Evidence map›Paper›PMID 26384289›Full record

ArticleBioorganic & medicinal chemistry letters2015

Lipid-conjugated Smac analogues.

Ewa D Micewicz, Josephine A Ratikan, Alan J Waring, Julian P Whitelegge, William H McBride, Piotr Ruchala

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Position of lipidation influences anticancer activity of Smac analogs.Bioorganic & medicinal chemistry letters · 2019
    Article
  2. Palladium-Mediated Arylation of Lysine in Unprotected Peptides.Angewandte Chemie (International ed. in English) · 2017
    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

6 authors.

Ewa D MicewiczDepartment of Radiation Oncology, University of California at Los Angeles, 10833 Le Conte Avenue, Los Angeles, CA 90095, USA.
Josephine A RatikanDepartment of Radiation Oncology, University of California at Los Angeles, 10833 Le Conte Avenue, Los Angeles, CA 90095, USA.
Alan J WaringDepartment of Medicine, Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center, 1000 West Carson Street, Torrance, CA 90502, USA; Department of Physiology and Biophysics, University of California Irvine, 1001 Health Sciences Road, Irvine, CA 92697, USA.
Julian P WhiteleggeDepartment of Psychiatry and Biobehavioral Sciences, University of California at Los Angeles, 760 Westwood Plaza, Los Angeles, CA 90024, USA; The Pasarow Mass Spectrometry Laboratory, The Jane and Terry Semel Institute for Neuroscience and Human Behavior, 760 Westwood Plaza, Los Angeles, CA 90024, USA.
William H McBrideDepartment of Radiation Oncology, University of California at Los Angeles, 10833 Le Conte Avenue, Los Angeles, CA 90095, USA.
Piotr RuchalaDepartment of Psychiatry and Biobehavioral Sciences, University of California at Los Angeles, 760 Westwood Plaza, Los Angeles, CA 90024, USA; The Pasarow Mass Spectrometry Laboratory, The Jane and Terry Semel Institute for Neuroscience and Human Behavior, 760 Westwood Plaza, Los Angeles, CA 90024, USA. Electronic address: pruchala@mednet.ucla.edu.

Funding

UCLA Center for Biological RadioprotectorsU19AI067769 · NIAID · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI CHUTE, JOHN P, MCBRIDE, WILLIAM H. · 2005 to 2019
$44.6M
Transgenic & Knock-out MouseP30DK063491 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI Andrea L Hevener · 2003 to 2026
$40.4M
NIAID NIH HHS 5U19AI067769NIAID NIH HHS U19 AI067769NIDDK NIH HHS 5P30DK063491NIDDK NIH HHS P30 DK063491
6 · The paper itself

Abstract

A small library of monovalent and bivalent Smac mimics was synthesized based on 2 types of monomers, with general structure NMeAla-Xaa-Pro-BHA (Xaa=Cys or Lys). Position 2 of the compounds was utilized to dimerize both types of monomers employing various bis-reactive linkers, as well as to modify selected compounds with lipids. The resulting library was screened in vitro against metastatic human breast cancer cell line MDA-MB-231, and the two most active compounds selected for in vivo studies. The most active lipid-conjugated analogue M11, showed in vivo activity while administered both subcutaneously and orally. Collectively, our findings suggest that lipidation may be a viable approach in the development of new Smac-based therapeutic leads.

Indexed as

AnimalsAntineoplastic AgentsApoptosis Regulatory ProteinsCell Line, TumorCell SurvivalDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansIntracellular Signaling Peptides and ProteinsLipidsMiceMitochondrial ProteinsMolecular StructureNeoplasms, ExperimentalStructure-Activity RelationshipAntineoplastic AgentsApoptosis Regulatory ProteinsDIABLO protein, humanIntracellular Signaling Peptides and ProteinsLipidsMitochondrial ProteinsAnticancer agentsApoptosisLipids-conjugated peptidesS-Alkylation of peptidesSmac mimics

Identifiers

PMID26384289
PMCPMC4592835

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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.