Evidence map›Paper›PMID 28968981›Full record

ArticleOncotarget2017

Structure based design, synthesis and activity studies of small hybrid molecules as HDAC and G9a dual inhibitors.

Lanlan Zang, Shukkoor M Kondengaden, Qing Zhang, Xiaobo Li, Dilep K Sigalapalli, Shameer M Kondengadan, Kenneth Huang, Keqin Kathy Li, Shanshan Li, Zhongying Xiao and 6 more

Open access · diamondAbstract read
In one paragraph

Article in Oncotarget, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.6field-weighted citation impact, top 17% 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

9 citing papers in PubMed, 35 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Review
  5. EHMT2/G9a as an Epigenetic Target in Pediatric and Adult Brain Tumors.International journal of molecular sciences · 2021
    Review
  6. Article
  7. Review
  8. Article
  9. Potential Epigenetic-Based Therapeutic Targets for Glioma.Frontiers in molecular neuroscience · 2018
    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

16 authors at 5 institutions in 3 countries.

Lanlan Zang *Central Laboratory, Linyi People's Hospital, Linyi, Shandong 276003, P.R. China.
Shukkoor M Kondengaden *Chemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Qing Zhang *Chemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Xiaobo LiDepartment of Immunology, Collaborative Innovation Center of Tianjin for Medical Epigenetics, Tianjin Key Laboratory of Medical Epigenetics, Tianjin Medical University, Tianjin 300070, P.R. China.
Dilep K SigalapalliDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana 500037, India.
Shameer M KondengadanDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Mohali, Punjab 160062, India.
Kenneth HuangChemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Keqin Kathy LiChemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Shanshan LiChemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Zhongying XiaoChemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Liuqing WenChemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Hailiang ZhuChemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Bathini N BabuDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana 500037, India.
Lijuan WangCentral Laboratory, Linyi People's Hospital, Linyi, Shandong 276003, P.R. China.
Fengyuan CheCentral Laboratory, Linyi People's Hospital, Linyi, Shandong 276003, P.R. China.
Peng George WangChemistry Department and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Georgia State University · USLinyi People's Hospital · CNNational Institute of Pharmaceutical Education and Research · INNational Institute of Pharmaceutical Education and Research · INTianjin Medical University · CN

Funding

Biosynthesis of PolysaccharidesR01GM085267 · NIGMS · OHIO STATE UNIVERSITY · PI WANG, PENG GEORGE · 2009 to 2017
$2.4M
NIGMS NIH HHS R01 GM085267
6 · The paper itself

Abstract

Aberrant enzymatic activities or expression profiles of epigenetic regulations are therapeutic targets for cancers. Among these, histone 3 lysine 9 methylation (H3K9Me2) and global de-acetylation on histone proteins are associated with multiple cancer phenotypes including leukemia, prostatic carcinoma, hepatocellular carcinoma and pulmonary carcinoma. Here, we report the discovery of the first small molecule capable of acting as a dual inhibitor targeting both G9a and HDAC. Our structure based design, synthesis, and screening for the dual activity of the small molecules led to the discovery of compound 14 which displays promising inhibition of both G9a and HDAC in low micro-molar range in cell based assays.

Indexed as

dual inhibitorsepigeneticsG9a inhibitorsHDAC inhibitorspharmacophore

Identifiers

PMID28968981
PMCPMC5609913
OpenAlexW2727030425

What OpenQuestion holds

Textmetadata
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.