Leon Jacobs

Corrigendum to “A subunit-selective negative allosteric modulator of GluN1/GluN3A glycine-activated receptor” [Molecular Pharmacology 108 (2026) 100104]

Leon Jacobs, TrangKimberly Thu Nguyen, Adam McCallum, Matt P. Epplin et autres

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A subunit-selective negative allosteric modulator of GluN1/GluN3A glycine-activated receptor

Leon Jacobs, TrangKimberly Thu Nguyen, Adam McCallum, Matt P. Epplin et autres

The ionotropic glutamate NMDA receptor gene family includes 7 homologous subunits (GluN1, GluN2A-D, and GluN3A-B). The co-assembly of GluN1 and GluN2 form the well-studied NMDA receptor, which requires binding of both glutamate and glycine to be activated. However, glycine alone can activate …

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EMU-116: An oral CXCR4 antagonist as mobilizer of stem and immune cells in normal, neutropenic and sickle cell mice.

Lawrence J. Wilson, Priscilla Davidson, Hayden Kissick, John A. Petros et autres

Abstract The use of CXCR4 antagonists as cell mobilization agents has resulted in 3 FDA approved drugs for use in hematopoietic stem cell transplantation (Plerixafor, Motixafortide) and for treating neutropenia (Mavorixafor). Given these developments, the need for agents which can be delivered …

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Mild and Chemoselective Triethylsilane-Mediated Debenzylation for Phosphate Synthesis

Luke Hodson, Paul Joseph Tholath, Leon Jacobs, Nicole Pribut et autres

The synthetic utility of tetrabenzyl pyrophosphate for achieving chemoselective phosphorylation of phenols, as well as primary, secondary, and tertiary alcohols, is reported here. Additionally, we introduce a rapid, mild, and chemoselective debenzylation procedure, enabling access to phosphates in the presence of redox …

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Mechanisms of Action Underlying Conductance-Modifying Positive Allosteric Modulators of the NMDA Receptor

Elijah Z. Ullman, Riley E. Perszyk, Srinu Paladugu, Russell G. Fritzemeier et autres

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Scale-Up Preparation of Best-In-Class Orally Bioavailable CXCR4 Antagonist EMU-116 in an Academic Setting

Leon Jacobs, Eric J Miller, Robert J. Wilson, Edgars Jēčs et autres

High Resolution Image Download MS PowerPoint Slide CXCR4 is a seven-transmembrane chemokine receptor that is intimately involved in stem cell niche maintenance and immune cell trafficking. Among several other pathophysiological states for which CXCR4 mis regulation is implicated, various hematological malignancies and …

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Accelerating Oral Wound Healing Using Bilayer Biomaterial Delivery of FTY720 Immunotherapy

Afra I. Toma, Daniel Shah, Daniela M. Roth, Jeremie D. Oliver et autres

Orofacial clefts are the most common congenital craniofacial anomaly. Adverse healing following cleft palate repair can lead to oronasal fistula (ONF), a persistent connection between the oral and nasal cavities. Although human allograft tissues are currently the gold standard for ONF repair, …

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Tetrahydroisoquinoline-Based Small Molecule Inhibitors of the Chemokine Receptor CXCR4

Eric J Miller, Petra Gregorova, Carrie Sun, Leon Jacobs et autres

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Harnessing Bilayer Biomaterial Delivery of FTY720 as an Immunotherapy to Accelerate Oral Wound Healing

Afra I. Toma, Daniela M. Roth, Jeremie D. Oliver, Lauren A. Hymel et autres

Orofacial clefts are the most common craniofacial congenital anomaly. Following cleft palate repair, up to 60% of surgeries have wound healing complications leading to oronasal fistula (ONF), a persistent connection between the roof of the mouth and the nasal cavity. The current …

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Design and Optimization of Novel Competitive, Non-peptidic, SARS-CoV‑2 Mpro Inhibitors

Leon Jacobs, Aletta van der Westhuyzen, Nicole Pribut, Zackery W. Dentmon et autres

Abstract The SARS-CoV-2 main protease (Mpro) has been proven to be a highly effective target for therapeutic intervention, yet only one drug currently holds FDA approval status for this target. We were inspired by a series of publications emanating from the Jorgensen …

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Synthesis of fused heterocyclic aromatic compounds as potential antiplasmodial agents

Leon Jacobs

ENGLISH ABSTRACT: 3-Methyl benzofuran antiplasmodial compounds have been described in literature and and synthesis of heterocyclic derivatives forms the basis of this project. These benzofuran compounds were synthesized with the primary role as effective inhibitors of the enzyme Plasmodium falciparum N-Myristoyl transferase …

Design, Synthesis, and Evaluation of Novel Ferroquine and Phenylequine Analogues as Potential Antiplasmodial Agents

Leon Jacobs, Carmen De Kock, Katherine A. de Villiers, Peter J. Smith et autres

7-Chloroquinoline-based antimalarial drugs are effective in the inhibition of hemozoin formation in the food vacuole of the Plasmodium parasite, the causative agent of malaria. We synthesized five series of ferroquine (FQ) and phenylequine (PQ) derivatives, which display good in vitro efficacy toward …

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