Literature DB >> 28003141

Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.

Jay A Markwalder1, Steven P Seitz2, Yuval Blat3, Lisa Elkin4, John T Hunt5, Jonathan G Pabalan5, Maria N Jure-Kunkel5, Gregory D Vite2, Kelly Covello5.   

Abstract

The discovery of a series of structurally-novel biaryl urea IDO inhibitors is described. Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to kynurenine led to potent inhibitors with favorable selectivity and metabolic stability profiles.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  IDO; Immuno-oncology; Indoleamine 2,3-dioxygenase; Kynurenine

Mesh：

Substances：

Year:  2016        PMID： 28003141     DOI： 10.1016/j.bmcl.2016.12.015

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  The dawn of vaccines for cancer prevention.

Authors:  Olivera J Finn
Journal:  Nat Rev Immunol       Date:  2017-12-27       Impact factor: 53.106

2.  High-resolution structures of inhibitor complexes of human indoleamine 2,3-dioxygenase 1 in a new crystal form.

Authors:  Shukun Luo; Ke Xu; Shaoyun Xiang; Jie Chen; Chunyun Chen; Chuangxin Guo; Youzhi Tong; Liang Tong
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2018-10-17       Impact factor: 1.056

Review 3.  Nuisance compounds in cellular assays.

Authors:  Jayme L Dahlin; Douglas S Auld; Ina Rothenaigner; Steve Haney; Jonathan Z Sexton; J Willem M Nissink; Jarrod Walsh; Jonathan A Lee; John M Strelow; Francis S Willard; Lori Ferrins; Jonathan B Baell; Michael A Walters; Bruce K Hua; Kamyar Hadian; Bridget K Wagner
Journal:  Cell Chem Biol       Date:  2021-02-15       Impact factor: 8.116

4.  Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form.

Authors:  Micah T Nelp; Patrick A Kates; John T Hunt; John A Newitt; Aaron Balog; Derrick Maley; Xiao Zhu; Lynn Abell; Alban Allentoff; Robert Borzilleri; Hal A Lewis; Zeyu Lin; Steven P Seitz; Chunhong Yan; John T Groves
Journal:  Proc Natl Acad Sci U S A       Date:  2018-03-12       Impact factor: 11.205

5.  Discovery of secondary sulphonamides as IDO1 inhibitors with potent antitumour effects in vivo.

Authors:  Shushan Ge; Haiqing Zhong; Xuewei Ma; Yingbo Zheng; Yi Zou; Fang Wang; Yan Wang; Yue Hu; Yuezhen Li; Wen Liu; Wenjie Guo; Qiang Xu; Yisheng Lai
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
  5 in total

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