Evidence map›Paper›PMID 24256330›Full record

ReviewJournal of medicinal chemistry2014

Recent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC).

Haijun Chen, Christopher Wild, Xiaobin Zhou, Na Ye, Xiaodong Cheng, Jia Zhou

Open access · greenAbstract readReview
In one paragraph

Review in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.

0numbers the graph read from it
0cells of the map it votes in
28citing papers in PubMed
2.7field-weighted citation impact, top 9% 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

28 citing papers in PubMed, 44 citations in OpenAlex.

  1. Therapeutic effects of alprostadil on CClMolecular and cellular biochemistry · 2026
    Article
  2. Article
  3. Role of serine/threonine phosphatases 1 and 2A in pancreatic acinar fluid and electrolyte secretion.American journal of physiology. Gastrointestinal and liver physiology · 2026
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  9. Cyclic AMP-dependent protein kinase A and EPAC mediate VIP and secretin stimulation of PAK4 and activation of NaAmerican journal of physiology. Gastrointestinal and liver physiology · 2019
    Article
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  13. Review
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  18. Review
  19. The role of Epac in the heart.Cellular and molecular life sciences : CMLS · 2017
    Review
  20. 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

6 authors at 2 institutions in 2 countries.

Haijun ChenDepartment of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, Texas 77555, United States.
Christopher Wild
Xiaobin Zhou
Na Ye
Xiaodong Cheng
Jia Zhou
The University of Texas Medical Branch at Galveston · USFuzhou University · CN

Funding

Epac/cAMP-GEF, A Novel Intracellular cAMP ReceptorR01GM066170 · NIGMS · UNIVERSITY OF TEXAS MEDICAL BR GALVESTON · PI CHENG, XIAODONG · 2003 to 2017
$4.6M
Core Center for Translational Addiction SciencesP30DA028821 · NIDA · UNIVERSITY OF TEXAS MED BR GALVESTON · PI CUNNINGHAM, KATHRYN A. · 2009 to 2010
$1.5M
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
Training in Pharmacological SciencesT32GM089657 · NIGMS · UNIVERSITY OF TEXAS HLTH SCI CTR HOUSTON · PI HANCOCK, JOHN F · 2010 to 2014
$728k
Optimization of Allosteric Modulators of 5-HT2C ReceptorR21MH093844 · NIMH · UNIVERSITY OF TEXAS MED BR GALVESTON · PI CUNNINGHAM, KATHRYN A., ZHOU, JIA · 2012 to 2013
$450k
High throughput assay for novel pharmacological probes targeting cAMP signalingR21NS066510 · NINDS · UNIVERSITY OF TEXAS MED BR GALVESTON · PI CHENG, XIAODONG · 2010 to 2012
$191k
NIDA NIH HHS P30 DA028821NIGMS NIH HHS R01 GM066170NIGMS NIH HHS R01 GM106218NIGMS NIH HHS T32 GM089657NIMH NIH HHS R21 MH093844NINDS NIH HHS R21 NS066510
6 · The paper itself

Abstract

3',5'-Cyclic adenosine monophosphate (cAMP) is a pivotal second messenger that regulates numerous biological processes under physiological and pathological conditions, including cancer, diabetes, heart failure, inflammation, and neurological disorders. In the past, all effects of cAMP were initially believed to be mediated by protein kinase A (PKA) and cyclic nucleotide-regulated ion channels. Since the discovery of exchange proteins directly activated by cyclic adenosine 5'-monophosphate (EPACs) in 1998, accumulating evidence has demonstrated that the net cellular effects of cAMP are also regulated by EPAC. The pursuit of the biological functions of EPAC has benefited from the development and applications of a growing number of pharmacological probes targeting EPACs. In this review, we seek to provide a concise update on recent advances in the development of chemical entities including various membrane-permeable analogues of cAMP and newly discovered EPAC-specific ligands from high throughput assays and hit-to-lead optimizations.

Indexed as

Drug DiscoveryCrystallography, X-RayGuanine Nucleotide Exchange FactorsModels, MolecularSignal TransductionSmall Molecule LibrariesStructure-Activity RelationshipGuanine Nucleotide Exchange FactorsRAPGEF3 protein, humanSmall Molecule Libraries

Identifiers

PMID24256330
PMCPMC4016168
OpenAlexW2416301418

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.