2. Academic Validation
  3. Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase

Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase

  • Eur J Med Chem. 2019 Jan 15:162:455-464. doi: 10.1016/j.ejmech.2018.11.010.
Maria Winters 1,  James B DuHadaway 2,  Khoa N Pham 3,  Ariel Lewis-Ballester 3,  Shorouk Badir 1,  Jenny Wai 1,  Eesha Sheikh 1,  Syun-Ru Yeh 3,  George C Prendergast 4,  Alexander J Muller 5,  William P Malachowski 6
Affiliations

Affiliations

  • 1 Department of Chemistry, Bryn Mawr College, Bryn Mawr, PA, 19010, USA.
  • 2 Lankenau Institute for Medical Research, 100 Lancaster Ave, Wynnewood, PA 19096, USA.
  • 3 Department of Physiology and Biophysics, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461, United States.
  • 4 Lankenau Institute for Medical Research, 100 Lancaster Ave, Wynnewood, PA 19096, USA; Department of Pathology, Anatomy & Cell Biology and, Philadelphia, PA 19104, USA; Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA 19104, USA. Electronic address: prendergast@limr.org.
  • 5 Lankenau Institute for Medical Research, 100 Lancaster Ave, Wynnewood, PA 19096, USA; Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA 19104, USA. Electronic address: muller@limr.org.
  • 6 Department of Chemistry, Bryn Mawr College, Bryn Mawr, PA, 19010, USA. Electronic address: wmalacho@brynmawr.edu.
PMID: 30469041 DOI: 10.1016/j.ejmech.2018.11.010
Abstract

Tryptophan (Trp) catabolizing Enzymes play an important and complex role in the development of Cancer. Significant evidence implicates them in a range of inflammatory and immunosuppressive activities. Whereas inhibitors of indoleamine 2,3-dioxygenase-1 (IDO1) have been reported and analyzed in the clinic, fewer inhibitors have been described for tryptophan dioxygenase (TDO) and indoleamine 2,3-dioxygenase-2 (IDO2) which also have been implicated more recently in Cancer, inflammation and immune control. Consequently the development of dual or pan inhibitors of these Trp catabolizing Enzymes may represent a therapeutically important area of research. This is the first report to describe the development of dual and pan inhibitors of IDO1, TDO and IDO2.

Keywords

Antitumor therapy; Diaryl oalkylhydroxylamines; Dual inhibitor; IDO1 inhibition; IDO2 inhibition; Pan inhibition; TDO inhibition.

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