Evidence map›Paper›PMID 23311288›Full record

ArticleJournal of medicinal chemistry2013

Hypoxia-selective O6-alkylguanine-DNA alkyltransferase inhibitors: design, synthesis, and evaluation of 6-(benzyloxy)-2-(aryldiazenyl)-9H-purines as prodrugs of O6-benzylguanine.

Rui Zhu, Raymond P Baumann, Philip G Penketh, Krishnamurthy Shyam, Alan C Sartorelli

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
0.6field-weighted citation impact, top 32% 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

10 citing papers in PubMed, 26 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Article
  6. Hypoxia-targeted drug delivery.Chemical Society reviews · 2019
    Review
  7. Hypoxia-activated prodrugs and redox-responsive nanocarriers.International journal of nanomedicine · 2018
    Review
  8. Article
  9. Review
  10. 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

5 authors at 1 institution in 1 country.

Rui ZhuDepartment of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, Connecticut 06520, USA.
Raymond P Baumann
Philip G Penketh
Krishnamurthy Shyam
Alan C Sartorelli
Yale University · US

Funding

TUMOR SELECTIVE INACTIVATION OF THE REPAIR PROTEIN AGTP01CA129186 · NCI · YALE UNIVERSITY · PI GLAZER, PETER M · 2007 to 2012
$8.5M
DEVELOPMENT OF ANTICANCER 1, 2-BIS(SULFONYL) HYDRAZINESR01CA090671 · NCI · YALE UNIVERSITY · PI SARTORELLI, ALAN CLAYTON · 2002 to 2009
$2.5M
Hypoxia-Activated O6-Benzylguanine ProdrugsR01CA122112 · NCI · YALE UNIVERSITY · PI SARTORELLI, ALAN CLAYTON · 2006 to 2012
$1.7M
Cancer Research UK 16466NCI NIH HHS CA090671NCI NIH HHS CA122112NCI NIH HHS CA129186NCI NIH HHS P01 CA129186NCI NIH HHS R01 CA090671NCI NIH HHS R01 CA122112
6 · The paper itself

Abstract

O(6)-Alkylguanine-DNA alkyltransferase (AGT) is a DNA repair protein which removes alkyl groups from the O-6 position of guanine, thereby providing strong resistance to anticancer agents which alkylate this position. The clinical usefulness of these anticancer agents would be substantially augmented if AGT could be selectively inhibited in tumor tissue, without a corresponding depletion in normal tissue. We report the synthesis of a new AGT inhibitor (5c) which selectively depletes AGT in hypoxic tumor cells.

Indexed as

Cell Line, TumorDrug DesignEnzyme InhibitorsGuanineHumansMagnetic Resonance SpectroscopyO(6)-Methylguanine-DNA MethyltransferaseOxidation-ReductionProdrugsEnzyme InhibitorsGuanineO(6)-benzylguanineO(6)-Methylguanine-DNA MethyltransferaseProdrugs

Identifiers

PMID23311288
PMCPMC3722860
OpenAlexW2008681329

What OpenQuestion holds

Textmetadata
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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.