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general/1-alkyltryptamines

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1-Methyltryptophan

1-Methyltryptophan is a chemical compound that is an inhibitor of the tryptophan catabolic enzyme indoleamine 2,3-dioxygenase (IDO or INDO ). It is a chiral compound that can exist as both D- and L-enantiomers.

The L-isomer (L-1MT) inhibits IDO weakly but also serves as an enzyme substrate.

The D-isomer (D-1MT) does not inhibit IDO at all, but it can inhibit the IDO-related enzyme IDO2 and restore mTOR signaling in cells starved of tryptophan due to IDO activity. D-1MT is also known as indoximod and it was in clinical trials for cancer treatment, such as for advanced melanoma, in 2017.

A U.S. patent covering salt and prodrug formulations of indoximod was issued to NewLink Genetics on August 15, 2017, providing exclusivity until at least 2036.

References

References

  1. (1991). "1-Methyl-{{small". Archives of Biochemistry and Biophysics.
  2. (2007). "Novel tryptophan catabolic enzyme IDO2 is the preferred biochemical target of the antitumor indoleamine 2,3-dioxygenase inhibitory compound {{small". Cancer Research.
  3. (2012). "IDO inhibits a tryptophan sufficiency signal that stimulates mTOR: A novel IDO effector pathway targeted by {{small". OncoImmunology.
  4. [http://www.onclive.com/publications/oncology-live/2017/vol-18-no-16/ido-inhibitors-emerging-as-new-players-on-checkpoint-blockade-scene?p=2 IDO Inhibitors Emerging as New Players on Checkpoint Blockade Scene. Aug 2017]
  5. "NewLink Genetics".
  6. (April 9, 2018). "NewLink Genetics Annual Report (Form 10-K)".
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1-alkyltryptamines alpha-amino-acids oxidoreductase-inhibitors
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