2. Academic Validation
  3. Fragment-based approach to identify IDO1 inhibitor building blocks

Fragment-based approach to identify IDO1 inhibitor building blocks

  • Eur J Med Chem. 2017 Dec 1;141:169-177. doi: 10.1016/j.ejmech.2017.09.044.
Alice Coletti 1,  Francesca Camponeschi 2,  Elisa Albini 3,  Francesco Antonio Greco 1,  Vincenzo Maione 2,  Chiara Custodi 1,  Federica Ianni 1,  Ursula Grohmann 3,  Ciriana Orabona 3,  Francesca Cantini 4,  Antonio Macchiarulo 5
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
  • 2 Center for Magnetic Resonance, University of Florence, Via L. Sacconi 6, 50019 Sesto Fiorentino (FI), Italy.
  • 3 Department of Experimental Medicine, University of Perugia, P.le Gambuli, 06132 Perugia, Italy.
  • 4 Center for Magnetic Resonance, University of Florence, Via L. Sacconi 6, 50019 Sesto Fiorentino (FI), Italy; Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019 Sesto Fiorentino (FI), Italy.
  • 5 Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy. Electronic address: antonio.macchiarulo@unipg.it.
PMID: 29031064 DOI: 10.1016/j.ejmech.2017.09.044
Abstract

Indoleamine 2,3-dioxygenase 1 (IDO1) is attracting a great deal of interest as drug target in immune-oncology 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.

Keywords

Cancer; Fragment-based; IDO; Immune; Inhibitor; Thermophoresis; Tryptophan; Water-LOGSY.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z