Evidence map›Paper›PMID 27878989›Full record

ArticleFEBS letters2017

Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors.

Taekyu Lee, Zhiguo Bian, Bin Zhao, Leah J Hogdal, John L Sensintaffar, Craig M Goodwin, Johannes Belmar, Subrata Shaw, James C Tarr, Nagarathanam Veerasamy and 14 more

Open access · greenAbstract readLetter
In one paragraph

Article in FEBS letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.

0numbers the graph read from it
0cells of the map it votes in
28citing papers in PubMed
4.4field-weighted citation impact, top 4% 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

28 citing papers in PubMed, 61 citations in OpenAlex.

  1. Saga of MCL1 inhibitors in multiple myeloma.Biochemical pharmacology · 2026
    Review
  2. Article
  3. Article
  4. Review
  5. Review
  6. Article
  7. Macrophage-enriched novel functional long noncoding RNAs LRRC75A-AS1 and GAPLINC regulate polarization and innate immune responses.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2024
    Article
  8. Article
  9. Article
  10. BH3-mimetics: recent developments in cancer therapy.Journal of experimental & clinical cancer research : CR · 2021
    Review
  11. Review
  12. Targeting MCL-1 in cancer: current status and perspectives.Journal of hematology & oncology · 2021
    Review
  13. Review
  14. Targeting apoptosis in cancer therapy.Nature reviews. Clinical oncology · 2020
    Review
  15. Review
  16. Article
  17. Article
  18. Article
  19. Article
  20. 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

24 authors at 5 institutions in 1 country.

Taekyu LeeDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Zhiguo BianDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Bin ZhaoDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Leah J HogdalDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
John L SensintaffarDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Craig M GoodwinDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Johannes BelmarDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Subrata ShawDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
James C TarrDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Nagarathanam VeerasamyDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Shannon M MatulisDepartment of Hematology and Medical Oncology and The Winship Cancer Institute, Emory University, Atlanta, GA, USA.
Brian KossDepartment of Cell and Molecular Biology, St. Jude Children's Research Hospital, Memphis, TN, USA.
Melissa A FischerVanderbilt University Medical Center, Nashville, TN, USA.
Allison L ArnoldDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
DeMarco V CamperDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Carrie F BrowningDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Olivia W RossaneseDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Amit BudhrajaDepartment of Cell and Molecular Biology, St. Jude Children's Research Hospital, Memphis, TN, USA.
Joseph OpfermanDepartment of Cell and Molecular Biology, St. Jude Children's Research Hospital, Memphis, TN, USA.
Lawrence H BoiseDepartment of Hematology and Medical Oncology and The Winship Cancer Institute, Emory University, Atlanta, GA, USA.
Michael R SavonaVanderbilt University Medical Center, Nashville, TN, USA.
Anthony LetaiDepartment of Adult Oncology, The Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.
Edward T OlejniczakDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Stephen W FesikDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.
Vanderbilt University · USSt. Jude Children's Research Hospital · USPiedmont Cancer Institute · USVanderbilt University Medical Center · USHarvard University · US

Funding

TYROSINE KINASE ONCOGENESIS IN MYELOID LEUKEMIAP01CA066996 · NCI · DANA-FARBER CANCER INSTITUTE · PI MATTHEW S DAVIDS · 1996 to 2026
$52.5M
TISSUE CoreP50CA098131 · NCI · VANDERBILT UNIVERSITY MEDICAL CENTER · PI PARK, BEN HO, PIETENPOL, JENNIFER A · 2003 to 2024
$48.7M
Expanding the druggable genomeDP1CA174419 · NCI · VANDERBILT UNIVERSITY · PI FESIK, STEPHEN W. · 2012 to 2014
$2.3M
Pathway Specific Combinational Therapy in Poor Prognosis B-Lineage Acute Lymphoblastic LeukemiaR01CA201069 · NCI · ST. JUDE CHILDREN'S RESEARCH HOSPITAL · PI OPFERMAN, JOSEPH T. · 2016 to 2020
$2.0M
Expanding the druggable genomeDP1OD006933 · OD · VANDERBILT UNIVERSITY · PI FESIK, STEPHEN W. · 2010 to 2011
$1.5M
Console upgrades for biological NMR spectrometersS10RR025677 · NCRR · VANDERBILT UNIVERSITY · PI SANDERS, CHARLES R · 2009 to 2009
$460k
CCR NIH HHS HHSN261200800001CNCI NIH HHS DP1 CA174419NCI NIH HHS HHSN261200800001ENCI NIH HHS P01 CA066996NCI NIH HHS P50 CA098131NCI NIH HHS R01 CA201069NCRR NIH HHS S10 RR025677NIH HHS DP1 OD006933
6 · The paper itself

Abstract

Myeloid cell leukemia 1 (Mcl-1) is an antiapoptotic member of the Bcl-2 family of proteins that when overexpressed is associated with high tumor grade, poor survival, and resistance to chemotherapy. Mcl-1 is amplified in many human cancers, and knockdown of Mcl-1 using RNAi can lead to apoptosis. Thus, Mcl-1 is a promising cancer target. Here, we describe the discovery of picomolar Mcl-1 inhibitors that cause caspase activation, mitochondrial depolarization, and selective growth inhibition. These compounds represent valuable tools to study the role of Mcl-1 in cancer and serve as useful starting points for the discovery of clinically useful Mcl-1 inhibitors. PDB ID CODES: Comp. 2: 5IEZ; Comp. 5: 5IF4.

Indexed as

AnimalsAntineoplastic AgentsBcl-2-Like Protein 11bcl-X ProteinCell Line, TumorCell ProliferationCell SurvivalDrug DesignDrug DiscoveryHumansImmunoprecipitationMembrane Potential, MitochondrialMiceMyeloid Cell Leukemia Sequence 1 ProteinAntineoplastic AgentsBcl-2-Like Protein 11bcl-X ProteinMyeloid Cell Leukemia Sequence 1 Proteinapoptosiscancerdrug discoverymyeloid cell leukemia 1structure-based drug design

Identifiers

PMID27878989
PMCPMC5381274
OpenAlexW2550870820

What OpenQuestion holds

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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.