Evidence map›Paper›PMID 19681093›Full record

ArticleChemMedChem2009

Structure-Based Design, Synthesis, and Evaluation of 2'-(2-Hydroxyethyl)-2'-deoxyadenosine and the 5'-Diphosphate Derivative as Ribonucleotide Reductase Inhibitors.

Dianqing Sun, Hai Xu, Sanath R Wijerathna, Chris Dealwis, Richard E Lee

Abstract read
In one paragraph

Article in ChemMedChem, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed, 5 citations in OpenAlex.

  1. Review
  2. The structural basis for the allosteric regulation of ribonucleotide reductase.Progress in molecular biology and translational science · 2013
    Review
  3. 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 2 institutions in 1 country.

Dianqing SunDepartment of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163 (USA).
Hai Xu
Sanath R Wijerathna
Chris Dealwis
Richard E Lee
Case Western Reserve University · USUniversity of Tennessee Health Science Center · US

Funding

Structure of enzymes in Multi-Drug Resistant Tuberculosis (MDR-TB)P01AI057836 · NIAID · COLORADO STATE UNIVERSITY-FORT COLLINS · PI MCNEIL, MICHAEL R · 2004 to 2008
$4.5M
Structure-Function and Inhibition of Rnr1R01CA100827 · NCI · UNIVERSITY OF TENNESSEE KNOXVILLE · PI DEALWIS, CHRIS G · 2003 to 2011
$2.5M
NCI NIH HHS R01 CA100827NIAID NIH HHS AI057836PHS HHS R01A10087
6 · The paper itself

Abstract

Analysis of the recently solved X-ray crystal structures of Saccharomyces cerevisiae ribonucleotide reductase I (ScRnr1) in complex with effectors and substrates led to the discovery of a conserved water molecule located at the active site that interacted with the 2'-hydroxy group of the nucleoside ribose. In this study 2'-(2-hydroxyethyl)-2'-deoxyadenosine 1 and the 5'-diphosphate derivative 2 were designed and synthesized to see if the conserved water molecule could be displaced by a hydroxymethylene group, to generate novel RNR inhibitors as potential antitumor agents. Herein we report the synthesis of analogues 1 and 2, and the co-crystal structure of adenosine diphosphate analogue 2 bound to ScRnr1, which shows the conserved water molecule is displaced as hypothesized.

Indexed as

Adenosine TriphosphateCrystallography, X-RayDeoxyadenosinesDrug DesignEnzyme InhibitorsRibonucleotide ReductasesSaccharomyces cerevisiae2'-(2-hydroxyethyl)-2'-deoxyadenosine2'-(2-hydroxyethyl)-2'-deoxyadenosine 5'-phosphateAdenosine TriphosphateDeoxyadenosinesEnzyme InhibitorsRibonucleotide Reductases

Identifiers

PMID19681093
PMCPMC3080699
OpenAlexW2021512177

What OpenQuestion holds

Textmetadata
LicenceTDM
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.