Evidence map›Paper›PMID 37931521›Full record

ArticleBioorganic & medicinal chemistry2023

Discovery of a potent and selective human AC2 inhibitor based on 7-deazapurine analogues of adefovir.

Pavel Kraina, Michal Česnek, Eva Tloušťová, Helena Mertlíková-Kaiserová, Camryn J Fulton, Emily K Davidson, Brenton P Smith, Val J Watts, Zlatko Janeba

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.3field-weighted citation impact, top 36% 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

1 citing paper in PubMed, 2 citations in OpenAlex.

  1. Review
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 at 4 institutions in 3 countries.

Pavel KrainaInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, 16000 Prague 6, Czech Republic; Department of Organic Chemistry, University of Chemistry and Technology Prague, 16628 Prague 6, Czech Republic.
Michal ČesnekInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, 16000 Prague 6, Czech Republic.
Eva TloušťováInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, 16000 Prague 6, Czech Republic.
Helena Mertlíková-KaiserováInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, 16000 Prague 6, Czech Republic.
Camryn J FultonBorch Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA.
Emily K DavidsonBorch Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA.
Brenton P SmithBorch Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA.
Val J WattsBorch Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA. Electronic address: wattsv@purdue.edu.
Zlatko JanebaInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, 16000 Prague 6, Czech Republic. Electronic address: janeba@uochb.cas.cz.
Purdue University West Lafayette · USCzech Academy of Sciences, Institute of Organic Chemistry and Biochemistry · CZCzech Academy of Sciences · CZInstitute of Organic Chemistry · PL

Funding

Pharmacological validation of adenylyl cyclase 1 as a drug target for chronic painR01NS119917 · NINDS · PURDUE UNIVERSITY · PI FLAHERTY, DANIEL PATRICK, WATTS, VAL J · 2021 to 2025
$2.0M
Non-Opioids for Inflammatory Pain: Adenylyl Cyclase 1 as a Novel TargetR33NS111070 · NINDS · UNIVERSITY OF IOWA · PI ROMAN, DAVID L., WATTS, VAL J · 2021 to 2022
$822k
Non-opioids for inflammatory pain: Adenylyl cyclase 1 as a novel targetR61NS111070 · NINDS · UNIVERSITY OF IOWA · PI ROMAN, DAVID L., WATTS, VAL J · 2019 to 2019
$443k
NINDS NIH HHS R01 NS119917NINDS NIH HHS R33 NS111070NINDS NIH HHS R61 NS111070
6 · The paper itself

Abstract

Adefovir based acyclic nucleoside phosphonates were previously shown to modulate bacterial and, to a certain extent, human adenylate cyclases (mACs). In this work, a series of 24 novel 7-substituted 7-deazaadefovir analogues were synthesized in the form of prodrugs. Twelve analogues were single-digit micromolar inhibitors of Bordetella pertussis adenylate cyclase toxin with no cytotoxicity to J774A.1 macrophages. In HEK293 cell-based assays, compound 14 was identified as a potent (IC

Indexed as

Adenylyl CyclasesOrganophosphonatesAdenineAdenylate Cyclase ToxinHEK293 CellsHumansNucleosidesPurines7-deazapurineadefovirAdenineAdenylate Cyclase ToxinAdenylyl CyclasesNucleosidesOrganophosphonatesPurines7-DeazapurineAcyclic nucleoside phosphonatesAdefovirAdenylate cyclaseProdrugs

Identifiers

PMID37931521
PMCPMC10842932
OpenAlexW4388204975

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.