Evidence map›Paper›PMID 38901801›Full record

ArticleMolecular and biochemical parasitology2024

Pyridopyrimidinones as a new chemotype of calcium dependent protein kinase 1 (CDPK1) inhibitors for Cryptosporidium.

Elise Waldron-Young, Wissarut Wijitrmektong, Ryan Choi, Grant R Whitman, Matthew A Hulverson, Raheela Charania, Aidan Keelaghan, Li Li, Songpol Srinual, Sameer Nikhar and 8 more

Abstract read
In one paragraph

Article in Molecular and biochemical parasitology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Article
  2. Article
  3. 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

18 authors.

Elise Waldron-YoungDepartment of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Wissarut WijitrmektongDepartment of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Ryan ChoiDepartment of Allergy and Infectious Diseases, University of Washington, Seattle, WA 98109, United States.
Grant R WhitmanDepartment of Allergy and Infectious Diseases, University of Washington, Seattle, WA 98109, United States.
Matthew A HulversonDepartment of Allergy and Infectious Diseases, University of Washington, Seattle, WA 98109, United States.
Raheela CharaniaDepartment of Pediatrics, Emory University and Children's Healthcare Organization of Atlanta, Atlanta, GA 30322, United States; Atlanta VA Medical Center, Decatur, GA 30033, United States.
Aidan KeelaghanDepartment of Pediatrics, Emory University and Children's Healthcare Organization of Atlanta, Atlanta, GA 30322, United States; Atlanta VA Medical Center, Decatur, GA 30033, United States.
Li LiDepartment of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Songpol SrinualDepartment of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Sameer NikharDepartment of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Case W McNamaraCalibr-Skaggs Institute for Innovative Medicines, A division of The Scripps Research Institute, La Jolla, CA 92037, United States.
Melissa S LoveCalibr-Skaggs Institute for Innovative Medicines, A division of The Scripps Research Institute, La Jolla, CA 92037, United States.
Lauren HuertaCalibr-Skaggs Institute for Innovative Medicines, A division of The Scripps Research Institute, La Jolla, CA 92037, United States.
Malina A BakowskiCalibr-Skaggs Institute for Innovative Medicines, A division of The Scripps Research Institute, La Jolla, CA 92037, United States.
Ming HuDepartment of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Wesley C Van VoorhisDepartment of Allergy and Infectious Diseases, University of Washington, Seattle, WA 98109, United States.
Jan R MeadDepartment of Pediatrics, Emory University and Children's Healthcare Organization of Atlanta, Atlanta, GA 30322, United States; Atlanta VA Medical Center, Decatur, GA 30033, United States.
Gregory D CunyDepartment of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States. Electronic address: gdcuny@central.uh.edu.

Funding

Optimization of Lead BKIs for Cryptosporidiosis TherapyR01AI155412 · NIAID · UNIVERSITY OF WASHINGTON · PI VAN VOORHIS, WESLEY C · 2021 to 2025
$4.1M
IMPDH inhibitors for the treatment of Cryptosporidium infectionsR01AI125362 · NIAID · UNIVERSITY OF HOUSTON · PI CUNY, GREGORY D · 2016 to 2020
$3.8M
NIAID NIH HHS R01 AI125362NIAID NIH HHS R01 AI155412
6 · The paper itself

Abstract

The protozoan protein kinase calcium-dependent protein kinase 1 (CDPK1) has emerged as a potential therapeutic target for the treatment of cryptosporidiosis. A focused screen of known kinase inhibitors identified a pyridopyrimidinone as a new chemotype of Cryptosporidium parvum (Cp) CDPK1 inhibitors. Structural comparison of CpCDPK1 to two representative human kinases, RIPK2 and Src, revealed differences in the positioning of the αC-helix that was used in the design of a potent pyridopyrimidinone-based CpCDPK1 inhibitor 7 (a.k.a. UH15-16, IC

Indexed as

CryptosporidiosisCryptosporidium parvumProtein Kinase InhibitorsProtein KinasesAnimalsAntiprotozoal AgentsCaco-2 CellsCalcium-Calmodulin-Dependent Protein KinasesCryptosporidiumDisease Models, AnimalHumansInhibitory Concentration 50MiceProtozoan ProteinsPyrimidinonesAntiprotozoal AgentsCalcium-Calmodulin-Dependent Protein KinasesProtein Kinase InhibitorsProtein KinasesProtozoan ProteinsPyrimidinonesCalcium dependent protein kinase 1CDPK1ChemotypeCryptosporidiumInhibitorPyridopyrimidinone

Identifiers

PMID38901801
PMCPMC11629397

What OpenQuestion holds

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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.