Evidence map›Paper›PMID 29100797›Full record

ArticleBioorganic & medicinal chemistry letters2017

Structure-activity relationships of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as novel antagonists of exchange proteins directly activated by cAMP (EPACs).

Zhiqing Liu, Yingmin Zhu, Haiying Chen, Pingyuan Wang, Fang C Mei, Na Ye, Xiaodong Cheng, Jia Zhou

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. 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 30% 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, 12 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

8 authors at 3 institutions in 1 country.

Zhiqing LiuChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, 301 University Blvd, Galveston, TX 77555, United States.
Yingmin ZhuDepartment of Integrative Biology and Pharmacology, Texas Therapeutics Institute, The University of Texas Health Science Center, 7000 Fannin St #1200, Houston, TX 77030, United States.
Haiying ChenChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, 301 University Blvd, Galveston, TX 77555, United States.
Pingyuan WangChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, 301 University Blvd, Galveston, TX 77555, United States.
Fang C MeiDepartment of Integrative Biology and Pharmacology, Texas Therapeutics Institute, The University of Texas Health Science Center, 7000 Fannin St #1200, Houston, TX 77030, United States.
Na YeChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, 301 University Blvd, Galveston, TX 77555, United States.
Xiaodong ChengDepartment of Integrative Biology and Pharmacology, Texas Therapeutics Institute, The University of Texas Health Science Center, 7000 Fannin St #1200, Houston, TX 77030, United States. Electronic address: xiaodong.cheng@uth.tmc.edu.
Jia ZhouChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, 301 University Blvd, Galveston, TX 77555, United States. Electronic address: jizhou@utmb.edu.
The University of Texas Medical Branch at Galveston · USThe University of Texas Health Science Center at Houston · USThe University of Texas Health Science Center · US

Funding

Preclinical Development of Novel Rickettsiosis Therapeutics Targeting EPAC1R01AI111464 · NIAID · UNIVERSITY OF TEXAS HLTH SCI CTR HOUSTON · PI CHENG, XIAODONG, WALKER, DAVID H · 2014 to 2018
$6.5M
Epac/cAMP-GEF, A Novel Intracellular cAMP ReceptorR01GM066170 · NIGMS · UNIVERSITY OF TEXAS MEDICAL BR GALVESTON · PI CHENG, XIAODONG · 2003 to 2017
$4.6M
Exchange Protein directly Activated by cAMP (EPAC): Structure, Function and TherapeuticsR35GM122536 · NIGMS · UNIVERSITY OF TEXAS HLTH SCI CTR HOUSTON · PI CHENG, XIAODONG · 2017 to 2021
$1.9M
Novel Pharmacological Probes Targeting Exchange Proteins Activated by cAMP (EPAC)R01GM106218 · NIGMS · UNIVERSITY OF TEXAS MED BR GALVESTON · PI CHENG, XIAODONG, ZHOU, JIA · 2013 to 2015
$1.1M
NIAID NIH HHS R01 AI111464NIGMS NIH HHS R01 GM066170NIGMS NIH HHS R01 GM106218NIGMS NIH HHS R35 GM122536
6 · The paper itself

Abstract

Exchange proteins directly activated by cAMP (EPACs) are critical cAMP-dependent signaling pathway mediators that play important roles in cancer, diabetes, heart failure, inflammations, infections, neurological disorders and other human diseases. EPAC specific modulators are urgently needed to explore EPAC's physiological function, mechanism of action and therapeutic applications. On the basis of a previously identified EPAC specific inhibitor hit ESI-09, herein we have designed and synthesized a novel series of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as potent EPAC inhibitors. Compound 31 (ZL0524) has been discovered as the most potent EPAC inhibitor with IC

Indexed as

Binding SitesCyanidesCyclic AMPGuanine Nucleotide Exchange FactorsHumansInhibitory Concentration 50Molecular Docking SimulationProtein Structure, TertiaryStructure-Activity RelationshipCyanidesCyclic AMPGuanine Nucleotide Exchange FactorsRAPGEF3 protein, humanRAPGEF4 protein, humanAntagonistEPACExchange proteins directly activated by cAMPMolecular docking

Identifiers

PMID29100797
PMCPMC5693616
OpenAlexW2766588840

What OpenQuestion holds

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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.