Evidence map›Paper›PMID 29932010›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2018

A highly potent and selective inhibitor Roxyl-WL targeting IDO1 promotes immune response against melanoma.

Guangwei Xu, Tianqi Wang, Yongtao Li, Zhi Huang, Xin Wang, Jianyu Zheng, Shengyong Yang, Yan Fan, Rong Xiang

Open access · goldAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.4field-weighted citation impact, top 45% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
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  5. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 3 institutions in 1 country.

Guangwei Xua Department of Medicinal Chemistry, School of Medicine , Nankai University , Tianjin , China.
Tianqi Wanga Department of Medicinal Chemistry, School of Medicine , Nankai University , Tianjin , China.
Yongtao Lia Department of Medicinal Chemistry, School of Medicine , Nankai University , Tianjin , China.
Zhi Huanga Department of Medicinal Chemistry, School of Medicine , Nankai University , Tianjin , China.
Xin Wanga Department of Medicinal Chemistry, School of Medicine , Nankai University , Tianjin , China.
Jianyu Zhengb State Key Laboratory and Institute of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering , Nankai University , Tianjin , China.
Shengyong Yangc State Key Laboratory of Biotherapy and Cancer Center , West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy , Chengdu , China.
Yan Fana Department of Medicinal Chemistry, School of Medicine , Nankai University , Tianjin , China.
Rong Xianga Department of Medicinal Chemistry, School of Medicine , Nankai University , Tianjin , China.
Nankai University · CNSichuan University · CNState Key Laboratory of Chemical Engineering · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Indoleamine 2,3-dioxygenase 1 (IDO1) activity links to immune escape of cancers. Inhibition of IDO1 provides a new approach for cancer treatment. Most clinical IDO1 drugs show marginal efficacy as single agents. On basis of molecular docking and pharmacophore modelling, a novel inhibitor Roxyl-WL was discovered with a half maximal inhibitory concentration (IC50) value of 1 nM against IDO1 and 10-100-fold increased potent activity compared with IDO1 drugs in clinical trials. Roxyl-WL displayed excellent kinase spectrum selectivity with no activity out of the 337 protein kinases. In vitro, Roxyl-WL effectively augmented the proliferation of T cells and reduced the number of regulatory T cell (Tregs).When administered to melanoma (B16F10) tumor-bearing mice orally, Roxyl-WL significantly suppressed tumor growth and induced immune response.

Indexed as

AnimalsCD4-Positive T-LymphocytesCell ProliferationDose-Response Relationship, DrugEnzyme InhibitorsFemaleIndoleamine-Pyrrole 2,3,-DioxygenaseMelanomaMiceMice, Inbred C57BLMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipEnzyme InhibitorsIDO1 protein, mouseIndoleamine-Pyrrole 2,3,-DioxygenaseIDO1immunotherapyinhibitormelanoma

Identifiers

PMID29932010
PMCPMC6022239
OpenAlexW2809087587

What OpenQuestion holds

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LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.