Human African trypanosomiasis (HAT), Chagas disease and leishmaniasis, belong to a group of infectious diseases defined as neglected tropical diseases, induced by infection with protozoan parasites named trypanosomatids. Current drugs present several issues and the development of new candidates appears to be needed. The majority of the current therapeutic trypanosomatid targets are represented by enzymes or cell surface receptors. Among these, eukaryotic protein kinases represent a major group of protein targets whose modulation may be beneficial for the treatment of neglected tropical protozoan diseases. This review summarizes over the finding of new hit compounds for neglected tropical protozoan diseases, by repurposing known human kinase inhibitors on trypanosomatids. Kinase inhibitors were grouped by human kinase family and discussed according to the screenings (target-based or phenotypic) reported for these drugs on trypanosomatids. This collection aims to provide an insight into repurposed human kinase inhibitors and their importance in the development of new chemical entities with potential beneficial effects on trypanosomatids diseases.

Repurposing of human kinase inhibitors in neglected protozoan diseases

Dichiara Maria;Marrazzo Agostino;Prezzavento Orazio;Rescifina Antonio;Amata Emanuele
2017-01-01

Abstract

Human African trypanosomiasis (HAT), Chagas disease and leishmaniasis, belong to a group of infectious diseases defined as neglected tropical diseases, induced by infection with protozoan parasites named trypanosomatids. Current drugs present several issues and the development of new candidates appears to be needed. The majority of the current therapeutic trypanosomatid targets are represented by enzymes or cell surface receptors. Among these, eukaryotic protein kinases represent a major group of protein targets whose modulation may be beneficial for the treatment of neglected tropical protozoan diseases. This review summarizes over the finding of new hit compounds for neglected tropical protozoan diseases, by repurposing known human kinase inhibitors on trypanosomatids. Kinase inhibitors were grouped by human kinase family and discussed according to the screenings (target-based or phenotypic) reported for these drugs on trypanosomatids. This collection aims to provide an insight into repurposed human kinase inhibitors and their importance in the development of new chemical entities with potential beneficial effects on trypanosomatids diseases.
2017
drug discovery; kinase inhibitor; Neglected Tropical Diseases; parasites; Repurposing
File in questo prodotto:
File Dimensione Formato  
cmdc201700259.pdf

accesso aperto

Tipologia: Versione Editoriale (PDF)
Dimensione 1.85 MB
Formato Adobe PDF
1.85 MB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11769/298151
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 25
  • ???jsp.display-item.citation.isi??? 24
social impact