Evidence map›Paper›PMID 29975048›Full record

ArticleBiochemistry2018

Identification of a PDE4-Specific Pocket for the Design of Selective Inhibitors.

Xiaoqing Feng, Huanchen Wang, Mengchun Ye, Xue-Tao Xu, Ying Xu, Wenzhe Yang, Han-Ting Zhang, Guoqiang Song, Hengming Ke

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 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
–field-weighted citation impact
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

8 citing papers in PubMed.

  1. Article
  2. Advances in pyrazolo[1,5-RSC advances · 2025
    Review
  3. Article
  4. Article
  5. Review
  6. Article
  7. Article
  8. 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

9 authors.

Xiaoqing FengSchool of Pharmaceutical Engineering and Life Sciences , Changzhou University , Changzhou , Jiangsu 213164 , P. R. China.
Huanchen WangDepartment of Biochemistry and Biophysics and Lineberger Comprehensive Cancer Center , The University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599-7260 , United States.
Mengchun YeDepartment of Biochemistry and Biophysics and Lineberger Comprehensive Cancer Center , The University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599-7260 , United States.
Xue-Tao XuSchool of Chemical and Environmental Engineering , Wuyi University , Jiangmen , Guangdong 529020 , P. R. China.
Ying XuDepartments of Behavioral Medicine and Psychiatry, Physiology, Pharmacology, and Neuroscience and Rockefeller Neurosciences Institute , West Virginia University Health Sciences Center , Morgantown , West Virginia 26506-9137 , United States.
Wenzhe YangDepartment of Biochemistry and Biophysics and Lineberger Comprehensive Cancer Center , The University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599-7260 , United States.
Han-Ting ZhangDepartments of Behavioral Medicine and Psychiatry, Physiology, Pharmacology, and Neuroscience and Rockefeller Neurosciences Institute , West Virginia University Health Sciences Center , Morgantown , West Virginia 26506-9137 , United States.
Guoqiang SongSchool of Pharmaceutical Engineering and Life Sciences , Changzhou University , Changzhou , Jiangsu 213164 , P. R. China.
Hengming KeDepartment of Biochemistry and Biophysics and Lineberger Comprehensive Cancer Center , The University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599-7260 , United States.ORCID 0000-0001-8864-7279

Funding

Case Center for Synchrotron BiosciencesP30EB009998 · NIBIB · CASE WESTERN RESERVE UNIVERSITY · PI CHANCE, MARK R · 2009 to 2018
$8.4M
Substrate specificity and inhibitor selectivity of PDER01GM059791 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI KE, HENGMING · 2000 to 2013
$3.0M
Intramural NIH HHS Z99 ES999999NIBIB NIH HHS P30 EB009998NIGMS NIH HHS R01 GM059791
6 · The paper itself

Abstract

Inhibitors of phosphodiesterases (PDEs) have been widely studied as therapeutics for the treatment of human diseases, but improvement of inhibitor selectivity is still desirable for the enhancement of inhibitor potency. Here, we report identification of a water-containing subpocket as a PDE4-specific pocket for inhibitor binding. We designed against the pocket and synthesized two enantiomers of PDE4 inhibitor Zl-n-91. The ( S)-Zl-n-91 enantiomer showed IC

Indexed as

Drug DesignAnimalsBinding SitesCatalytic DomainCyclic Nucleotide Phosphodiesterases, Type 4FuransHumansHydrogen BondingMaleMemoryMice, Inbred ICRMolecular Docking SimulationPhenyl EthersPhosphodiesterase 4 InhibitorsRolipramStereoisomerismCyclic Nucleotide Phosphodiesterases, Type 4FuransPhenyl EthersPhosphodiesterase 4 InhibitorsRolipramWaterZl-n-91 compound

Identifiers

PMID29975048
PMCPMC6088244

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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.