Lindsay McMurray
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View article: CCDC 2150924: Experimental Crystal Structure Determination
CCDC 2150924: Experimental Crystal Structure Determination Open
View article: A unified “top-down” approach for the synthesis of diverse lead-like molecular scaffolds
A unified “top-down” approach for the synthesis of diverse lead-like molecular scaffolds Open
A "top-down" synthetic approach enabled the step-efficient synthesis of 21 diverse novel molecular scaffolds. The scaffolds were derived from four complex intermediates that had been prepared using cycloaddition chemistry. Scaffold-hopping…
View article: Pharmacological inhibition of MERTK induces in vivo retinal degeneration: a multimodal imaging ocular safety assessment
Pharmacological inhibition of MERTK induces in vivo retinal degeneration: a multimodal imaging ocular safety assessment Open
The receptor tyrosine kinase, MERTK, plays an essential role in homeostasis of the retina via efferocytosis of shed outer nuclear segments of photoreceptors. The Royal College of Surgeons rat model of retinal degeneration has been linked t…
View article: Optimization of an Imidazo[1,2-<i>a</i>]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with <i>In Vivo</i> Efficacy
Optimization of an Imidazo[1,2-<i>a</i>]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with <i>In Vivo</i> Efficacy Open
Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncology therapeutics by restoring the innate immune response in the tumor microenvironment. Highly selective dual Mer/Axl k…
View article: Synthesis and Assessment of Novel Probes for Imaging Tau Pathology in Transgenic Mouse and Rat Models
Synthesis and Assessment of Novel Probes for Imaging Tau Pathology in Transgenic Mouse and Rat Models Open
Aggregated tau protein is a core pathology present in several neurodegenerative diseases. Therefore, the development and application of positron emission tomography (PET) imaging radiotracers that selectively bind to aggregated tau in fibr…
View article: Generating Selective Leads for Mer Kinase Inhibitors—Example of a Comprehensive Lead-Generation Strategy
Generating Selective Leads for Mer Kinase Inhibitors—Example of a Comprehensive Lead-Generation Strategy Open
Mer is a member of the TAM (Tyro3, Axl, Mer) kinase family that has been associated with cancer progression, metastasis, and drug resistance. Their essential function in immune homeostasis has prompted an interest in their role as modulato…
View article: Linked PDF of Table of Contents
Linked PDF of Table of Contents Open
visible light photocatalyst simple carboxylic acid or complex drug-like substrate medicinally
View article: Radiosynthesis of (<i>R</i>,<i>S</i>)‐[<sup>18</sup>F]GE387: A Potential PET Radiotracer for Imaging Translocator Protein 18 kDa (TSPO) with Low Binding Sensitivity to the Human Gene Polymorphism rs6971
Radiosynthesis of (<i>R</i>,<i>S</i>)‐[<sup>18</sup>F]GE387: A Potential PET Radiotracer for Imaging Translocator Protein 18 kDa (TSPO) with Low Binding Sensitivity to the Human Gene Polymorphism rs6971 Open
Translocator protein (TSPO) is a biomarker of neuroinflammation, which is a hallmark of many neurodegenerative diseases and has been exploited as a positron emission tomography (PET) target. Carbon‐11‐labelled PK11195 remains the most appl…
View article: Front Cover: [<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography (ChemMedChem 2/2018)
Front Cover: [<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography (ChemMedChem 2/2018) Open
The Front Cover shows the in vivo evaluation of a prospective radioligand for cPLA2a, a biomarker for neuroinflammation, in a mouse brain by positron emission tomography (PET). In order to reversibly bind to the enzyme target, the 11C-labe…
View article: [<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography
[<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography Open
Cytosolic phospholipase A2α (cPLA2α) may play a critical role in neuropsychiatric and neurodegenerative disorders associated with oxidative stress and neuroinflammation. An effective PET radioligand for imaging cPLA2α in living brain might…