Evidence map›Paper›PMID 37082750›Full record

ArticleACS pharmacology & translational science2023

Biochemical Discovery, Intracellular Evaluation, and Crystallographic Characterization of Synthetic and Natural Product Adenosine 3',5'-Cyclic Monophosphate-Dependent Protein Kinase A (PKA) Inhibitors.

Brice A P Wilson, Ning Li, Juliana A Martinez Fiesco, Masoumeh Dalilian, Dongdong Wang, Emily A Smith, Antony Wamiru, Rohan Shah, Ekaterina I Goncharova, John A Beutler and 3 more

Open access · greenAbstract read
In one paragraph

Article in ACS pharmacology & translational science, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 31% 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

5 citing papers in PubMed, 4 citations in OpenAlex.

  1. Article
  2. Article
  3. Identification of Cembrane Diterpenoids fromJournal of natural products · 2025
    Article
  4. Article
  5. 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

13 authors at 3 institutions in 1 country.

Brice A P WilsonMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.ORCID https://orcid.org/0000-0001-8988-1964
Ning LiCenter for Structural Biology, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
Juliana A Martinez FiescoCenter for Structural Biology, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
Masoumeh DalilianMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
Dongdong WangMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.ORCID https://orcid.org/0000-0002-7824-2507
Emily A SmithMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
Antony WamiruMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
Rohan ShahMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
Ekaterina I GoncharovaMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
John A BeutlerMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.ORCID https://orcid.org/0000-0002-4646-1924
Tanja GrkovicMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.ORCID https://orcid.org/0000-0002-6537-3997
Ping ZhangCenter for Structural Biology, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
Barry R O'KeefeMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.ORCID https://orcid.org/0000-0003-0772-4856
Target (United States) · USLeidos (United States) · USNational Cancer Institute · US

Funding

WORK ORDER 126643 B539 EXPAND IC SUITE75N91019D00024 · NIAID · LEIDOS BIOMEDICAL RESEARCH, INC. · PI BRISCOE, LYNN · 2019 to 2025
$3932.6M
Assay development and screening for molecular targets and discoveryZIABC011904 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI WILSON, BRICE · 2019 to 2025
$12.8M
Structures and Mechanisms of Kinase Signaling ComplexesZIABC011744 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI ZHANG, PING · 2017 to 2025
$12.6M
Cell-free assay technologies for the identification of active compoundsZIABC011471 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI OKEEFE, BARRY · 2012 to 2025
$12.4M
Development of Natural Product Leads as Anticancer TherapeuticsZIABC011470 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BEUTLER, JOHN · 2012 to 2025
$7.8M
NCI Program for Natural Products Discovery - CuresZIABC011854 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI OKEEFE, BARRY · 2020 to 2025
$5.2M
Intramural NIH HHS ZIA BC011471Intramural NIH HHS ZIA BC011744Intramural NIH HHS ZIA BC011854Intramural NIH HHS ZIA BC011904NCI NIH HHS 75N91019D00024
6 · The paper itself

Abstract

The recent demonstration that adenosine 3',5'-cyclic monophosphate (cAMP)-dependent protein kinase A (PKA) plays an oncogenic role in a number of important cancers has led to a renaissance in drug development interest targeting this kinase. We therefore have established a suite of biochemical, cell-based, and structural biology assays for identifying and evaluating new pharmacophores for PKA inhibition. This discovery process started with a 384-well high-throughput screen of more than 200,000 substances, including fractionated natural product extracts. Identified active compounds were further prioritized in biochemical, biophysical, and cell-based assays. Priority lead compounds were assessed in detail to fully characterize several previously unrecognized PKA pharmacophores including the generation of new X-ray crystallography structures demonstrating unique interactions between PKA and bound inhibitor molecules.

Identifiers

PMID37082750
PMCPMC10111623
OpenAlexW4328123449

What OpenQuestion holds

Textmetadata
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.