Νicholas Barlow
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View article: Altered Glut4, <scp>IRAP</scp> , and Brain Insulin Signaling in a Mouse Model of Epilepsy and Contributions to Glucose Transport in Neurons and Astrocytes
Altered Glut4, <span>IRAP</span> , and Brain Insulin Signaling in a Mouse Model of Epilepsy and Contributions to Glucose Transport in Neurons and Astrocytes Open
There is evidence that glucose transport is impaired between seizures, which can promote seizure generation. In addition to glucose transporters Glut1 and Glut3, Glut4 is also found in the brain. Glut4 translocation is regulated by insulin…
View article: Inhibition of IRAP Enhances the Expression of Pro-Cognitive Markers Drebrin and MAP2 in Rat Primary Neuronal Cells
Inhibition of IRAP Enhances the Expression of Pro-Cognitive Markers Drebrin and MAP2 in Rat Primary Neuronal Cells Open
The insulin-regulated aminopeptidase (IRAP; oxytocinase) is part of the M1 aminopeptidase family and is highly expressed in many tissues, including the neocortex and hippocampus of the brain. IRAP is involved in various physiological funct…
View article: Inhibition of IRAP Enhance the Expression of Pro-cognitive Markers Drebrin and MAP2 in Rat Primary Neuronal Cells
Inhibition of IRAP Enhance the Expression of Pro-cognitive Markers Drebrin and MAP2 in Rat Primary Neuronal Cells Open
The insulin-regulated aminopeptidase (IRAP; oxytocinase) is part of the M1 aminopeptidase family and is highly expressed in many tissues, including the neocortex and hippocampus of the brain. IRAP is involved in various physiological funct…
View article: Targeting HIV-1 Reverse Transcriptase Using a Fragment-Based Approach
Targeting HIV-1 Reverse Transcriptase Using a Fragment-Based Approach Open
Human immunodeficiency virus type I (HIV-1) is a retrovirus that infects cells of the host’s immune system leading to acquired immunodeficiency syndrome and potentially death. Although treatments are available to prevent its progression, H…
View article: The challenges of using live-streamed data in a predictive digital twin
The challenges of using live-streamed data in a predictive digital twin Open
A key component of a digital twin is the monitored data, communicated from the physical system to the virtual representation, for visualization and simulation. Yet little attention has been paid to the practicalities of working with live-s…
View article: Targeting Melanocortin Receptors Using S<sub><i>N</i></sub>Ar-Type Macrocyclization: A Doubly Orthogonal Route to Cyclic Peptide Conjugates
Targeting Melanocortin Receptors Using S<sub><i>N</i></sub>Ar-Type Macrocyclization: A Doubly Orthogonal Route to Cyclic Peptide Conjugates Open
While a range of strategies exist to accomplish peptide macrocyclization, they are frequently limited by the need for orthogonal protection or provide little opportunity for structural diversification. We have evaluated an efficient macroc…
View article: Membrane Permeating Macrocycles: Design Guidelines from Machine Learning
Membrane Permeating Macrocycles: Design Guidelines from Machine Learning Open
The ability to predict cell-permeable candidate molecules has great potential to assist drug discovery projects. Large molecules that lie beyond the Rule of Five (bRo5) are increasingly important as drug candidates and tool molecules for c…
View article: Granzyme K initiates IL-6 and IL-8 release from epithelial cells by activating protease-activated receptor 2
Granzyme K initiates IL-6 and IL-8 release from epithelial cells by activating protease-activated receptor 2 Open
Granzyme K (GzmK) is a tryptic member of the granzyme family of chymotrypsin-like serine proteases produced by cells of the immune system. Previous studies have indicated that GzmK activates protease-activated receptor 1 (PAR1) enhancing a…
View article: IRAP Inhibitors: M1-Aminopeptidase Family Inspiration
IRAP Inhibitors: M1-Aminopeptidase Family Inspiration Open
The insulin regulated aminopeptidase (IRAP) has been proposed as an important therapeutic target for indications including Alzheimer's disease and immune disorders. To date, a number of IRAP inhibitor designs have been investigated but the…
View article: Improving Membrane Permeation in the Beyond Rule-of-Five Space by Using Prodrugs to Mask Hydrogen Bond Donors
Improving Membrane Permeation in the Beyond Rule-of-Five Space by Using Prodrugs to Mask Hydrogen Bond Donors Open
A wide range of drug targets can be effectively modulated by peptides and macrocycles. Unfortunately, the size and polarity of these compounds prevents them from crossing the cell membrane to reach target sites in the cell cytosol. As such…
View article: Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP)
Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP) Open
The IRAP inhibition of the macrocyclic peptide, HA-08 has been explored by analogue design coupled to molecular dynamics analysis.
View article: Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief
Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief Open
Therapeutic targeting of the neurokinin 1 receptor in endosomes provides efficacious and prolonged pain relief.
View article: Antagonism of the proinflammatory and pronociceptive actions of canonical and biased agonists of protease‐activated receptor‐2
Antagonism of the proinflammatory and pronociceptive actions of canonical and biased agonists of protease‐activated receptor‐2 Open
Background and Purpose Diverse proteases cleave protease‐activated receptor‐2 (PAR2) on primary sensory neurons and epithelial cells to evoke pain and inflammation. Trypsin and tryptase activate PAR2 by a canonical mechanism that entails c…