ROCK inhibitor [Neurosurgery Wiki]

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====== ROCK inhibitor ======

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### **ROCK Inhibitors: Overview and Applications**

#### **1. What are ROCK Inhibitors?**
ROCK inhibitors are pharmacological agents that block the activity of **Rho-associated protein kinase (ROCK)**, a key enzyme in the **RhoA/ROCK signaling pathway**. These inhibitors reduce actin-myosin contractility, influencing various cellular processes like migration, proliferation, and adhesion.

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#### **2. Mechanism of Action**
ROCK inhibitors prevent the phosphorylation of:
- **Myosin Light Chain (MLC):** Reduces actin-myosin contraction.
- **LIM Kinase (LIMK):** Affects actin stability.
- **Adhesion Proteins:** Modulate cellular stiffness and motility.

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#### **3. Common ROCK Inhibitors**
| **Inhibitor** | **Clinical Use**                   | **Key Features**                          |
|---------------|------------------------------------|--------------------------------------------|
| **Fasudil**   | Cerebral vasospasm, hypertension    | Approved in Japan; improves vasodilation. |
| **Ripasudil** | Glaucoma                            | Lowers intraocular pressure.              |
| **Y-27632**   | Research (fibrosis, neuroprotection)| Widely used in preclinical studies.       |
| **AT13148**   | Cancer (experimental)               | Targets multiple kinases, including ROCK. |

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#### **4. Clinical Applications**
- **Cardiovascular Diseases:**
  - **Hypertension:** ROCK inhibitors reduce vascular resistance and blood pressure.
  - **Pulmonary Hypertension:** Improve arterial function by relaxing smooth muscle.

- **Neurological Disorders:**
  - **Stroke:** Enhance neuroprotection and axonal regeneration.
  - **Spinal Cord Injury:** Promote axon growth and functional recovery.see [[ROCK inhibitor for spinal cord injury]] 

  - **Neurodegenerative Diseases:** Potential benefits in Parkinson’s and Alzheimer’s.

- **Ophthalmology:**
  - **Glaucoma:** Ripasudil improves aqueous humor outflow, reducing intraocular pressure.

- **Oncology:**
  - **Cancer Metastasis:** Reduce tumor cell migration and invasion.

- **Fibrosis:**
  - **Lung, Liver, and Kidney Fibrosis:** Decrease fibroblast activation and extracellular matrix deposition.

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#### **5. Emerging Research**
- Development of **selective ROCK2 inhibitors** to minimize side effects.
- Combination therapies with ROCK inhibitors for enhanced efficacy in **oncology** and **neurological diseases**.