Evidence map›Paper›PMID 24953177›Full record

ArticleNeoplasia (New York, N.Y.)2014

A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas.

Jason M Foulks, Kent J Carpenter, Bai Luo, Yong Xu, Anna Senina, Rebecca Nix, Ashley Chan, Adrianne Clifford, Marcus Wilkes, David Vollmer and 15 more

Open access · goldAbstract read
In one paragraph

Article in Neoplasia (New York, N.Y.), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.

0numbers the graph read from it
0cells of the map it votes in
36citing papers in PubMed
5.1field-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

36 citing papers in PubMed, 91 citations in OpenAlex.

  1. Review
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  8. PIM1 kinase and its diverse substrate in solid tumors.Cell communication and signaling : CCS · 2024
    Review
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  10. Review
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  12. Review
  13. Pim-1 kinase is a positive feedback regulator of the senescent lung fibroblast inflammatory secretome.American journal of physiology. Lung cellular and molecular physiology · 2022
    Article
  14. Review
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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

25 authors at 4 institutions in 1 country.

Jason M FoulksAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Kent J CarpenterTolero Pharmaceuticals, Inc, Lehi, UT.
Bai LuoAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Yong XuAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Anna SeninaAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Rebecca NixAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Ashley ChanAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Adrianne CliffordAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Marcus WilkesAstex Pharmaceuticals, Inc, Salt Lake City, UT.
David VollmerAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Benjamin BrenningAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Shannon MerxAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Shuping LaiAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Michael V McCullarAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Koc-Kan HoAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Daniel J AlbertsonDepartment of Pathology, University of Utah School of Medicine, Salt Lake City, UT.
Lee T CallTolero Pharmaceuticals, Inc, Lehi, UT.
Jared J BearssHuntsman Cancer Institute, University of Utah, Salt Lake City, UT.
Sheryl TrippARUP Laboratories, Salt Lake City, UT.
Ting LiuDepartment of Pathology, University of Utah School of Medicine, Salt Lake City, UT.
Bret J StephensTolero Pharmaceuticals, Inc, Lehi, UT.
Alexis MollardTolero Pharmaceuticals, Inc, Lehi, UT.
Steven L WarnerTolero Pharmaceuticals, Inc, Lehi, UT.
David J BearssTolero Pharmaceuticals, Inc, Lehi, UT. Electronic address: dbearss@toleropharma.com.
Steven B KannerAstex Pharmaceuticals, Inc, Salt Lake City, UT.
Arrien Pharmaceuticals (United States) · USTolero Pharmaceuticals (United States) · USUniversity of Utah · USARUP Laboratories (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The proto-oncogene proviral integration site for moloney murine leukemia virus (PIM) kinases (PIM-1, PIM-2, and PIM-3) are serine/threonine kinases that are involved in a number of signaling pathways important to cancer cells. PIM kinases act in downstream effector functions as inhibitors of apoptosis and as positive regulators of G1-S phase progression through the cell cycle. PIM kinases are upregulated in multiple cancer indications, including lymphoma, leukemia, multiple myeloma, and prostate, gastric, and head and neck cancers. Overexpression of one or more PIM family members in patient tumors frequently correlates with poor prognosis. The aim of this investigation was to evaluate PIM expression in low- and high-grade urothelial carcinoma and to assess the role PIM function in disease progression and their potential to serve as molecular targets for therapy. One hundred thirty-seven cases of urothelial carcinoma were included in this study of surgical biopsy and resection specimens. High levels of expression of all three PIM family members were observed in both noninvasive and invasive urothelial carcinomas. The second-generation PIM inhibitor, TP-3654, displays submicromolar activity in pharmacodynamic biomarker modulation, cell proliferation studies, and colony formation assays using the UM-UC-3 bladder cancer cell line. TP-3654 displays favorable human ether-à-go-go-related gene and cytochrome P450 inhibition profiles compared with the first-generation PIM inhibitor, SGI-1776, and exhibits oral bioavailability. In vivo xenograft studies using a bladder cancer cell line show that PIM kinase inhibition can reduce tumor growth, suggesting that PIM kinase inhibitors may be active in human urothelial carcinomas.

Indexed as

AnimalsAntineoplastic AgentsBlotting, WesternCarcinoma, Transitional CellFemaleHumansImidazolesMaleMiceMice, NudeMultiplex Polymerase Chain ReactionOligopeptidesProtein Kinase InhibitorsProto-Oncogene MasProto-Oncogene Proteins c-pim-1PyridazinesAntineoplastic AgentsImidazolesMAS1 protein, humanOligopeptidesProtein Kinase InhibitorsProto-Oncogene MasProto-Oncogene Proteins c-pim-1proto-oncogene proteins pimPyridazinesRNA, Small InterferingSGI 1776TP 3654Vasoactive Intestinal Peptide

Identifiers

PMID24953177
PMCPMC4198696
OpenAlexW2111803606

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.