John F. Fay
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View article: State-dependent release of extracellular particles with distinct α2,6-sialylation patterns and small RNA cargo related to neuroinflammation
State-dependent release of extracellular particles with distinct α2,6-sialylation patterns and small RNA cargo related to neuroinflammation Open
Neuroinflammation is a significant contributor to neurodegenerative diseases, including Alzheimer’s disease, Parkinson’s disease, and related dementias; yet peripheral biomarkers for neuroinflammation remain an unmet medical need. Microgli…
View article: Exploring Size Exclusion Chromatography Columns 20 and 35 nm Pore Size Effect for Isolation of Extracellular Vesicles
Exploring Size Exclusion Chromatography Columns 20 and 35 nm Pore Size Effect for Isolation of Extracellular Vesicles Open
Extracellular vesicles (EVs) have shown great promise as minimally invasive biomarkers for a variety of diseases. However, challenges persist regarding EV isolation, particularly in their co-isolation with impurities such as soluble protei…
View article: Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Biological and Pharmacological Profiling
Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Biological and Pharmacological Profiling Open
Severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) continues to be a global threat due to its ability to evolve and generate new subvariants, leading to new waves of infection. Additionally, other coronaviruses like Middle E…
View article: Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Bio-Logical and Pharmacological Profiling
Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Bio-Logical and Pharmacological Profiling Open
Severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) continues to be a global threat due to its ability to evolve and generate new subvariants, leading to new waves of infection. Additionally, other coronaviruses like Middle E…
View article: Structure, function and pharmacology of human itch GPCRs
Structure, function and pharmacology of human itch GPCRs Open
The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-coupled receptors that have evolved relatively recently1. Of these, MRGPRX2 and MRGPRX4 are key physiological and pathological mediators of itch and related ma…
View article: Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator
Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator Open
The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS modulates dopamine neuronal activity, ind…
View article: Molecular basis for selective activation of DREADD-based chemogenetics
Molecular basis for selective activation of DREADD-based chemogenetics Open
Designer receptors exclusively activated by designer drugs (DREADDs) represent a powerful chemogenetic technology for the remote control of neuronal activity and cellular signalling1–4. The muscarinic receptor-based DREADDs are the most wi…
View article: Ligand recognition and allosteric modulation of the human MRGPRX1 receptor
Ligand recognition and allosteric modulation of the human MRGPRX1 receptor Open
The human MAS-related G protein–coupled receptor X1 (MRGPRX1) is preferentially expressed in the small-diameter primary sensory neurons and involved in the mediation of nociception and pruritus. Central activation of MRGPRX1 by the endogen…
View article: Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors Open
Using the HIV-1 protease binding mode of MK-8718 and PL-100 as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this c…
View article: The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design
The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design Open
View article: Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group Open
A novel HIV protease inhibitor was designed using a morpholine core as the aspartate binding group. Analysis of the crystal structure of the initial lead bound to HIV protease enabled optimization of enzyme potency and antiviral activity. …