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Novel GPER/GPR30 receptor ligands

GPER/GPR30 receptorneurodegenerative diseasesNicotinamideNicotinic acidTumors


The invention relates to the use of nicotinic acid or nicotinamide and to compositions thereof for use in the treatment of pathological conditions that can benefit from the biological activity induced by the activation of GPER/GPR30. The biological activity exerted by nicotinic acid and nicotinamide as ligands of this receptor will determine the development of innovative diagnostic and therapeutic approaches.

Technical features

The GPER/GPR30 receptor is widely distributed in different tissues, such as heart and vessels, ovary, placenta, prostate, liver, pancreas, kidney, surrenal, epithelial and bone tissue, nervous and lymphatic systems. The present invention is based on the finding of two new GPR30 receptor ligands which selectively activate the transduction pathway mediated by this receptor. The new ligands are nicotinic acid, also known as vitamin B3, and the amidic derivative of nicotinic acid, known as nicotinamide. Our findings demonstrated that nicotinic acid and nicotinamide acting as agonists for GPER induce stimulatory effects in breast cancer cells and cancer–associated fibroblasts (CAFs) and other relevant biological responses.The invention has been validated by experimental data obtained through real-time PCR methods, western blots, transients transients for gene silencing and various biological assays.

Possible Applications

  • Research, development and implementation of new diagnostic-therapeutic applications related to the use of nicotinic acid and nicotinamide as GPER ligands for a wide range of pathophysiological conditions (cardiovascular, neurodegenerative, metabolic, etc.);
  • Development of new anticancer drugs.


  • Improvement of current diagnostic, prognostic and therapeutic tools in a wide range of pathophysiological conditions: Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, peripheral diabetic neuropathy, multiple sclerosis, amyotrophic lateral sclerosis, stroke, head injury, peripheral nerve damage, hypoglycemia, spinal cord injury, epilepsy, anoxia and hypoxia, tumors, etc.