Evidence map›Paper›PMID 29476592›Full record

ArticleChemMedChem2018

Chemical Features Important for Activity in a Class of Inhibitors Targeting the Wip1 Flap Subdomain.

Harichandra D Tagad, Subrata Debnath, Victor Clausse, Mrinmoy Saha, Sharlyn J Mazur, Ettore Appella, Daniel H Appella

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.5field-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

7 citing papers in PubMed, 10 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

7 authors at 1 institution in 1 country.

Harichandra D TagadLaboratory of Cell Biology, National Cancer Institute, US National Institutes of Health, Bethesda, MD, 20892, USA.
Subrata DebnathLaboratory of Cell Biology, National Cancer Institute, US National Institutes of Health, Bethesda, MD, 20892, USA.
Victor ClausseSynthetic Bioactive Molecules Section, LBC, NIDDK, US National Institutes of Health, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.
Mrinmoy SahaSynthetic Bioactive Molecules Section, LBC, NIDDK, US National Institutes of Health, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.
Sharlyn J MazurLaboratory of Cell Biology, National Cancer Institute, US National Institutes of Health, Bethesda, MD, 20892, USA.
Ettore AppellaLaboratory of Cell Biology, National Cancer Institute, US National Institutes of Health, Bethesda, MD, 20892, USA.
Daniel H AppellaSynthetic Bioactive Molecules Section, LBC, NIDDK, US National Institutes of Health, 8 Center Drive, Room 404, Bethesda, MD, 20892, USA.ORCID 0000-0001-7195-7764
National Institutes of Health · US

Funding

Chemically Modified Peptide Nucleic AcidsZIADK031143 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI APPELLA, DANIEL H · 2009 to 2025
$13.9M
Regulation and Function of WIP1 Phosphatase and its Role in Tumor CellsZIABC011197 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI APPELLA, ETTORE · 2009 to 2025
$11.5M
Small Molecular Inactivators of HIVZIADK075135 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI APPELLA, DANIEL H · 2016 to 2025
$7.2M
Chemically Modified Peptide Nucleic AcidsZ01DK031143 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI APPELLA, DANIEL H · 2005 to 2008
$892k
Intramural NIH HHS Z01 DK031143Intramural NIH HHS ZIA BC011197
6 · The paper itself

Abstract

The wild-type p53 induced phosphatase 1, Wip1 (PP2Cδ), is a protein phosphatase 2C (PP2C) family serine/threonine phosphatase that negatively regulates the function of the tumor suppressor p53 and several of its positive regulators such as ATM, Chk1, Chk2, Mdm2, and p38 MAPK. Wip1 dephosphorylates and inactivates its protein targets, which are critical for cellular stress responses. Additionally, Wip1 is frequently amplified and overexpressed in several human cancer types. Because of its negative role in regulating the function of tumor suppressor proteins, Wip1 has been identified as a potential therapeutic target in various types of cancers. Based on a recently reported Wip1 inhibitor (G-1), we performed an extensive structure-activity relationship (SAR) analysis. This led us to interesting findings in SAR trends and to the discovery of new chemical analogues with good specificity and bioavailability.

Indexed as

Dose-Response Relationship, DrugEnzyme InhibitorsHumansMCF-7 CellsProtein Phosphatase 2CStructure-Activity RelationshipTumor Cells, CulturedEnzyme InhibitorsPPM1D protein, humanProtein Phosphatase 2CELISAenzyme kineticsinhibitorsWip1

Identifiers

PMID29476592
PMCPMC8022280
OpenAlexW2791471728

What OpenQuestion holds

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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.