Explanipedia

Safety, tolerability and potential biomarkers of vodobatinib in patients with dementia with Lewy bodies Open

Fernando Pagán, Yasar Torres‐Yaghi, Michaeline Hebron, Barbara Wilmarth, Xiaoguang Liu , et al. · 2025

Vodobatinib appears to be safe and tolerated, but larger trials and longer treatment periods are needed to determine its effects on biomarkers and clinical outcomes.

Safety, Cognitive, and Behavioral Outcomes in Patients with Dementia with Lewy Bodies Treated with Nilotinib Open

Fernando Pagán, Yasar Torres‐Yaghi, Michaeline Hebron, Barbara Wilmarth, Raymond Scott Turner , et al. · 2025

Background/Objectives: We previously demonstrated that nilotinib can sufficiently enter the brain to pharmacologically inhibit discoidin domain receptors (DDR)-1 in patients with Parkinson’s and Alzheimer’s disease. We primarily hypothesiz…

Resveratrol Attenuates CSF Markers of Neurodegeneration and Neuroinflammation in Individuals with Alzheimer’s Disease Open

Xiaoguang Liu, Sean Baxley, Michaeline Hebron, Raymond Scott Turner, Charbel Moussa · 2025

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder that is characterized by amyloid-beta (Aβ) accumulation and neuroinflammation. A previous multicenter, phase 2, double-blind, placebo-controlled trial randomized 179 part…

A Novel Small Molecule Enhances Stable Dopamine Delivery to the Brain in Models of Parkinson’s Disease Open

Margaret Liu, Michaeline Hebron, Max Stevenson, Charbel Moussa · 2025

Levodopa is the gold standard symptomatic treatment for Parkinson’s disease. Disease progression due to alpha-synuclein accumulation, brain inflammation, and the loss of dopamine neurons, as well as motor fluctuations, due to variations in…

Modulation of Peripheral Mast Cell and Brain Microglia Axis via Kinase Inhibition Open

Xiaoguang Liu, Michaeline Hebron, Kaluvu Balaraman, L L Ballard, Kui Liu , et al. · 2025

Background/Objectives: Kinase inhibition is a hot therapeutic strategy for several human diseases, including neurodegeneration. Tyrosine kinase c-KIT activates peripheral mast cells, while other kinases including Abelson (c-Abl) promotes a…

c-KIT inhibitors reduce pathology and improve behavior in the Tg(SwDI) model of Alzheimer’s disease Open

Max Stevenson, Michaeline Hebron, Xiaoguang Liu, Kaluvu Balaraman, Christian Wolf , et al. · 2024

Treatments for Alzheimer’s disease have primarily focused on removing brain amyloid plaques to improve cognitive outcomes in patients. We developed small compounds, known as BK40143 and BK40197, and we hypothesize that these drugs alleviat…

325 Tyrosine kinase inhibition reduces pathological markers of Alzheimer’s Disease Open

Max Stevenson, Xiaoguang Liu, Michaeline Hebron, Charbel Moussa · 2024

OBJECTIVES/GOALS: Alzheimer’s Disease (AD) displays numerous pathological features, including amyloid-beta deposition, extensive neuroinflammation, and vascular fibrosis. However, putative therapeutic options for alleviating these features…

DDR1 regulates CNS collagen IV expression and vascular fibrosis in AD to improve CNS vascular integrity Open

Max E Stevenson, Rency S. Varghese, Michaeline Hebron, Xiaoguang Liu, Raymond Scott Turner , et al. · 2023

Background Blood‐brain barrier breakdown, a feature associated with AD pathology and treatments, was examined as a potential therapeutic target in both genetic mouse models of AD and clinical trial data from human patients with AD treated …

Inhibition of discoidin domain receptor (DDR)-1 with nilotinib alters CSF miRNAs and is associated with reduced inflammation and vascular fibrosis in Alzheimer’s disease Open

Max Stevenson, Rency S. Varghese, Michaeline Hebron, Xiaoguang Liu, Nick Ratliff , et al. · 2023

Discoidin Domain Receptor (DDR)-1 is activated by collagen. Nilotinib is a tyrosine kinase inhibitor that is FDA-approved for leukemia and potently inhibits DDR-1. Individuals diagnosed with mild–moderate Alzheimer’s disease (AD) treated w…

Inhibition of discoidin domain receptor (DDR)-1 with nilotinib induces autophagy and reduces inflammation and vascular fibrosis in Alzheimer’s disease Open

Max Stevenson, Rency S. Varghese, Michaeline Hebron, Xiaoguang Liu, Nick Ratliff , et al. · 2023

Discoidin Domain Receptor (DDR)-1 is activated by collagen. Nilotinib is a tyrosine kinase inhibitor that is FDA-approved for leukemia and potently inhibits DDR-1. Individuals diagnosed with mild-moderate Alzheimer’s disease (AD) treated w…

Correction: Parkin ubiquitinates TAR-DNA binding protein-43 (TDP-43) and promotes its cytosolic accumulation via interaction with histone deacetylase 6 (HDAC6) Open

Michaeline Hebron, Irina Lonskaya, Kaydee Sharpe, Puwakdandawe P.K. Weerasinghe, Norah K. Algarzae , et al. · 2022

In the published article western blot image for Figure 4G HDAC6 panel was inserted by a mistake. The amended Figure 4G below shows the correct HDAC6 blot. The authors state that the scientific conclusions of the article are not affected by…

Alteration of Autophagy and Glial Activity in Nilotinib-Treated Huntington’s Disease Patients Open

Karen E. Anderson, Max Stevenson, Rency S. Varghese, Michaeline Hebron, Erin Koppel , et al. · 2022

Nilotinib is a tyrosine kinase inhibitor that is safe and tolerated in neurodegeneration, it achieves CSF concentration that is adequate to inhibit discoidin domain receptor (DDR)-1. Nilotinib significantly affects dopamine metabolites, in…

Label-free affinity screening, design and synthesis of inhibitors targeting the Mycobacterium tuberculosis L-alanine dehydrogenase Open

Heung-Bok Kim, J.P. Bacik, Ruilian Wu, Ramesh K. Jha, Michaeline Hebron , et al. · 2022

The ability of Mycobacterium tuberculosis ( Mtb ) to persist in its host may enable an evolutionary advantage for drug resistant variants to emerge. A potential strategy to prevent persistence and gain drug efficacy is to directly target t…

Inhibition of Ubiquitin-Specific Protease-13 Improves Behavioral Performance in Alpha-Synuclein Expressing Mice Open

Xiaoguang Liu, Kaluvu Balaraman, Ciarán C. Lynch, Michaeline Hebron, Priya Ketankumar Shah , et al. · 2022

Ubiquitin-Specific Protease-13 (USP13) promotes protein de-ubiquitination. USP13 levels are upregulated in post-mortem Parkinson’s disease, whereas USP13 knockdown via shRNA reduces alpha-synuclein levels in animal models. We studied the r…

Safety, target engagement, and biomarker effects of bosutinib in dementia with Lewy bodies Open

Fernando Pagán, Yasar Torres‐Yaghi, Michaeline Hebron, Barbara Wilmarth, Raymond Scott Turner , et al. · 2022

Introduction Bosutinib, a dual Abelson/Src inhibitor, was investigated in individuals with dementia with Lewy bodies (DLB). Methods A single site, randomized, double‐blind, placebo‐controlled study of the effects of oral bosutinib, 100 mg …

Novel Ubiquitin Specific Protease-13 Inhibitors Alleviate Neurodegenerative Pathology Open

Xiaoguang Liu, Kaluvu Balaraman, Ciarán C. Lynch, Michaeline Hebron, Christian Wolf , et al. · 2021

Ubiquitin Specific Protease-13 (USP13) promotes protein de-ubiquitination and is poorly understood in neurodegeneration. USP13 is upregulated in Alzheimer’s disease (AD) and Parkinson’s disease (PD), and USP13 knockdown via shRNA reduces n…

Erratum to: Discoidin Domain Receptor 1 is a therapeutic target for neurodegenerative diseases Open

Alan J. Fowler, Michaeline Hebron, Kaluvu Balaraman, Wangke Shi, Alexander A. Missner , et al. · 2021

60941 Vaginal pH predicts cervical intraepithelial neoplasia-2 regression in women living with human immunodeficiency virus Open

Katherine G. Michel, Christine Colie, Robert D. Burk, L. Stewart Massad, Cuiwei Wang , et al. · 2021

IMPACT: The potential to use vaginal pH as a low cost, non-invasive diagnostic test at the point of CIN2 diagnosis to predict worsening of cervical disease. OBJECTIVES/GOALS: We previously reported that persistence/progression of cervical …

Long‐Term Safety and Clinical Effects of Nilotinib in Parkinson's Disease Open

Fernando Pagán, Barbara Wilmarth, Yasar Torres‐Yaghi, Michaeline Hebron, Sanjana Mulki , et al. · 2020

Background Nilotinib is US Food and Drug Administration–approved for leukemia, and this open‐label study investigated the safety, tolerability, and potential clinical effects of nilotinib in medically optimized patients with Parkinson's di…

Discoidin Domain Receptor 1 is a therapeutic target for neurodegenerative diseases Open

Alan J. Fowler, Michaeline Hebron, Kaluvu Balaraman, Wangke Shi, Alexander A. Missner , et al. · 2020

The role of Discoidin Domain Receptors (DDRs) is poorly understood in neurodegeneration. DDRs are upregulated in Alzheimer’s and Parkinson’s disease (PD), and DDRs knockdown reduces neurotoxic protein levels. Here we show that potent and p…

4564 Nilotinib alters microRNAs that regulate specific autophagy and ubiquitination genes in the cerebrospinal fluid of Parkinson’s patients Open

Alan J. Fowler, Yasar Torres-Yhagi, Fernando Pagán, Michaeline Hebron, Barbara Willmarth , et al. · 2020

OBJECTIVES/GOALS: Our preclinical data demonstrate that the principal effects of nilotinib, a multi-tyrosine kinase inhibitor, in models of neurodegeneration is clearance of misfolded proteins via autophagy. Here we aimed to evaluate the e…

Nilotinib Effects on Safety, Tolerability, and Biomarkers in Alzheimer's Disease Open

Raymond Scott Turner, Michaeline Hebron, Abigail Lawler, Elizabeth Mundel, Nadia Yusuf , et al. · 2020

Objective Preclinical evidence with nilotinib, a US Food and Drug Administration (FDA)‐approved drug for leukemia, indicates improvement in Alzheimer's disease phenotypes. We investigated whether nilotinib is safe, and detectable in cerebr…

Nilotinib Effects on Safety, Tolerability, and Potential Biomarkers in Parkinson Disease Open

Fernando Pagán, Michaeline Hebron, Barbara Wilmarth, Yasar Torres‐Yaghi, Abigail Lawler , et al. · 2019

ClinicalTrials.gov identifier: NCT02954978.

DT‐02‐06: A NOVEL SMALL MOLECULE INHIBITOR OF THE DISCOIDIN DOMAIN RECEPTORS (DDR) REDUCES TAU AND AMYLOID‐β AND IMPROVES COGNITION IN MODELS OF ALZHEIMER'S DISEASE Open

Alan J. Fowler, Michaeline Hebron, Wangke Shi, Alexander A. Missner, Diandra S. Hassan , et al. · 2019

Many neurodegenerative diseases share the feature that there is an accumulation of proteins which become neurotoxic. For example, amyloid-beta or tau in Alzheimer's Disease (AD), α-synuclein in Parkinson's disease (PD), or an overlapping o…

Multikinase Abl/DDR/Src Inhibition Produces Optimal Effects for Tyrosine Kinase Inhibition in Neurodegeneration Open

Alan J. Fowler, Michaeline Hebron, Alexander A. Missner, Ruochong Wang, Xiaokong Gao , et al. · 2019

Pharmacokinetics and pharmacodynamics of a single dose Nilotinib in individuals with Parkinson's disease Open

Fernando Pagán, Michaeline Hebron, Barbara Wilmarth, Yasar Torres‐Yaghi, Abigail Lawler , et al. · 2019

Nilotinib is a broad‐based tyrosine kinase inhibitor with the highest affinity to inhibit Abelson (c‐Abl) and discoidin domain receptors ( DDR 1/2). Preclinical evidence indicates that Nilotinib reduces the level of brain alpha‐synuclein a…

Nilotinib Safety and Clinical Effects on 'ON' Disability in Parkinson's Disease Patients Open

Charbel Moussa, Fernando Pagán, Yasar Torres‐Yaghi, Ellen Valladez, Abigail Lawler , et al. · 2019

Ubiquitin specific protease-13 independently regulates parkin ubiquitination and alpha-synuclein clearance in alpha-synucleinopathies Open

Xiaoguang Liu, Michaeline Hebron, Wangke Shi, Irina Lonskaya, Charbel Moussa · 2018

Ubiquitin specific proteases (USPs) are de-ubiquitinases (DUBs) that control protein ubiquitination cycle. The role of DUBs is poorly understood in neurodegenerative diseases. We found that USP13 is overexpressed in post-mortem Parkinson's…

Pazopanib Reduces Phosphorylated Tau Levels and Alters Astrocytes in a Mouse Model of Tauopathy Open

Monica Javidnia, Michaeline Hebron, Yue Xin, Nikolas G. Kinney, Charbel Moussa · 2017

Hyperphosphorylation and aggregation of tau protein is a critical factor in many neurodegenerative diseases. These diseases are increasing in prevalence, and there are currently no cures. Previous work from our group and others has shown t…

[P4–095]: NILOTINIB REDUCES PHOSPHORYLATED NEUROFILAMENTS AND CORRELATES WITH COGNITIVE IMPROVEMENT IN PARKINSON's DISEASE WITH DEMENTIA AND LEWY BODY DEMENTIA Open

Charbel Moussa, Fernando Pagán, Michaeline Hebron · 2017

Parkinson's disease (PD) is a neurodegenerative disorder that affects motor and non-motor functions. Our pre-clinical data indicate that the tyrosine kinase inhibitor (TKI) Nilotinib improves motor behavior and cognition in several models …

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