Kinases in cerebral cavernous malformations: Pathogenesis and therapeutic targets

Chunxiao Qi1, Richard Sean Bujaroski2, Jonathan Baell3

  • 1Department of Pharmacology and Tianjin Key Laboratory of Inflammation Biology, School of Basic Medical Sciences, Tianjin Medical University, 300070, China.

Insights

Cerebral cavernous malformations (CCMs) involve genetic pathways and kinase signaling. Targeting these pathways offers a promising non-surgical treatment option for CCM disease.

Area of Science:

  • Neuroscience
  • Genetics
  • Pharmacology

Background:

  • Cerebral cavernous malformations (CCMs) are genetic vascular lesions in the central nervous system causing stroke-like symptoms and seizures.
  • Identification of CCM1, CCM2, and CCM3 genes has elucidated molecular mechanisms underlying CCM pathogenesis.

Purpose of the Study:

  • To review the general aspects of CCM disease.
  • To discuss kinase-mediated signaling pathways involved in CCM pathogenesis.
  • To explore current potential therapeutic strategies for CCM.

Main Methods:

  • Literature review of CCM disease mechanisms and signaling pathways.
  • Analysis of kinase signaling cascades (e.g., MEKK3/MEK5/ERK5, Rho/Rock, CCM3/GCKIII, PI3K/mTOR).
  • Examination of preclinical and clinical trial data for CCM therapeutics.

Main Results:

  • Kinases play a central role in CCM pathogenesis, with several key signaling cascades identified.
  • Inhibitors targeting Rho/Rock signaling and other kinase components have shown potential in preclinical and clinical studies.
  • Drug development targeting kinase signaling pathways is advancing.

Conclusions:

  • Kinase-targeted drug development presents a viable non-surgical treatment option for CCM disease.
  • Further research into kinase inhibitors may address the unmet need for effective CCM therapies.
  • Understanding kinase signaling is crucial for developing novel therapeutic interventions for CCM.

Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
215
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
7.7K
Regulation of Angiogenesis and Blood Supply01:24

Regulation of Angiogenesis and Blood Supply

Rapidly dividing tumors, embryos, and wounded tissues require more oxygen than usual, lowering the oxygen concentration in the blood. At low oxygen or hypoxic conditions, an oxygen-sensitive transcription factor called the hypoxia-inducible factor 1 or HIF1 is activated. HIF1 is a dimeric protein of alpha (ɑ) and beta (β) subunits.  Under optimal oxygen conditions, HIF1β is present in the nucleus while HIF1ɑ remains in the cytosol. HIF1ɑ is hydroxylated by prolyl...
2.6K