FFC#9/2021

Lead optimization of MKT-077 analogues as HSP70 allosteric inhibitors combined with F508del CFTR correctors: a multi-drug approach to contrast cystic fibrosis

AREA 1 Therapies to correct the underlying defect

FFC#9/2021

Lead optimization of MKT-077 analogues as HSP70 allosteric inhibitors combined with F508del CFTR correctors: a multi-drug approach to contrast cystic fibrosis
€ 0 still needed
0%
€ 102.000 goal

pRINCIPAL INVESTIGATOR

Enrico Millo (Dipartimento di Medicina Sperimentale – DIMES, Università degli Studi di Genova)

Partner

Elena Cichero (Dip. di Farmacia, Università degli Studi di Genova); Santina Bruzzone (Dip. Medicina Sperimentale, Università degli Studi di Genova)

Researchers

11

Category

AREA 1 Therapies to correct the underlying defect

Duration

2 years

Goal

€ 102.000

Funds raised

€ 102.000

Objectives

The effective recovery of the function of the CFTR channel can be achieved with correctors when administered in the presence of allosteric inhibitors of HSP70 (Heat Shock Protein 70), a protein involved in the assembly of protein complexes (such as CFTR). The aim of this project is therefore to identify novel HSP70 inhibitors. Researchers will synthesize new HSP70 inhibitors using conventional methods of chemical synthesis and, with biochemical and functional assays, they will test the effectiveness of the CFTR recovery in the presence of correctors. With bioinformatics methods, chemical synthesis and functional assays, the researchers also aim to generate analogues of a known inhibitor of HSP70, rhodocyanine MKT-077. Combinations of inhibitors and correctors (VX809 and others) will be tested on primary bronchial epithelial cells.


XIX Convention FFC Ricerca – download here a brief presentation of the project

WHO ADOPTED THE PROJECT

Delegazione FFC Ricerca di Como Dongo

€ 102.000

Delegazione FFC Ricerca di Alberobello

€ 25.000

Gruppo di sostegno FFC Ricerca di Bolzano

€ 20.000

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FFC#2/2025

Developing RNA-targeted therapies to regulate gene expression and restore CFTR synthesis