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Structure and Plasticity of Indoleamine 2,3-Dioxygenase 1 (IDO1)

Published inJournal of medicinal chemistry, vol. 64, no. 24, p. 17690-17705
Publication date2021-12-23
First online date2021-12-15
Abstract

Since the discovery of the implication of indoleamine 2,3-dioxygenase 1 (IDO1) in tumoral immune resistance in 2003, the search for inhibitors has been intensely pursued both in academia and in pharmaceutical companies, supported by the publication of the first crystal structure of IDO1 in 2006. More recently, it has become clear that IDO1 is an important player in various biological pathways and diseases ranging from neurodegenerative diseases to infection and autoimmunity. Its inhibition may lead to clinical benefit in different therapeutic settings. At present, over 50 experimental structures of IDO1 in complex with different ligands are available in the Protein Data Bank. Our analysis of this wealth of structural data sheds new light on several open issues regarding IDO1's structure and function.

Keywords
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / antagonists & inhibitors
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / chemistry
  • Structure-Activity Relationship
Affiliation entities Not a UNIGE publication
Citation (ISO format)
RÖHRIG, Ute F, MICHIELIN, Olivier, ZOETE, Vincent. Structure and Plasticity of Indoleamine 2,3-Dioxygenase 1 (IDO1). In: Journal of medicinal chemistry, 2021, vol. 64, n° 24, p. 17690–17705. doi: 10.1021/acs.jmedchem.1c01665
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Journal ISSN0022-2623
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