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Enhancing the Engraftment of Human Induced Pluripotent Stem Cell-derived Cardiomyocytes via a Transient Inhibition of Rho Kinase Activity
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Light-controlled inhibition of BRAFV600E kinase

Mark W H Hoorens1, Maria E Ourailidou2, Theo Rodat3

  • 1University Medical Center Groningen, Department of Radiology, Medical Imaging Center, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, Netherlands; Stratingh Institute for Chemistry, Faculty of Science and Engineering, University of Groningen, Nijenborgh 7, 9747 AG Groningen, Netherlands.

European Journal of Medicinal Chemistry
|June 29, 2019
PubMed

Insights

Researchers developed light-activated BRAF inhibitors for metastatic melanoma. This targeted therapy allows drug activation only at the tumor site, reducing side effects and improving treatment efficacy.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Metastatic melanoma is a challenging cancer with treatments often targeting BRAF V600E kinase.
  • Current BRAF inhibitors can paradoxically increase wild-type BRAF activity in healthy tissues, leading to side effects and secondary tumors.

Purpose of the Study:

  • To develop novel BRAF V600E kinase inhibitors with light-switchable activity.
  • To enable targeted drug activation at the tumor site, minimizing systemic toxicity.

Main Methods:

  • Design and synthesis of eight photoswitchable BRAF V600E inhibitors incorporating an azobenzene photoswitch.
  • Evaluation of inhibitor efficacy and light-responsiveness.

Main Results:

  • Development of a promising BRAF V600E inhibitor with reversible light-controlled activity.
  • Demonstrated approximately 10-fold increase in inhibitor activity upon light activation.

Conclusions:

  • Light-activatable BRAF V600E inhibitors offer a potential strategy for targeted metastatic melanoma therapy.
  • This approach allows for high spatial and temporal control of drug activity, potentially reducing damage to healthy tissues.
Keywords:
AzobenzeneBRAF(V600E)Metastatic melanomaPhotocontrolled inhibitorPhotopharmacology

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