Characterization of Apo‐Form Selective Inhibition of Indoleamine 2,3‐Dioxygenase**,ChemBioChem

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Characterization of Apo‐Form Selective Inhibition of Indoleamine 2,3‐Dioxygenase**
ChemBioChem ( IF 2.6 ) Pub Date : 2020-09-24 , DOI: 10.1002/cbic.202000298
Rodrigo F Ortiz-Meoz ₁ , Liping Wang ₁ , Rosalie Matico ₁ , Anna Rutkowska-Klute ₂ , Martha De la Rosa ₃ , Sabrina Bedard ₁ , Robert Midgett ₁ , Katrin Strohmer ₂ , Douglas Thomson ₂ , Cunyu Zhang ₁ , Makda Mebrahtu ₁ , Jeffrey Guss ₁ , Rachel Totoritis ₁ , Thomas Consler ₁ , Nino Campobasso ₁ , David Taylor ₁ , Tia Lewis ₁ , Kurt Weaver ₁ , Marcel Muelbaier ₂ , John Seal ₁ , Richard Dunham ₃ , Wieslaw Kazmierski ₃ , David Favre ₃ , Giovanna Bergamini ₂ , Lisa Shewchuk ₁ , Alan Rendina ₁ , Guofeng Zhang ₁

Affiliation

Inhibiting IDO1: IDO1 is a heme‐containing tryptophan metabolizing enzyme, and identified as antitumor target. Many groups have achieved effective IDO1 inhibition. This study defines two distinct molecular mechanisms of inhibiting apo and holo forms of IDO1. The approach can serve as an example for enzyme form selective drug screening and design.

中文翻译：

Apo-Form 选择性抑制吲哚胺 2,3-双加氧酶的表征**

抑制 IDO1：IDO1 是一种含有血红素的色氨酸代谢酶，被确定为抗肿瘤靶点。许多小组已经实现了有效的 IDO1 抑制。该研究定义了两种不同的抑制 IDO1 载脂蛋白和全息形式的分子机制。该方法可以作为酶形式选择性药物筛选和设计的一个例子。

更新日期：2020-09-24

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