Evidence map›Paper›PMID 24471466›Full record

ArticleJournal of medicinal chemistry2014

Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis.

Lillian Onwuha-Ekpete, Lisa Tack, Anna Knapinska, Lyndsay Smith, Gaurav Kaushik, Travis Lavoi, Marc Giulianotti, Richard A Houghten, Gregg B Fields, Dmitriy Minond

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.3field-weighted citation impact, top 37% 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

6 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. Cell Death Modalities in Therapy of Melanoma.International journal of molecular sciences · 2025
    Review
  3. Review
  4. Article
  5. Article
  6. A Novel Probe for Spliceosomal Proteins that Induces Autophagy and Death of Melanoma Cells Reveals New Targets for Melanoma Drug Discovery.Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology · 2019
    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

10 authors at 2 institutions in 1 country.

Lillian Onwuha-EkpeteTorrey Pines Institute for Molecular Studies , 11350 South West Village Parkway, Port St. Lucie, Florida 34987, United States.
Lisa Tack
Anna Knapinska
Lyndsay Smith
Gaurav Kaushik
Travis Lavoi
Marc Giulianotti
Richard A Houghten
Gregg B Fields
Dmitriy Minond
Torrey Pines Institute For Molecular Studies · USUniversity of Kansas Medical Center · US

Funding

Mechanism &Inhibition of Collagenolytic ActivityR01CA098799 · NCI · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI FIELDS, GREGG B · 2003 to 2017
$4.5M
High throughput in vivo screening: translational generation of novel analgesicsR01DA031370 · NIDA · TORREY PINES INST FOR MOLECULAR STUDIES · PI HOUGHTEN, RICHARD ALLEN · 2011 to 2015
$2.2M
HTS Assays to Discover Selective Inhibitors of ADAM10 and 17R03DA033985 · NIDA · TORREY PINES INST FOR MOLECULAR STUDIES · PI MINOND, DMITRIY · 2012 to 2013
$90k
NCI NIH HHS CA098799NCI NIH HHS R01 CA098799NIDA NIH HHS DA031370NIDA NIH HHS DA033985NIDA NIH HHS R01 DA031370NIDA NIH HHS R03 DA033985
6 · The paper itself

Abstract

A common liability of cancer drugs is toxicity to noncancerous cells. Thus, molecules are needed that are potent toward cancer cells while sparing healthy cells. The cost of traditional cell-based HTS is dictated by the library size, which is typically in the hundreds of thousands of individual compounds. Mixture-based combinatorial libraries offer a cost-effective alternative to single-compound libraries while eliminating the need for molecular target validation. Presently, lung cancer and melanoma cells were screened in parallel with healthy cells using a mixture-based library. A novel class of compounds was discovered that selectively inhibited melanoma cell growth via apoptosis with submicromolar potency while sparing healthy cells. Additionally, the cost of screening and biological follow-up experiments was significantly lower than in typical HTS. Our findings suggest that mixture-based phenotypic HTS can significantly reduce cost and hit-to-lead time while yielding novel compounds with promising pharmacology.

Indexed as

ApoptosisAnimalsMelanoma, ExperimentalMicePiperazinesPyrrolidinesPiperazinesPyrrolidines

Identifiers

PMID24471466
PMCPMC3983399
OpenAlexW2315955486

What OpenQuestion holds

Textmetadata
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.