Evidence map›Paper›PMID 27884693›Full record

ArticleBioorganic & medicinal chemistry letters2017

Design, synthesis, and characterization of rhein analogs as novel inhibitors of scavenger receptor A.

Yi Zheng, Xia Li, Piyusha P Pagare, Yunyun Yuan, Xiang-Yang Wang, Yan Zhang

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.3field-weighted citation impact, top 30% 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

2 citing papers in PubMed, 4 citations in OpenAlex.

  1. Article
  2. Article
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

6 authors at 1 institution in 1 country.

Yi ZhengDepartment of Medicinal Chemistry, Virginia Commonwealth University, 800 E. Leigh Street, Richmond, VA 23298, United States.
Xia LiDepartment of Human and Molecular Genetics, Virginia Commonwealth University, Richmond, VA 23298, United States.
Piyusha P PagareDepartment of Medicinal Chemistry, Virginia Commonwealth University, 800 E. Leigh Street, Richmond, VA 23298, United States.
Yunyun YuanDepartment of Medicinal Chemistry, Virginia Commonwealth University, 800 E. Leigh Street, Richmond, VA 23298, United States.
Xiang-Yang WangDepartment of Human and Molecular Genetics, Virginia Commonwealth University, Richmond, VA 23298, United States; Institute of Molecular Medicine, Virginia Commonwealth University, Richmond, VA 23298, United States; Massey Cancer Center, Virginia Commonwealth University, Richmond, VA 23298, United States. Electronic address: xywang@vcu.edu.
Yan ZhangDepartment of Medicinal Chemistry, Virginia Commonwealth University, 800 E. Leigh Street, Richmond, VA 23298, United States; Massey Cancer Center, Virginia Commonwealth University, Richmond, VA 23298, United States. Electronic address: yzhang2@vcu.edu.
Virginia Commonwealth University · US

Funding

Large heat shock proteins and their role in cancer therapyR01CA099326 · NCI · ROSWELL PARK CANCER INSTITUTE CORP · PI REPASKY, ELIZABETH A, WANG, XIANG-YANG SHAWN · 2003 to 2020
$5.7M
Host-tumor interactions and cancer relapse after radiation therapyR01CA175033 · NCI · VIRGINIA COMMONWEALTH UNIVERSITY · PI WANG, XIANG-YANG SHAWN · 2014 to 2018
$1.6M
Large Stress Proteins in Biology and MedicineR01CA154708 · NCI · VIRGINIA COMMONWEALTH UNIVERSITY · PI WANG, XIANG-YANG SHAWN · 2011 to 2015
$1.5M
Scavenger Receptor-A and Immune RegulationR01CA129111 · NCI · VIRGINIA COMMONWEALTH UNIVERSITY · PI WANG, XIANG-YANG SHAWN · 2007 to 2011
$1.2M
NCI NIH HHS R01 CA099326NCI NIH HHS R01 CA129111NCI NIH HHS R01 CA154708NCI NIH HHS R01 CA175033
6 · The paper itself

Abstract

Scavenger receptor A (SRA) has been known as an immunosuppressive factor and therefore therapeutic inhibition of SRA may be potentially exploited for cancer immunotherapy. Our previously work suggested that rhein may act as an inhibitor of SRA in reversing immunosuppression of SRA during T cells activation. Herein, three deconstruction analogs of rhein, compound 1, 2, and 3, were further studied as inhibitors of SRA. These three compounds, particularly compound 1, also known as a natural product danthron, enhanced T cells activation, indicated by increased transcriptional activation of interleukin 2 (Il2) gene, production of IL-2 protein, and proliferation of T cells. Additionally, the interaction between these compounds and SRA was studied by molecular modeling. Compound 1 showed a favorable binding mode with the cysteine rich domain of SRA protein compared to compound 2 and 3. Collectively, those results would provide insight for future design and development of next generation rhein derivatives as SRA inhibitors.

Indexed as

Drug DesignAnimalsAnthraquinonesCell Line, TumorCell ProliferationDose-Response Relationship, DrugHumansMiceMolecular Docking SimulationMolecular StructureNeoplasms, ExperimentalScavenger Receptors, Class AStructure-Activity RelationshipT-LymphocytesAnthraquinonesrheinScavenger Receptors, Class ACancer immunotherapyDanthronRheinScavenger receptor A

Identifiers

PMID27884693
PMCPMC5142634
OpenAlexW2550869088

What OpenQuestion holds

Textmetadata
LicenceTDM
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.