Evidence map›Paper›PMID 30380297›Full record

ArticleBiochemistry2018

Identification of Inhibitors of the dNTP Triphosphohydrolase SAMHD1 Using a Novel and Direct High-Throughput Assay.

Christopher H Mauney, Fred W Perrino, Thomas Hollis

Abstract read
In one paragraph

Article in Biochemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
0.7field-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

11 citing papers in PubMed, 16 citations in OpenAlex.

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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

3 authors at 1 institution in 1 country.

Christopher H MauneyCenter for Structural Biology, Department of Biochemistry , Wake Forest School of Medicine , Winston-Salem , North Carolina 27157 , United States.
Fred W PerrinoCenter for Structural Biology, Department of Biochemistry , Wake Forest School of Medicine , Winston-Salem , North Carolina 27157 , United States.
Thomas HollisCenter for Structural Biology, Department of Biochemistry , Wake Forest School of Medicine , Winston-Salem , North Carolina 27157 , United States.ORCID 0000-0002-4996-6346
Wake Forest University · US

Funding

Structural and Computational Biophysics Training ProgramT32GM095440 · NIGMS · WAKE FOREST UNIVERSITY HEALTH SCIENCES · PI HOLLIS, THOMAS J, LYLES, DOUGLAS S. · 2011 to 2020
$1.7M
Cellular Nucleotide Metabolism in HIV RestrictionR01GM110734 · NIGMS · WAKE FOREST UNIVERSITY HEALTH SCIENCES · PI PERRINO, FRED W · 2014 to 2017
$1.5M
Structure and Regulation of the TREX1 ExonucleaseR01GM108827 · NIGMS · WAKE FOREST UNIVERSITY HEALTH SCIENCES · PI HOLLIS, THOMAS J · 2014 to 2017
$1.1M
NIGMS NIH HHS R01 GM108827NIGMS NIH HHS R01 GM110734NIGMS NIH HHS T32 GM095440
6 · The paper itself

Abstract

The dNTP triphosphohydrolase SAMHD1 is a regulator of cellular dNTP pools. Given its central role in nucleotide metabolism, SAMHD1 performs important functions in cellular homeostasis, cell cycle regulation, and innate immunity. It therefore represents a high-profile target for small molecule drug design. SAMHD1 has a complex mechanism of catalytic activation that makes the design of an activating compound challenging. However, an inhibitor of SAMHD1 could serve multiple therapeutic roles, including the potentiation of antiviral and anticancer drug regimens. The lack of high-throughput screens that directly measure SAMHD1 catalytic activity has impeded efforts to identify inhibitors of SAMHD1. Here we describe a novel high-throughput screen that directly measures SAMHD1 catalytic activity. This assay results in a colorimetric end point that can be read spectrophotometrically and utilizes bis(4-nitrophenyl) phosphate as the substrate and Mn

Indexed as

Drug DiscoveryEnzyme InhibitorsHigh-Throughput Screening AssaysHumansManganeseNitrophenolsProtein MultimerizationSAM Domain and HD Domain-Containing Protein 1bis(4-nitrophenyl)phosphateEnzyme InhibitorsManganeseNitrophenolsSAM Domain and HD Domain-Containing Protein 1SAMHD1 protein, human

Identifiers

PMID30380297
PMCPMC6322912
OpenAlexW2898720030

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.