PHOTOCHROMIC MOLECULES FOR THE CARE OF DYSTROPHIES

Data di pubblicazione

02-01-2019

Codice

CH.18.020.A

Data di priorità

06-04-2018

Fase

Italian

Titolare

Istituto Italiano di Tecnologia (IIT) e Politecnico di Milano

Dipartimento

Department of Chemistry Materials and Chemical Engineering

Autori

Lanzani Guglielmo, Bertarelli Chiara, Colella Letizia, Benfenati Fabio, Di Francesco Mattia, Colombo Elisabetta, Lodola Francesco, Paternò Giuseppe, Maya-Vetencourt Jose Fernando

Descrizione

Retinal dystrophies, such as retinitis pigmentosa and senile macular degeneration, are caused by genetic mutations that compromise the survival of the cones and rods and there is no pharmacological treatment to prevent photoreceptor degeneration, by now.

The invention relates to a family of photochromic amphiphilic molecules that spontaneously place themselves in the cell membrane and generate a significant variation in the membrane potential following a light stimulus. These properties are particularly advantageous in the modulation of the activity of neurons, as demonstrated by the generation of firing signals following photoexcitation in neuronal networks containing synaptic blockers. Photomediable azobenzene molecules for cellular photostimulation are already known, however they are specifically bound to K + channels, blocking them in dark conditions and returning to a physiological configuration under illumination with the reopening of the channels themselves. This means that the conformational state of the photochromic molecule interferes with the cell physiology.

The molecules described here, on the other hand, do not have a specific affinity with the cellular exchange channels and are located in the phospholipid layer. These characteristics give the compounds of the invention the ability to photo-regulate membrane turnover and secretory activity, allowing to separate neuronal photostimulation from physiological activity. These molecules are used in the optical stimulation of animal cells. In particular, the molecules of the invention have proved ability to restoring the neuronal activity in the animal model and are, therefore, particularly promising in the treatment, by means of intraocular injection, of degenerative diseases of the retina, such as retinitis pigmentosa and senile macular degeneration.

Campo di applicazione

<p> The invention relates to the field of photopharmacology for the optical stimulation of cells, in particular retinal photoreceptors damaged by degenerative diseases such as retinitis pigmentosa and senile macular degeneration. This field can be extend to different cell photojustment applications. </p>

Vantaggi

<p> • Relevant reversible variation of membrane potential </p> <p>• Elimination of the hyperexcitability caused by blockage of the K + channels </p> <p>• Increase of the half-life of the compound </p> <p>• Activity with visible light instead of ultraviolet harmful to the eyes and in general for biological tissues </p>

Stadio di sviluppo

Test on animals

Contatto

licensing.tto@polimi.it

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