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临床试验中用于癌症免疫治疗的吲哚胺 2,3-双加氧酶 1（IDO1）抑制剂。

Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors in clinical trials for cancer immunotherapy.

机构信息

School of Pharmaceutical Sciences and Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, 450001, China.

School of Life Sciences, Zhengzhou University, Zhengzhou, 450001, China.

出版信息

J Hematol Oncol. 2021 Apr 21;14(1):68. doi: 10.1186/s13045-021-01080-8.

DOI:10.1186/s13045-021-01080-8
PMID:33883013
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8061021/
Abstract

Indoleamine 2,3-dioxygenase 1 (IDO1) is a heme enzyme that catalyzes the oxidation of L-tryptophan. Functionally, IDO1 has played a pivotal role in cancer immune escape via catalyzing the initial step of the kynurenine pathway, and overexpression of IDO1 is also associated with poor prognosis in various cancers. Currently, several small-molecule candidates and peptide vaccines are currently being assessed in clinical trials. Furthermore, the "proteolysis targeting chimera" (PROTAC) technology has also been successfully used in the development of IDO1 degraders, providing novel therapeutics for cancers. Herein, we review the biological functions of IDO1, structural biology and also extensively summarize medicinal chemistry strategies for the development of IDO1 inhibitors in clinical trials. The emerging PROTAC-based IDO1 degraders are also highlighted. This review may provide a comprehensive and updated overview on IDO1 inhibitors and their therapeutic potentials.

摘要

吲哚胺 2,3-双加氧酶 1（IDO1）是一种血红素酶，可催化 L-色氨酸的氧化。从功能上讲，IDO1 通过催化犬尿氨酸途径的起始步骤，在癌症免疫逃逸中发挥了关键作用，IDO1 的过表达也与各种癌症的预后不良有关。目前，几种小分子候选药物和肽疫苗正在临床试验中进行评估。此外，“蛋白水解靶向嵌合体”（PROTAC）技术也已成功用于 IDO1 降解剂的开发，为癌症提供了新的治疗方法。本文综述了 IDO1 的生物学功能、结构生物学，并广泛总结了临床试验中 IDO1 抑制剂的药物化学策略。还强调了新兴的基于 PROTAC 的 IDO1 降解剂。这篇综述可能提供了关于 IDO1 抑制剂及其治疗潜力的全面和最新概述。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/2c01442e5148/13045_2021_1080_Fig12_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/b3f907aa787c/13045_2021_1080_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/2c01442e5148/13045_2021_1080_Fig12_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/af18c6d56a0f/13045_2021_1080_Fig1_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/855f7541b834/13045_2021_1080_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/ba17cea98807/13045_2021_1080_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/6746479c8eef/13045_2021_1080_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/3473bd6f27c8/13045_2021_1080_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/43fe404ffa7c/13045_2021_1080_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/de4cc7d062b0/13045_2021_1080_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/86f0c8bf3d65/13045_2021_1080_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/1c8d04274607/13045_2021_1080_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/b3f907aa787c/13045_2021_1080_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86af/8061021/2c01442e5148/13045_2021_1080_Fig12_HTML.jpg

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引用本文的文献

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Dual regulation of gastrointestinal tumor progression by the IFN-γ/STAT1 pathway and prospects for targeted therapy.

Front Oncol. 2025-8-20

[2]
Indoleamine 2,3-dioxygenase 1 in cancer immunotherapy: from small-molecule inhibition to PROTAC-mediated degradation.

Front Pharmacol. 2025-8-12

[3]
Expression of immune checkpoints (IDO and PD-L1) in oral tongue cancer patients: a 10-year retrospective cohort study in Pakistan.

Front Oncol. 2025-8-12

[4]
Role of indoleamine 2,3-Dioxygenase 1 in modulating the malignant biological behavior of cervical cancer cells through the Tryptophan-Kynurenine pathway.

J Mol Histol. 2025-8-22

[5]
Substituted 1,4-naphthoquinones for potential anticancer therapeutics: cytotoxic effects and QSAR-guided design of new analogs.

Comput Struct Biotechnol J. 2025-7-25

[6]
Targeted protein degradation with small molecules for cancer immunotherapy.

Asian J Pharm Sci. 2025-8

[7]
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J Clin Med. 2025-7-19

[8]
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Front Immunol. 2025-7-9

[9]
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[10]
Lymphatic dissemination of HPV-positive oropharyngeal squamous cell carcinoma: underlying mechanisms and treatment innovations.

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本文引用的文献

[1]
PROTACs to address the challenges facing small molecule inhibitors.

Eur J Med Chem. 2021-1-15

[2]
Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1.

Acta Pharm Sin B. 2020-10

[3]
Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges.

Eur J Med Chem. 2021-1-15

[4]
PROTACs: New method to degrade transcription regulating proteins.

Eur J Med Chem. 2020-12-1

[5]
Indoximod opposes the immunosuppressive effects mediated by IDO and TDO via modulation of AhR function and activation of mTORC1.

Oncotarget. 2020-6-23

[6]
A phase 1 study of PF-06840003, an oral indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor in patients with recurrent malignant glioma.

Invest New Drugs. 2020-12

[7]
Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.

Eur J Med Chem. 2020-7-15

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Cell Intrinsic and Systemic Metabolism in Tumor Immunity and Immunotherapy.

Cancers (Basel). 2020-4-1

[9]
Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to Pharmacodynamic Activity.

J Med Chem. 2020-3-17

[10]
Interferon-Induced IDO1 Mediates Radiation Resistance and Is a Therapeutic Target in Colorectal Cancer.

Cancer Immunol Res. 2020-3-3

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