Indoleamine 2,3-dioxygenase 1 (IDO1) is attracting a great deal of interest as drug target in immuneoncology being highly expressed in cancer cells and participating to the tumor immune-editing process. Although several classes of IDO1 inhibitors have been reported in literature and patent applications, only few compounds have proved optimal pharmacological profile in preclinical studies to be advanced in clinical trials. Accordingly, the quest for novel structural classes of IDO1 inhibitors is still open. In this paper, we report a fragment-based screening campaign that combines Water-LOGSY NMR experiments and microscale thermophoresis approach to identify fragments that may be helpful for the development of novel IDO1 inhibitors as therapeutic agents in immune-oncology disorders.

Fragment-based approach to identify IDO1 inhibitor building blocks

Coletti, Alice;Albini, Elisa;Greco, Francesco Antonio;Custodi, Chiara;Ianni, Federica;Grohmann, Ursula;Orabona, Ciriana;Macchiarulo, Antonio
2017

Abstract

Indoleamine 2,3-dioxygenase 1 (IDO1) is attracting a great deal of interest as drug target in immuneoncology being highly expressed in cancer cells and participating to the tumor immune-editing process. Although several classes of IDO1 inhibitors have been reported in literature and patent applications, only few compounds have proved optimal pharmacological profile in preclinical studies to be advanced in clinical trials. Accordingly, the quest for novel structural classes of IDO1 inhibitors is still open. In this paper, we report a fragment-based screening campaign that combines Water-LOGSY NMR experiments and microscale thermophoresis approach to identify fragments that may be helpful for the development of novel IDO1 inhibitors as therapeutic agents in immune-oncology disorders.
2017
File in questo prodotto:
File Dimensione Formato  
1-s2.0-S0223523417307596-main.pdf

accesso aperto

Descrizione: Full text
Tipologia di allegato: PDF-editoriale
Licenza: Creative commons
Dimensione 1.32 MB
Formato Adobe PDF
1.32 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/11391/1421951
Citazioni
  • ???jsp.display-item.citation.pmc??? 3
  • Scopus 16
  • ???jsp.display-item.citation.isi??? 16
social impact