ArticleACS chemical neuroscience2015
Water-Soluble MMP-9 Inhibitor Reduces Lesion Volume after Severe Traumatic Brain Injury.
Article in ACS chemical neuroscience, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 25 citations in OpenAlex.
- Predicting glioma survival and extracellular matrix remodeling through MRI radiogenomics.Cell reports. Medicine · 2026Article
- The evolving pathophysiology of TBI and the advantages of temporally-guided combination therapies.Neurochemistry international · 2024Review
- NF-κB/RelA signaling in secretoglobin progenitors mediates plasticity and MMP-induced barrier disruption in house dust mite-induced allergic asthma.American journal of physiology. Lung cellular and molecular physiology · 2024Article
- The Role of MMP-9 and MMP-9 Inhibition in Different Types of Thyroid Carcinoma.Molecules (Basel, Switzerland) · 2023Review
- Design, Synthesis and Biological Evaluation of Prodrugs of 666-15 as Inhibitors of CREB-Mediated Gene Transcription.ACS medicinal chemistry letters · 2022Article
- Blood-Brain Barrier Mechanisms in Stroke and Trauma.Handbook of experimental pharmacology · 2022Review
- Mechanisms of Action of Novel Drugs Targeting Angiogenesis-Promoting Matrix Metalloproteinases.Frontiers in immunology · 2019Review
- Extracellular matrix and traumatic brain injury.Journal of neuroscience research · 2018Review
- Early to Long-Term Alterations of CNS Barriers After Traumatic Brain Injury: Considerations for Drug Development.The AAPS journal · 2017Review
- Exploitation of Conformational Dynamics in Imparting Selective Inhibition for Related Matrix Metalloproteinases.ACS medicinal chemistry letters · 2017Article
- Neurovascular dysfunction and neurodegeneration in dementia and Alzheimer's disease.Biochimica et biophysica acta · 2016Review
- Inhibition of Matrix Metalloproteinase 9 Enhances Rod Survival in the S334ter-line3 Retinitis Pigmentosa Model.PloS one · 2016Article
- The Prodrug Approach: A Successful Tool for Improving Drug Solubility.Molecules (Basel, Switzerland) · 2015Review
Corrections and comments
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Authors and funding
16 authors at 2 institutions in 1 country.
Funding
Abstract
SB-3CT is a potent and selective inhibitor of matrix metalloproteinase (MMP)-2 and -9, which has shown efficacy in an animal model of severe traumatic brain injury (TBI). However, SB-3CT is poorly water-soluble and is metabolized primarily to p-hydroxy SB-3CT (2), a more potent inhibitor than SB-3CT. We synthesized the O-phosphate prodrug (3) of compound 2 to enhance its water solubility by more than 2000-fold. The prodrug 3 was a poor MMP inhibitor, but readily hydrolyzed to the active 2 in human blood. Pharmacokinetics and brain distribution studies in mice showed that 2 crossed the blood-brain barrier (BBB) and achieved therapeutic concentrations in the brain. The prodrug 3/compound 2 was evaluated in a mouse model of severe TBI and found to significantly decrease the brain lesion volume and improve neurological outcomes. MMP-9 inhibition by a water-soluble thiirane inhibitor is a promising therapy for treatment of TBI.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.