Evidence map›Paper›PMID 29517836›Full record

ArticleChembiochem : a European journal of chemical biology2018

Deletion of the C26 Methyl Substituent from the Bryostatin Analogue Merle 23 Has Negligible Impact on Its Biological Profile and Potency.

Xiguang Zhao, Noemi Kedei, Alexandra Michalowski, Nancy E Lewin, Gary E Keck, Peter M Blumberg

Open access · greenAbstract read
In one paragraph

Article in Chembiochem : a European journal of chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.5field-weighted citation impact, top 44% 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

1 citing paper in PubMed, 4 citations in OpenAlex.

  1. 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 at 2 institutions in 1 country.

Xiguang ZhaoDepartment of Chemistry, University of Utah, 315 South 1400 East, RM 2020, Salt Lake City, Utah, 84112, USA.
Noemi KedeiLaboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, Building 37, Room 4048, 37 Convent Drive MSC4255, Bethesda, MD, 20892-4255, USA.ORCID 0000-0002-6625-6119
Alexandra MichalowskiLaboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, Building 37, Room 4048, 37 Convent Drive MSC4255, Bethesda, MD, 20892-4255, USA.
Nancy E LewinLaboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, Building 37, Room 4048, 37 Convent Drive MSC4255, Bethesda, MD, 20892-4255, USA.
Gary E KeckDepartment of Chemistry, University of Utah, 315 South 1400 East, RM 2020, Salt Lake City, Utah, 84112, USA.
Peter M BlumbergLaboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, Building 37, Room 4048, 37 Convent Drive MSC4255, Bethesda, MD, 20892-4255, USA.
National Cancer Institute · USUniversity of Utah · US

Funding

Molecular Mechanism of Action of Phorbol EsterZIABC005270 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BLUMBERG, PETER · 2009 to 2018
$18.4M
CHIRAL APPROACHES TO NATURAL PRODUCT SYNTHESISR01GM028961 · NIGMS · UNIVERSITY OF UTAH · PI KECK, GARY E · 1985 to 2014
$5.5M
MOLECULAR MECHANISM OF ACTION OF PHORBOL ESTER TUMOR PROMOTERSZ01BC005270 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BLUMBERG, PETER · 1996 to 2008
$4.3M
Intramural NIH HHS Z01 BC005270NIGMS NIH HHS R01 GM028961
6 · The paper itself

Abstract

Important strides are being made in understanding the effects of structural features of bryostatin 1, a candidate therapeutic agent for cancer and dementia, in conferring its potency toward protein kinase C and the unique spectrum of biological responses that it induces. A critical pharmacophoric element in bryostatin 1 is the secondary hydroxy group at the C26 position, with a corresponding primary hydroxy group playing an analogous role in binding of phorbol esters to protein kinase C. Herein, we describe the synthesis of a bryostatin homologue in which the C26 hydroxy group is primary, as it is in the phorbol esters, and show that its biological activity is almost indistinguishable from that of the corresponding compound with a secondary hydroxy group.

Indexed as

Drug DesignAnimalsBryostatinsCell Line, TumorHumansMethylationMiceProtein Kinase CProtein Kinase InhibitorsStructure-Activity RelationshipBryostatinsMerle 23Protein Kinase CProtein Kinase Inhibitorsdrug designnatural productsprotein kinase Csignal transductionstructure-activity relationships

Identifiers

PMID29517836
PMCPMC7032040
OpenAlexW2791463469

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.