ROCK inhibitors such as fasudil protected against dopaminergic degeneration and other neurodegenerative processes in several experimental models throu…

Read the full paper: Anti-inflammatory and pro-proliferative effects of fasudil in human trisomy 21 neural progenitor cells

ROCK inhibitors such as fasudil protected against dopaminergic degeneration and other neurodegenerative processes in several experimental models through inhibition of neuroinflammation and activation ...

Human α-synuclein is an intrinsically disordered protein concentrated at presynaptic terminals and strongly linked to Parkinson’s disease and other synucleinopathies. Its dynamic C-terminal region mediates interactions with small molecules and metal ions. Here, we used high-resolution nuclear magnetic resonance spectroscopy (NMR) and molecular dynamics (MD) simulations to characterize interactions between the C-terminal α-synuclein construct, the small molecule fasudil, and calcium ions. NMR data show that fasudil and Ca2+ bind preferentially to overlapping regions enriched in alternating tyrosine and acidic residues while preserving the protein’s disordered nature. Side-chain-resolved spectra indicate distinct driving forces for fasudil and calcium binding. MD simulations reveal that Ca2+ modifies the local electrostatic environment, decreasing fasudil interaction frequency through electrostatic screening and steric effects. Despite this, fasudil retains dynamic, reversible contacts with key tyrosine residues. Overall, exposed α-synuclein conformations allow simultaneous, ligand-specific interactions, highlighting side-chain hotspots governing binding in Ca2+-rich conditions.

Hemorrhagic transformation (HT) is a common complication of ischemic stroke that significantly increases the rates of disability and mortality, which could be promoted by hyperglycemia as a risk factor for HT after stroke. Neuronal ferroptosis was implicated as a key contributor to neuronal death during the development of HT which currently has few effective therapies in clinic. The compound fasudil dichloroacetate (FDCA), synthesized with ROCK inhibitor fasudil (F) and PDK inhibitor dichloroacetate (DCA) was previously reported to exhibit neuroprotective effects in ischemic stroke, but whether FDCA could ameliorate HT post-stroke remains unknown. In this study, FDCA was synthesized by combining the Rho kinase inhibitor F with the PDK inhibitor DCA. Rats with acute hyperglycemia and ischemic stroke were divided into the control group, 10 mg/kg FDCA treatment group, 7.875 mg/kg F + 3.6 mg/kg DCA combination treatment group, and other relevant control groups. Our findings dem

NEW YORK, Dec. 9, 2024 /PRNewswire/ -- Woolsey Pharmaceuticals, a clinical-stage pharmaceutical company developing BRAVYL (oral fasudil) for the treatment of Amyotrophic Lateral Sclerosis (ALS), annou...

📅 Publication Date: April 2026 | ⏳ Forecast Period: 2026-2033 📊 Market Intelligence Overview | Access Research Sample | Explore Full Market Study United States Fasudil Market Snapshot The United State...

📅 Publication Date: April 2026 | ⏳ Forecast Period: 2026-2033 📊 Market Intelligence Overview | Access Research Sample | Explore Full Market Study United States Fasudil Market Snapshot The United State...

📅 Publication Date: April 2026 | ⏳ Forecast Period: 2026-2033 📊 Market Intelligence Overview | Access Research Sample | Explore Full Market Study United States Fasudil Market Snapshot The United State...

📅 Publication Date: April 2026 | ⏳ Forecast Period: 2026-2033 📊 Market Intelligence Overview | Access Research Sample | Explore Full Market Study United States Fasudil Market Snapshot The United State...

📅 Publication Date: April 2026 | ⏳ Forecast Period: 2026-2033 📊 Market Intelligence Overview | Access Research Sample | Explore Full Market Study United States Fasudil Market Snapshot The United State...

📅 Publication Date: April 2026 | ⏳ Forecast Period: 2026-2033 📊 Market Intelligence Overview | Access Research Sample | Explore Full Market Study United States Fasudil Market Snapshot The United State...

📥 Download Sample 💰 Get Special Discount Malaysia Fasudil Hydrochloride Injection Market Size, Strategic Outlook & Forecast 2026-2033Market size (2024): USD 150 millionForecast (2033): USD 300 million...

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Ischemic stroke is a leading cause of disability worldwide and poses a serious threat to public health, affecting tens of millions of people all over the world per year. The lack of a humanized organ model reflecting the real situation of patients has quite limited the pathogenesis research and therapeutic drug development of ischemic stroke. In this study, we developed an ischemic stroke model based on a high-throughput microfluidic chip device, simulating ischemia-reperfusion injury in an ischemic stroke. In this ischemic stroke model, we observed a series of injury characteristics, including significant blood–brain barrier (BBB) destruction, cell apoptosis, and mitochondrial dysfunction. Transcriptome sequencing analysis showed that the expression of genes involved in autophagy, oxidative stress, angiogenesis, and other related pathways was significantly dysregulated in the ischemic stroke model. Drug screening experiments revealed that acetazolamide (AZA), edaravone (EDA), and fasudil (FAS) could significantly reduce the damage in an ischemic stroke model. Overall, the ischemic stroke model recapitulated the physiological and pathological responses of ischemic stroke, and it was innovative that our model focused on reperfusion injury using microfluidic organ-on-a-chip technology. This ischemic stroke brain model holds promise for advancing the development and testing of therapeutic drugs for ischemic stroke, thus contributing to the evolution of treatment strategies.