Evidence map›Paper›PMID 26504023›Full record

ArticleAnticancer research2015

Antitumor Activity of 3-Indolylmethanamines 31B and PS121912.

Margaret L Guthrie, Preetpal S Sidhu, Emily K Hill, Timothy C Horan, Premchendar Nandhikonda, Kelly A Teske, Nina Y Yuan, Marina Sidorko, Revathi Rodali, James M Cook and 6 more

Abstract read
In one paragraph

Article in Anticancer research, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
  4. 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.

Margaret L GuthrieDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Preetpal S SidhuDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Emily K HillMolecular Therapeutics Laboratory, Program in Women's Oncology, Women and Infants' Hospital of Rhode Island, Alpert Medical School, Brown University, Providence, RI, U.S.A.
Timothy C HoranMolecular Therapeutics Laboratory, Program in Women's Oncology, Women and Infants' Hospital of Rhode Island, Alpert Medical School, Brown University, Providence, RI, U.S.A.
Premchendar NandhikondaDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Kelly A TeskeDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Nina Y YuanDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Marina SidorkoDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Revathi RodaliDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
James M CookDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Lanlan HanDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Nicholas R SilvaggiDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.
Daniel D BikleEndocrine Research Unit, Department of Medicine, Veterans Affairs Medical Center, San Francisco, CA, U.S.A.
Richard G MooreMolecular Therapeutics Laboratory, Program in Women's Oncology, Women and Infants' Hospital of Rhode Island, Alpert Medical School, Brown University, Providence, RI, U.S.A.
Rakesh K SinghMolecular Therapeutics Laboratory, Program in Women's Oncology, Women and Infants' Hospital of Rhode Island, Alpert Medical School, Brown University, Providence, RI, U.S.A.
Leggy A ArnoldDepartment of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A. arnold2@uwm.edu.

Funding

Vitamin D Receptor Coactivators in KeratinocytesR01AR050023 · NIAMS · NORTHERN CALIFORNIA INSTITUTE RES &EDUC · PI BIKLE, DANIEL DAVID · 2004 to 2014
$3.4M
Development of new drugs for asthma by targeting GABA(A) receptors in the lungR01HL118561 · NHLBI · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2014 to 2017
$2.0M
Design of New Therapeutic Agents to Treat SchizophreniaR01MH096463 · NIMH · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2013 to 2017
$1.9M
Synthesis of Alpha2/Alpha3 GABA Agonists to Treat Neuropathic PainR01NS076517 · NINDS · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2012 to 2015
$1.3M
Small molecule inhibitors of the vitamin D receptor-coactivator interactionR03DA031090 · NIDA · UNIVERSITY OF WISCONSIN MILWAUKEE · PI ARNOLD, ALEXANDER · 2010 to 2011
$73k
NHLBI NIH HHS R01 HL118561NIAMS NIH HHS R01 AR050023NIDA NIH HHS R03 DA031090NIMH NIH HHS R01 MH096463NINDS NIH HHS R01 NS076517
6 · The paper itself

Abstract

aimTo investigate the in vivo effects of 3-indolylmethanamines 31B and PS121912 in treating ovarian cancer and leukemia, respectively. MATERIALS AND

methodsTerminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and western blotting were applied to demonstrate the induction of apoptosis. Xenografted mice were investigated to show the antitumor effects of 3-indolylmethanamines. (13)C-Nuclear magnetic resource (NMR) and western blotting were used to demonstrate inhibition of glucose metabolism.

results31B inhibited ovarian cancer cell proliferation and activated caspase-3, cleaved poly (ADP-ribose) polymerase 1 (PARP1), and phosphorylated mitogen-activated protein kinases (MAPK), JUN N-terminal kinase/stress-activated protein kinase (JNK/SAPK) and p38. 31B reduced ovarian cancer xenograft tumor growth and PS121912 inhibited the growth of HL-60-derived xenografts without any sign of toxicity. Compound 31B inhibited de novo glycolysis and lipogenesis mediated by the reduction of fatty acid synthase and lactate dehydrogenase-A expression.

conclusion3-Indolylmethanamines represent a new class of antitumor agents. We have shown for the first time the in vivo anticancer effects of 3-indolylmethanamines 31B and PS121912.

Indexed as

AminesAniline CompoundsAnimalsAntineoplastic AgentsApoptosisBlotting, WesternCell ProliferationFemaleFlow CytometryHumansHydrocarbons, AromaticIndolesMagnetic Resonance SpectroscopyMiceMice, NudeOvarian Neoplasms4-chloro-N-((2-chlorophenyl)(2-methyl-1H-indol-3-yl)methyl)anilineAminesAniline CompoundsAntineoplastic AgentsHydrocarbons, AromaticIndolesPS1219123-Indolylmethanamineleukemiaovarian cancer

Identifiers

PMID26504023
PMCPMC4633305

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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.