Evidence map›Paper›PMID 26954567›Full record

ArticlePloS one2016

Inhibition of CXCR4 by LY2624587, a Fully Humanized Anti-CXCR4 Antibody Induces Apoptosis of Hematologic Malignancies.

Sheng-Bin Peng, Xiaoyi Zhang, Donald Paul, Lisa M Kays, Ming Ye, Peter Vaillancourt, Michele Dowless, Louis F Stancato, Julie Stewart, Mark T Uhlik and 3 more

Open access · goldAbstract read
In one paragraph

Article in PloS one, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.

0numbers the graph read from it
0cells of the map it votes in
40citing papers in PubMed
4.3field-weighted citation impact, top 5% 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

40 citing papers in PubMed, 58 citations in OpenAlex.

  1. Trial
  2. Anti-myeloma activity of the CXCR4 antagonist WZ811.Journal of molecular medicine (Berlin, Germany) · 2026
    Article
  3. Review
  4. Review
  5. Review
  6. Article
  7. Modulation of infiltrating CD206The European respiratory journal · 2025
    Article
  8. Review
  9. Structural insights into CXCR4 modulation and oligomerization.Nature structural & molecular biology · 2025
    Article
  10. Review
  11. CXC chemokine receptor 4 (CXCR4) blockade in cancer treatment.Journal of cancer research and clinical oncology · 2023
    Review
  12. CXCL12-CXCR4/CXCR7 Axis in Cancer: from Mechanisms to Clinical Applications.International journal of biological sciences · 2023
    Review
  13. Review
  14. Article
  15. Review
  16. Article
  17. Article
  18. Therapeutic Targeting of the Leukaemia Microenvironment.International journal of molecular sciences · 2021
    Review
  19. Review
  20. 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

13 authors at 1 institution in 1 country.

Sheng-Bin PengLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Xiaoyi ZhangLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Donald PaulLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Lisa M KaysLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Ming YeLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Peter VaillancourtLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Michele DowlessLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Louis F StancatoLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Julie StewartLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Mark T UhlikLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Haiyan LongLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Shaoyou ChuLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Victor H ObunguLilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, 46285, United States of America.
Eli Lilly (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

SDF-1 and CXCR4 are a chemokine and chemokine receptor pair playing critical roles in tumorigenesis. Overexpression of CXCR4 is a hallmark of many hematological malignancies including acute myeloid leukemia, chronic lymphocytic leukemia and non-Hodgkin's lymphoma, and generally correlates with a poor prognosis. In this study, we developed a humanized anti-CXCR4 monoclonal antibody, LY2624587 as a potent CXCR4 antagonist that was advanced into clinical study for cancer. LY2624587 blocked SDF-1 binding to CXCR4 with an IC50 of 0.26 nM, and inhibited SDF-1-induced GTP binding with a Kb of 0.66 nM. In human lymphoma U937 and leukemia CCRF-CEM cells expressing endogenous CXCR4, LY2624587 inhibited SDF-1-induced cell migration with IC50 values of 3.7 and 0.26 nM, respectively. This antibody also inhibited CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT in tumor cells expressing CXCR4. Bifocal microscopic and flow cytometry analyses revealed that LY2624587 mediated receptor internalization and caused CXCR4 down-regulation on the cell surface. In human hematologic cancer cells, LY2624587 caused dose dependent apoptosis in vitro and in vivo. In mouse xenograft models developed with human leukemia and lymphoma cells expressing high levels of CXCR4, LY2624587 exhibited dose-dependent tumor growth inhibition and provided significant survival benefit in a disseminated lymphoma model. Collectively, we have demonstrated that CXCR4 inhibition by LY2624587 has the potential for the treatment of human hematological malignancies.

Indexed as

AnimalsAnnexin A5Antibodies, Monoclonal, HumanizedAntineoplastic AgentsApoptosisCaspase 3Cell Line, TumorCell MovementCell ProliferationChemokine CXCL12Disease Models, AnimalDose-Response Relationship, DrugDown-RegulationExtracellular Signal-Regulated MAP KinasesHematologic NeoplasmsHumansAnnexin A5Antibodies, Monoclonal, HumanizedAntineoplastic AgentsCaspase 3Chemokine CXCL12Extracellular Signal-Regulated MAP KinasesLY2624587Proto-Oncogene Proteins c-aktReceptors, CXCR4

Identifiers

PMID26954567
PMCPMC4782998
OpenAlexW2295722228

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.