulated, downregulated, or mutated, form a distinguishing feature of some breast, ovarian, and prostate cancers. These receptors act to induce tumor proliferation. In the imaging context, total expression together with modulation of express...
Article
Herein a new (11) C radiolabelling strategy for the fast and efficient synthesis of thioureas and related derivatives using the novel synthon, (11) CS2 , is reported. This approach has enabled the facile labelling of a potent progesterone receptor (PR) agonist, [(11) C]Tanaproget, by the intramolecular reaction of the acyclic aminohydroxyl precurso...

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