Evidence map›Paper›PMID 28841379›Full record

ArticleJournal of medicinal chemistry2017

New Mandelalides Expand a Macrolide Series of Mitochondrial Inhibitors.

Mohamad Nazari, Jeffrey D Serrill, Xuemei Wan, Minh H Nguyen, Clemens Anklin, David A Gallegos, Amos B Smith, Jane E Ishmael, Kerry L McPhail

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing 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

15 citing papers in PubMed.

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  7. Natural products and other inhibitors of FEuropean journal of medicinal chemistry · 2020
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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

9 authors.

Mohamad NazariDepartment of Pharmaceutical Sciences, College of Pharmacy, Oregon State University , Corvallis, Oregon 97331, United States.
Jeffrey D SerrillDepartment of Pharmaceutical Sciences, College of Pharmacy, Oregon State University , Corvallis, Oregon 97331, United States.
Xuemei WanDepartment of Pharmaceutical Sciences, College of Pharmacy, Oregon State University , Corvallis, Oregon 97331, United States.
Minh H NguyenDepartment of Chemistry, University of Pennsylvania , Philadelphia, Pennsylvania 19104-6323, United States.ORCID 0000-0003-3280-5375
Clemens AnklinBruker BioSpin , 15 Fortune Drive, Billerica, Massachusetts 01821, United States.
David A GallegosDepartment of Pharmaceutical Sciences, College of Pharmacy, Oregon State University , Corvallis, Oregon 97331, United States.ORCID 0000-0002-5552-8107
Amos B SmithDepartment of Chemistry, University of Pennsylvania , Philadelphia, Pennsylvania 19104-6323, United States.ORCID 0000-0002-1712-8567
Jane E IshmaelDepartment of Pharmaceutical Sciences, College of Pharmacy, Oregon State University , Corvallis, Oregon 97331, United States.
Kerry L McPhailDepartment of Pharmaceutical Sciences, College of Pharmacy, Oregon State University , Corvallis, Oregon 97331, United States.ORCID 0000-0003-2076-1002

Funding

SYNTHESIS OF PHYLLANTHOSIDE RELATED ANTITUMOR AGENTSR01CA019033 · NCI · UNIVERSITY OF PENNSYLVANIA · PI SMITH, AMOS B · 1985 to 2024
$5.9M
Natural Product Drug Discovery from South African Tunicates by Leveraging International Training OpportunitiesR15GM122016 · NIGMS · OREGON STATE UNIVERSITY · PI MCPHAIL, KERRY LEIGH · 2017 to 2017
$405k
NCI NIH HHS R01 CA019033NIGMS NIH HHS R15 GM122016
6 · The paper itself

Abstract

Mandelalides A-D (1-4) are macrocyclic polyketides known to have an unusual bioactivity profile influenced by compound glycosylation and growth phase of cultured cells. The isolation and characterization of additional natural congeners, mandelalides E-L (5-12), and the supply of synthetic compounds 1 and 12, as well as seco-mandelalide A methyl ester (13), have now facilitated mechanism of action and structure-activity relationship studies. Glycosylated mandelalides are effective inhibitors of aerobic respiration in living cells. Macrolides 1 and 2 inhibit mitochondrial function similar to oligomycin A and apoptolidin A, selective inhibitors of the mammalian ATP synthase (complex V). 1 inhibits ATP synthase activity from isolated mitochondria and triggers caspase-dependent apoptosis in HeLa cells, which are more sensitive to inhibition by 1 in the presence of the glycolysis inhibitor 2-deoxyglucose. Thus, mandelalide cytotoxicity depends on basal metabolic phenotype; cells with an oxidative phenotype are most likely to be inhibited by the mandelalides.

Indexed as

ApoptosisCell SurvivalGlycosylationHEK293 CellsHeLa CellsHumansMacrolidesMitochondriaMitochondrial Proton-Translocating ATPasesMacrolidesmandelalide Amandelalide EMitochondrial Proton-Translocating ATPases

Identifiers

PMID28841379
PMCPMC5702619

What OpenQuestion holds

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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.