Evidence map›Paper›PMID 29302039›Full record

ArticleNature communications2018

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors.

Jay H Kalin, Muzhou Wu, Andrea V Gomez, Yun Song, Jayanta Das, Dawn Hayward, Nkosi Adejola, Mingxuan Wu, Izabela Panova, Hye Jin Chung and 24 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Nature communications, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 142 papers.

0numbers the graph read from it
0cells of the map it votes in
142citing papers in PubMed
–field-weighted citation impact
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

142 citing papers in PubMed.

  1. Article
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  7. Review
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  11. Review
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  14. Epstein-Barr Virus Encoded lncRNAs Control the Viral Lytic Switch.bioRxiv : the preprint server for biology · 2025
    Article
  15. Review
  16. Article
  17. Article
  18. Review
  19. Small-Molecule Drugs in Pediatric Neuro-Oncology.Current oncology (Toronto, Ont.) · 2025
    Review
  20. Article

82 more citing papers are in PubMed but not listed here.

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

34 authors.

Jay H KalinDivision of Genetics, Departments of Medicine and Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Brigham and Women's Hospital, Boston, MA, 02115, USA.
Muzhou WuDepartment of Dermatology, Boston University School of Medicine, Boston, MA, 02118, USA.
Andrea V GomezDepartment of Biology and Biotechnology, University of Pavia, 27100, Pavia, Italy.
Yun SongDepartment of Molecular and Cell Biology, University of Leicester, Leicester, LE1 9HN, UK.
Jayanta DasDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Dawn HaywardDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Nkosi AdejolaDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Mingxuan WuDivision of Genetics, Departments of Medicine and Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Brigham and Women's Hospital, Boston, MA, 02115, USA.
Izabela PanovaDepartment of Dermatology, Boston University School of Medicine, Boston, MA, 02118, USA.
Hye Jin ChungDepartment of Dermatology, Boston University School of Medicine, Boston, MA, 02118, USA.
Edward KimDepartment of Dermatology, Boston University School of Medicine, Boston, MA, 02118, USA.
Holly J RobertsDepartment of Dermatology, Boston University School of Medicine, Boston, MA, 02118, USA.
Justin M RobertsDepartment of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, USA.ORCID http://orcid.org/0000-0001-6112-7476
Polina PrusevichDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Jeliazko R JeliazkovProgram in Molecular Biophysics, Johns Hopkins University, Baltimore, MD, 21218, USA.
Shourya S Roy BurmanDepartment of Chemical and Biomolecular Engineering, Johns Hopkins University, Baltimore, MD, 21218, USA.
Louise FairallDepartment of Molecular and Cell Biology, University of Leicester, Leicester, LE1 9HN, UK.
Charles MilanoDepartment of Molecular and Cell Biology, University of Leicester, Leicester, LE1 9HN, UK.
Abdulkerim ErogluDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Charlotte M ProbyDivision of Cancer Research, Jacqui Wood Cancer Centre, University of Dundee, Dundee, DD1 9SY, UK.
Albena T Dinkova-KostovaDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Wayne W HancockDepartment of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine, Philadelphia, PA, 19104, USA.
Jeffrey J GrayProgram in Molecular Biophysics, Johns Hopkins University, Baltimore, MD, 21218, USA.ORCID http://orcid.org/0000-0001-6380-2324
James E BradnerDepartment of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, USA.ORCID http://orcid.org/0000-0002-2718-4415
Sergio ValentePasteur Institute, Cenci-Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, 00185, Rome, Italy.
Antonello MaiPasteur Institute, Cenci-Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, 00185, Rome, Italy.
Nicole M AndersSidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Michelle A RudekSidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Yong HuDepartment of Oncology, BioDuro LLC, Shanghai, 200131, China.
Byungwoo RyuDepartment of Dermatology, Boston University School of Medicine, Boston, MA, 02118, USA.
John W R SchwabeDepartment of Molecular and Cell Biology, University of Leicester, Leicester, LE1 9HN, UK. js336@leicester.ac.uk.
Andrea MatteviDepartment of Biology and Biotechnology, University of Pavia, 27100, Pavia, Italy. andrea.mattevi@unipv.it.ORCID http://orcid.org/0000-0002-9523-7128
Rhoda M AlaniDepartment of Dermatology, Boston University School of Medicine, Boston, MA, 02118, USA. alani@bu.edu.
Philip A ColeDivision of Genetics, Departments of Medicine and Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Brigham and Women's Hospital, Boston, MA, 02115, USA. pacole@bwh.harvard.edu.

Funding

BIOCHEMISTRY, CELLULAR AND MOLECULAR BIOLOGY PROGRAMT32GM007445 · NIGMS · JOHNS HOPKINS UNIVERSITY · PI GREEN, RACHEL · 1985 to 2021
$24.1M
Chemical Approaches to Protein PhosphorylationR01CA074305 · NCI · JOHNS HOPKINS UNIVERSITY · PI COLE, PHILIP A · 2002 to 2025
$8.0M
Protein Acylation and Methylation Mechanisms_Administrative SupplementR37GM062437 · NIGMS · JOHNS HOPKINS UNIVERSITY · PI COLE, PHILIP A · 2013 to 2022
$4.1M
Prediction of the Structure of Therapeutic Antibodies with their AntigensR01GM078221 · NIGMS · JOHNS HOPKINS UNIVERSITY · PI GRAY, JEFFREY J · 2006 to 2020
$4.0M
Targeting Transcriptional Co-repressor CoREST Complex in MelanomaR01CA212639 · NCI · HACKENSACK UNIVERSITY MEDICAL CENTER · PI RYU, BYUNGWOO · 2017 to 2021
$2.0M
Histone Lysine deMethylation: Structures, Inhibitions and MechanismsR01GM114306 · NIGMS · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI CHENG, XIAODONG · 2015 to 2018
$1.2M
Cancer Research UK 10270Cancer Research UK 18644NCI NIH HHS R01 CA074305NCI NIH HHS R01 CA212639NIGMS NIH HHS R01 GM078221NIGMS NIH HHS R01 GM114306NIGMS NIH HHS R37 GM062437NIGMS NIH HHS T32 GM007445Wellcome Trust 100237/Z/12/Z
6 · The paper itself

Abstract

Here we report corin, a synthetic hybrid agent derived from the class I HDAC inhibitor (entinostat) and an LSD1 inhibitor (tranylcypromine analog). Enzymologic analysis reveals that corin potently targets the CoREST complex and shows more sustained inhibition of CoREST complex HDAC activity compared with entinostat. Cell-based experiments demonstrate that corin exhibits a superior anti-proliferative profile against several melanoma lines and cutaneous squamous cell carcinoma lines compared to its parent monofunctional inhibitors but is less toxic to melanocytes and keratinocytes. CoREST knockdown, gene expression, and ChIP studies suggest that corin's favorable pharmacologic effects may rely on an intact CoREST complex. Corin was also effective in slowing tumor growth in a melanoma mouse xenograft model. These studies highlight the promise of a new class of two-pronged hybrid agents that may show preferential targeting of particular epigenetic regulatory complexes and offer unique therapeutic opportunities.

Indexed as

AgedAnimalsAntineoplastic AgentsBenzamidesCell Line, TumorCell ProliferationCo-Repressor ProteinsDrug DesignDrug Screening Assays, AntitumorFemaleHistone Deacetylase InhibitorsHistone DeacetylasesHumansMaleMelanomaMiceAntineoplastic AgentsBenzamidesCo-Repressor ProteinsentinostatHistone Deacetylase InhibitorsHistone DeacetylasesNerve Tissue ProteinsPyridinesRCOR1 protein, humanRcor2 protein, mouseRepressor ProteinsTranylcypromine

Identifiers

PMID29302039
PMCPMC5754352

What OpenQuestion holds

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Registered trials

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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.