Leonard G. Luyt
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View article: Macroaggregated albumin kits radiolabeled with cyclotron-produced [<sup>68</sup>Ga]GaCl<sub>3</sub> for lung perfusion imaging in healthy pigs and preliminary studies toward radiolabeling with [<sup>89</sup>Zr]ZrCl<sub>4</sub>
Macroaggregated albumin kits radiolabeled with cyclotron-produced [<sup>68</sup>Ga]GaCl<sub>3</sub> for lung perfusion imaging in healthy pigs and preliminary studies toward radiolabeling with [<sup>89</sup>Zr]ZrCl<sub>4</sub> Open
Macroaggregated albumin (MAA) particles bearing a radioactive label are routinely used to assess the lung blood flow during the perfusion phase of ventilation/perfusion scans. Although originally developed for labelling with 99m Tc, MAA ki…
View article: Growth Hormone Secretagogue Receptor (GHSR) Is Elevated in Myocardial Tissues of DMD mdx:utrn−/− Mice, and Correlates Strongly with Inflammatory Markers, and Negatively with Cardiac Function
Growth Hormone Secretagogue Receptor (GHSR) Is Elevated in Myocardial Tissues of DMD mdx:utrn−/− Mice, and Correlates Strongly with Inflammatory Markers, and Negatively with Cardiac Function Open
Dilated cardiomyopathy affects greater than 1 in 2500 patients worldwide, including those with the neuromuscular disorder Duchenne muscular dystrophy (DMD). While inflammation within skeletal muscle is strongly associated with DMD patholog…
View article: A survey of stapling methods to increase affinity, activity, and stability of ghrelin analogues
A survey of stapling methods to increase affinity, activity, and stability of ghrelin analogues Open
In this paper we present a survey of stapling methods for the peptide ghrelin, resulting in the discovery of ghrelin analogues with improved affinity, stability and efficacy.
View article: Cellular Uptake of a Fluorescent Ligand Reveals Ghrelin <i>O</i>-Acyltransferase Interacts with Extracellular Peptides and Exhibits Unexpected Localization for a Secretory Pathway Enzyme
Cellular Uptake of a Fluorescent Ligand Reveals Ghrelin <i>O</i>-Acyltransferase Interacts with Extracellular Peptides and Exhibits Unexpected Localization for a Secretory Pathway Enzyme Open
Ghrelin O-acyltransferase (GOAT) plays a central role in the maturation and activation of the peptide hormone ghrelin, which performs a wide range of endocrinological signaling roles. Using a tight-binding fluorescent ghrelin-derive…
View article: Discovery of Ghrelin(1–8) Analogues with Improved Stability and Functional Activity for PET Imaging
Discovery of Ghrelin(1–8) Analogues with Improved Stability and Functional Activity for PET Imaging Open
The highest affinity ghrelin-based analogue for fluorine-18 positron emission tomography, [Inp1,Dpr3(6-FN),1Nal4,Thr8]ghrelin(1-8) amide (1), has remarkable subnanomolar receptor affinity …
View article: Ghrelin proteolysis increases in plasma of men, but not women, with obesity
Ghrelin proteolysis increases in plasma of men, but not women, with obesity Open
View article: In vivo multimodal imaging of hyaluronan-mediated inflammatory response in articular cartilage
In vivo multimodal imaging of hyaluronan-mediated inflammatory response in articular cartilage Open
View article: A remarkably specific ligand reveals ghrelin<i>O</i>-acyltransferase interacts with extracellular peptides and exhibits unexpected cellular localization for a secretory pathway enzyme
A remarkably specific ligand reveals ghrelin<i>O</i>-acyltransferase interacts with extracellular peptides and exhibits unexpected cellular localization for a secretory pathway enzyme Open
Ghrelin O- acyltransferase (GOAT) plays a central role in the maturation and activation of the peptide hormone ghrelin, which performs a wide range of endocrinological signaling roles. Using a tight-binding fluorescent ghrelin-derived pept…
View article: In vivo multimodal imaging of inflammation in articular cartilage after joint injury
In vivo multimodal imaging of inflammation in articular cartilage after joint injury Open
View article: Targeting Glioblastoma Using a Novel Peptide Specific to a Deglycosylated Isoform of Brevican
Targeting Glioblastoma Using a Novel Peptide Specific to a Deglycosylated Isoform of Brevican Open
Glioblastoma (GBM) is the most common and deadliest form of brain tumor and remains amongst the most difficult cancers to treat. Brevican (Bcan), a central nervous system (CNS)‐specific extracellular matrix protein, is upregulated in high‐…
View article: Regional Differences in the Ghrelin-Growth Hormone Secretagogue Receptor Signalling System in Human Heart Disease
Regional Differences in the Ghrelin-Growth Hormone Secretagogue Receptor Signalling System in Human Heart Disease Open
View article: Regional Differences in the Ghrelin-Growth Hormone Secretagogue Receptor Signalling System in Human Heart Disease
Regional Differences in the Ghrelin-Growth Hormone Secretagogue Receptor Signalling System in Human Heart Disease Open
The hormone ghrelin and its receptor, the growth hormone secretagogue receptor (GHSR) are expressed in myocardium. GHSR binding activates signalling pathways coupled to cardiomyocyte survival and contractility. These properties have made t…
View article: BTP-7, a novel peptide for therapeutic targeting of malignant brain tumors
BTP-7, a novel peptide for therapeutic targeting of malignant brain tumors Open
Background Targeted therapies for malignant brain cancer that are currently available have little clinical activity, highlighting an urgent need for the development of novel precision medicines. Brevican (Bcan), a central nervous system (C…
View article: Author Index
Author Index Open
View article: A Hyaluronan-binding Peptide (P15-1) Reduces Inflammatory and Catabolic Events in IL-1β-treated Human Articular Chondrocytes
A Hyaluronan-binding Peptide (P15-1) Reduces Inflammatory and Catabolic Events in IL-1β-treated Human Articular Chondrocytes Open
View article: A Decade’s Progress in the Development of Molecular Imaging Agents Targeting the Growth Hormone Secretagogue Receptor
A Decade’s Progress in the Development of Molecular Imaging Agents Targeting the Growth Hormone Secretagogue Receptor Open
The growth hormone secretagogue receptor 1a (GHSR), also called the ghrelin receptor, is a G protein-coupled receptor known to play an important metabolic role in the regulation of various physiological processes, including energy expendit…
View article: The development of peptide–boron difluoride formazanate conjugates as fluorescence imaging agents
The development of peptide–boron difluoride formazanate conjugates as fluorescence imaging agents Open
Conjugation of a boron difluoride formazanate dye to receptor targeting peptides provides cancer imaging agents for fluorescence microscopy.
View article: Molecular basis for activation and biased signaling at the thrombin-activated GPCR proteinase activated receptor-4 (PAR4)
Molecular basis for activation and biased signaling at the thrombin-activated GPCR proteinase activated receptor-4 (PAR4) Open
Proteinase-activated receptor (PAR)-4 is a member of the proteolytically-activated PAR family of G-protein-coupled receptors (GPCR) that represents an important target in the development of anti-platelet therapeutics. PARs are activated by…
View article: Nitrone-Modified Gold Nanoparticles: Synthesis, Characterization, and Their Potential as <sup>18</sup> F-Labeled Positron Emission Tomography Probes via I-SPANC
Nitrone-Modified Gold Nanoparticles: Synthesis, Characterization, and Their Potential as <sup>18</sup> F-Labeled Positron Emission Tomography Probes via I-SPANC Open
A novel bioorthogonal gold nanoparticle (AuNP) template displaying interfacial nitrone functional groups for bioorthogonal interfacial strain-promoted alkyne-nitrone cycloaddition reactions has been synthesized. These nitrone-AuNPs were ch…
View article: DDIS-36. BTP-7, A NOVEL PEPTIDE FOR THERAPEUTIC TARGETING OF MALIGNANT BRAIN TUMORS
DDIS-36. BTP-7, A NOVEL PEPTIDE FOR THERAPEUTIC TARGETING OF MALIGNANT BRAIN TUMORS Open
High-grade gliomas are deadly cancers, and current standard-of-care has demonstrated limited success. The ability to specifically target glioma cells allows for the development of safer and more efficacious brain cancer therapy strategies.…
View article: Front Cover: Single Amino Acid Replacement in G‐7039 Leads to a 70‐fold Increase in Binding toward GHS‐R1a (ChemMedChem 20/2019)
Front Cover: Single Amino Acid Replacement in G‐7039 Leads to a 70‐fold Increase in Binding toward GHS‐R1a (ChemMedChem 20/2019) Open
The Front Cover depicts the unique interaction between a tyrosine residue of our peptidomimetic and Arg283 in the binding pocket of the ghrelin receptor. This interaction is the rationale for the subnanomolar binding affinity of our ghreli…
View article: Molecular Basis for G-protein-Coupled Receptor (GPCR) Activation and Biased Signalling at the Platelet Thrombin Receptor Proteinase Activated Receptor-4 (PAR4)
Molecular Basis for G-protein-Coupled Receptor (GPCR) Activation and Biased Signalling at the Platelet Thrombin Receptor Proteinase Activated Receptor-4 (PAR4) Open
Proteinase Activated Receptor-4 (PAR4) is a member of the proteolytically-activated PAR family of G-Protein-coupled Receptors (GPCRs). PARs are activated following proteolytic cleavage of the receptor N-terminus by enzymes such as thrombin…
View article: Nitrone Modified Gold Nanoparticles: Synthesis, Characterization and Their Potential as 18F-Labeled PET Probes via I-SPANC
Nitrone Modified Gold Nanoparticles: Synthesis, Characterization and Their Potential as 18F-Labeled PET Probes via I-SPANC Open
A bioorthogonal gold nanoparticle template displaying interfacial nitrone functional groups for bioorthogonal interfacial strain-promoted alkyne-nitrone cycloaddition (I-SPANC) reactions has been synthesized. The Nitrone-AuNPs were charact…
View article: Nitrone Modified Gold Nanoparticles: Synthesis, Characterization and Their Potential as 18F-Labeled PET Probes via I-SPANC
Nitrone Modified Gold Nanoparticles: Synthesis, Characterization and Their Potential as 18F-Labeled PET Probes via I-SPANC Open
A bioorthogonal gold nanoparticle template displaying interfacial nitrone functional groups for bioorthogonal interfacial strain-promoted alkyne-nitrone cycloaddition (I-SPANC) reactions has been synthesized. The Nitrone-AuNPs were charact…
View article: High Affinity Fluorescent Probe for Proteinase-Activated Receptor 2 (PAR2)
High Affinity Fluorescent Probe for Proteinase-Activated Receptor 2 (PAR2) Open
PAR2 is a proteolytically activated G protein-coupled receptor (GPCR) that is implicated in various cancers and inflammatory diseases. Ligands with low nanomolar affinity for PAR2 have been developed, but there is a paucity of research on …
View article: Dynamics of the Ghrelin/Growth Hormone Secretagogue Receptor System in the Human Heart Before and After Cardiac Transplantation
Dynamics of the Ghrelin/Growth Hormone Secretagogue Receptor System in the Human Heart Before and After Cardiac Transplantation Open
Currently, the early preclinical detection of left ventricular dysfunction is difficult because biomarkers are not specific for the cardiomyopathic process. The underlying molecular mechanisms leading to heart failure remain elusive, highl…
View article: The Chimera That Curbs Appetite
The Chimera That Curbs Appetite Open
A chimeric drug design approach, merging the structure of an antagonist and an inverse agonist, results in a new molecular scaffold for targeting the ghrelin receptor (GHSR).
View article: DDIS-26. BTP-7, A NOVEL PEPTIDE FOR THERAPEUTIC TARGETING OF MALIGNANT BRAIN TUMORS
DDIS-26. BTP-7, A NOVEL PEPTIDE FOR THERAPEUTIC TARGETING OF MALIGNANT BRAIN TUMORS Open
High-grade gliomas are deadly cancers, and current standard-of-care has demonstrated limited success. The ability to specifically target glioma cells can allow for the development of safer and more efficacious brain cancer therapy strategi…
View article: Evidence Supporting a Role for the Blood-Cerebrospinal Fluid Barrier Transporting Circulating Ghrelin into the Brain
Evidence Supporting a Role for the Blood-Cerebrospinal Fluid Barrier Transporting Circulating Ghrelin into the Brain Open
View article: THE GROWTH HORMONE SECRETAGOGUE RECEPTOR, GHRELIN AND BIOCHEMICAL SIGNALING MOLECULES IN HUMAN HEART DISEASE
THE GROWTH HORMONE SECRETAGOGUE RECEPTOR, GHRELIN AND BIOCHEMICAL SIGNALING MOLECULES IN HUMAN HEART DISEASE Open