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Selective phosphoinositide 3-kinase inhibitors and implication in diabetic retinopathy as pharmacological tools

Carmela Bonaccorso1, Francesca Lazzara2,3,4, Isabel La Rosa2

  • 1Department of Chemical Sciences, University of Catania, Catania, Italy.

Frontiers in Pharmacology
|March 30, 2026
PubMed

Insights

Phosphoinositide 3-kinases (PI3K) signaling plays a role in diabetic retinopathy. Inhibiting PI3Kδ may offer a new therapeutic strategy for this eye condition.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Ophthalmology

Background:

  • Phosphoinositide 3-kinases (PI3Ks) are crucial enzymes regulating cellular functions and are implicated in cancer pathogenesis.
  • PI3K inhibitors are approved for certain blood cancers, and leniolisib targets PI3Kδ for Activated Phosphoinositide 3-kinase Delta Syndrome (APDS).
  • PI3K/AKT signaling is downstream of VEGF-A, contributing to diabetic retinopathy, a microvascular complication of diabetes.

Purpose of the Study:

  • To investigate the role of PI3K signaling in diabetic retinopathy.
  • To review molecular features of selective class I PI3K inhibitors.
  • To guide the development of novel PI3Kδ-targeting drugs for retinal diseases.

Main Methods:

  • Exploration of PI3K signaling in diabetic retinopathy.
  • Literature review of class I PI3K selective inhibitors.
  • Analysis of molecular features for drug design.

Main Results:

  • Recent studies show PI3Kδ inhibition benefits in an in-vivo diabetic retinopathy model.
  • PI3Kδ is a potential therapeutic target for diabetic retinopathy.

Conclusions:

  • PI3K signaling is implicated in diabetic retinopathy progression.
  • Selective PI3Kδ inhibitors represent a promising therapeutic avenue for diabetic retinopathy and other proliferative retinal diseases.
Keywords:
PI3K inhibitordiabetic retinopathyquantitative structure activity relationship (QSAR)repurposingretina

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