Andrew Sutherland
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Longitudinal [18F]LW223 PET imaging of macrophage-driven inflammation following myocardial infarction in a rat model: implications for left ventricular remodelling Open
Purpose Inflammation affects cardiac remodelling following myocardial infarction (MI), and can be imaged using Positron Emission Tomography (PET) targeting the 18 kDa translocator protein (TSPO). We utilised a rat reperfusion MI model to a…
Synthesis and evaluation of enantiomeric quinoline-2-carboxamides: positron emission tomography imaging agents for the translocator protein Open
Synthesis and biological testing of the R - and S -enantiomers of LW223, a third generation TSPO PET imaging agent using human brain tissue showed that despite a 7.5-fold difference in affinity, both are insensitive to rs6971 polymorphism.
Performance evaluation of the nanoScan® P123S total-body PET Open
Purpose Before utilising preclinical Position Emission Tomography (PET) systems for biological studies, evaluating their performance is important to better qualify the scanner’s applications. This study aims to assess the performance of th…
One-Pot Synthesis of Alkynyl-Conjugated Phenylalanine Analogues for Peptide-Based Fluorescent Imaging Open
A series of unnatural amino acids featuring conjugated aryl-alkyne side chains was synthesized from tyrosine via a one-pot hydroxyl group activation and copper-free Sonogashira cross-coupling. This efficient strategy enabled rapid access t…
Iron-Catalyzed Thioarylation of Arenes Using Saccharin-Derived Reagents Open
Biaryl sulfides are important scaffolds found in various natural products and pharmaceutically active compounds. One of the main approaches for the synthesis of this compound class involves the substitution of arenes using electrophilic th…
Synthesis of Fluorescent Dibenzofuran α-Amino Acids: Conformationally Rigid Analogues of Tyrosine Open
We report two synthetic strategies for the preparation of dibenzofuran α-amino acids, expanding the structural toolbox of fluorescent probes. The strategies involved dibenzofuran synthesis via a Pd(II)-catalyzed C-O cyclization, alongside …
Environment-sensitive fluorescent tryptophan analogues <i>via</i> indole C-2 alkenylation reactions Open
A synthetic approach for the C-2 alkenylation of tryptophan has been developed, leading to the discovery of an environment-sensitive fluorescent probe that can be excited via two-photon absorption in the near-infrared.
Expanding the fluorescence toolkit: molecular design, synthesis and biological application of unnatural amino acids Open
This perspective describes recent advances in the discovery of fluorescent unnatural amino acids as intrinsic peptidic probes for the minimally invasive measurement, sensing and imaging of biological processes.
Expedient discovery of fluorogenic amino acid-based probes <i>via</i> one-pot palladium-catalysed arylation of tyrosine Open
A one-pot palladium-catalysed arylation process has been used to expedite the synthesis of biaryl α-amino acids, leading to the discovery of an environment-sensitive fluorescent probe that was used to monitor the activity of a serine prote…
Synthesis and evaluation of 6-arylaminobenzamides as positron emission tomography imaging ligands for the sphingosine-1-phosphate-5 receptor Open
A series of fluorinated 6-arylaminobenzamides have been shown to be selective and potent agonists of the sphingosine-1-phosphate-5 receptor. Radiofluorination and PET imaging with the lead compound showed fast uptake in rat brain and spina…
View article: Collaborative Care Model for Patients With Opioid Use Disorder and Mental Illness
Collaborative Care Model for Patients With Opioid Use Disorder and Mental Illness Open
This cohort study uses data from a randomized clinical trial for opioid use disorder (OUD) co-occurring with mental illness to examine patient characteristics associated with collaborative care model engagement and fidelity.
Quantification of extra-cardiac damage following acute myocardial infarction using cis- and trans-4-[18F]fluoro-L-proline PET imaging Open
The preclinical surgically-induced models of myocardial infarction (MI) have been extensively utilised for studying the wound healing response in the mammalian heart. It is well-established that these invasive procedures induce marked acut…
View article: Key roles of C2/GAP domains in SYNGAP1-related pathophysiology
Key roles of C2/GAP domains in SYNGAP1-related pathophysiology Open
Mutations in SYNGAP1 are a common genetic cause of intellectual disability (ID) and a risk factor for autism. SYNGAP1 encodes a synaptic GTPase-activating protein (GAP) that has both signaling and scaffolding roles. Most pathogenic variant…
Ultrasensitive Raman Detection of Biomolecular Conformation at the Attomole Scale using Chiral Nanophotonics Open
Understanding the function of a biomolecule hinges on its 3D conformation or secondary structure. Chirally sensitive, optically active techniques based on the differential absorption of UV–vis circularly polarized light excel at rapid char…
Stereoselective Synthesis of <i>meso</i>- and <span>l</span>,<span>l</span>-Diaminopimelic Acids from Enone-Derived α-Amino Acids Open
The stereoselective synthesis of meso-diaminopimelic acid (meso-DAP), the key cross-linking amino acid of the peptidoglycan cell wall layer in Gram-negative bacteria, and its biological precursor, l,l-DAP, is described. The key step involv…
Correction to: Modelling [18F]LW223 PET data using simplified imaging protocols for quantification of TSPO expression in the rat heart and brain Open
Correct Figure 5: Figure 5.The impact of PET scan duration truncation on 2TCM parameter accuracy in all datasets.a) Correlation between K 1 calculated using a 120 min PET scan duration and 5 other truncated durations.b) The same is shown f…
View article: Synthesis of β-Pyridyl α-Amino Acids: Conformationally Sensitive Charge Transfer-Based Fluorophores
Synthesis of β-Pyridyl α-Amino Acids: Conformationally Sensitive Charge Transfer-Based Fluorophores Open
Unnatural α-amino acids with charge transfer-based poly aromatic side chains have been designed as conformationally sensitive fluorophores. These were prepared using a hetero-Diels-Alder reaction and a Knoevenagel-Stobbe process to generat…
RWOP4 Exploring age- and sex-dependent dynamics in cardiac collagen synthesis through non-invasive PET imaging Open
Age, a key cardiovascular disease risk factor, leads to collagen accumulation, driving age-dependent cardiac remodelling. Sex differences in cardiac health are noted, with females more resistant to age-related collagen accumulation until m…
Ligand-Enabled Copper-Mediated Radioiodination of Arenes Open
The discovery of a copper precatalyst that facilitates the key mechanistic steps of arene halodeboronation has allowed a step change in the synthesis of radioiodine-containing arenes. The active precatalyst [Cu(OAc)(phen)2]OAc was shown to…
Correction: Hot off the Press Open
Correction for ‘Hot off the Press’ by Robert A. Hill et al. , Nat. Prod. Rep. , 2023, 40 , 1816–1821, https://doi.org/10.1039/d3np90052e.
Fluorescent carbazole-derived α-amino acids: structural mimics of tryptophan Open
Unnatural α-amino acids bearing carbazole side-chains have been shown to be effective structural mimics of tryptophan in peptides and valuable fluorescent probes for the analysis of protein–protein interactions.
Trifluoromethylthiolation of Arenes Using Lewis Acid and Lewis Base Dual Catalysis Open
Incorporation of the highly lipophilic trifluoromethanesulfenyl group into bioactive molecules facilitates transport through lipid membranes, and thus, CF3S-containing compounds are important for drug discovery. Although reagents and proce…
CCDC 2305671: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
Sexually dimorphic murine brain uptake of the 18 kDa translocator protein PET radiotracer [18F]LW223 Open
The 18 kDa translocator protein is a well-known biomarker of neuroinflammation, but also plays a role in homeostasis. PET with 18 kDa translocator protein radiotracers [11C]PBR28 in humans and [18F]GE180 in mice has demonstrated sex-depend…
Synthesis of Thiazoloindole α-Amino Acids: Chromophores Amenable to One- and Two-Photon Induced Fluorescence Open
Thiazoloindole α-amino acids have been synthesized in four steps from tryptophan using a dual-catalytic thiolation reaction and a copper-mediated intramolecular N-arylation process. Late-stage diversification of the thiazoloindole core wit…
[<sup>18</sup>F]LW223 has low non-displaceable binding in murine brain, enabling high sensitivity TSPO PET imaging Open
Neuroinflammation is associated with a number of brain diseases, making it a common feature of cerebral pathology. Among the best-known biomarkers for neuroinflammation in Positron Emission Tomography (PET) research is the 18 kDa transloca…