Evidence map›Paper›PMID 38866385›Full record

ArticleJournal of medicinal chemistry2024

Discovery of CDC42 Inhibitors with a Favorable Pharmacokinetic Profile and Anticancer In Vivo Efficacy.

Nicoletta Brindani, Linh M Vuong, Maria Antonietta La Serra, Noel Salvador, Andrea Menichetti, Isabella Maria Acquistapace, Jose Antonio Ortega, Marina Veronesi, Sine Mandrup Bertozzi, Maria Summa and 5 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

15 authors.

Nicoletta BrindaniMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.
Linh M VuongDepartment of Dermatology, University of California, Irvine, California 92697, United States.
Maria Antonietta La SerraMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.ORCID 0000-0001-8732-9965
Noel SalvadorDepartment of Dermatology, University of California, Irvine, California 92697, United States.
Andrea MenichettiMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.
Isabella Maria AcquistapaceMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.ORCID 0000-0002-5820-7683
Jose Antonio OrtegaMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.
Marina VeronesiStructural Biophysics Facility, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.
Sine Mandrup BertozziAnalytical Chemistry Facility, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.
Maria SummaTranslational Pharmacology Facility, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.
Stefania GirottoStructural Biophysics Facility, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.ORCID 0000-0002-0339-6675
Rosalia BertorelliTranslational Pharmacology Facility, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.
Andrea ArmirottiAnalytical Chemistry Facility, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.ORCID 0000-0002-3766-8755
Anand K GanesanDepartment of Dermatology, University of California, Irvine, California 92697, United States.
Marco De VivoMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, via Morego 30, 16163 Genova, Italy.ORCID 0000-0003-4022-5661

Funding

UCI P30 Skin Center Systems Biology CoreP30AR075047 · NIAMS · UNIVERSITY OF CALIFORNIA-IRVINE · PI ANDERSEN, BOGI, GANESAN, ANAND K · 2019 to 2025
$5.1M
Identifying Therapeutic Targets for Stage III MelanomaR01CA244571 · NCI · UNIVERSITY OF CALIFORNIA-IRVINE · PI GANESAN, ANAND K · 2020 to 2024
$2.4M
NCI NIH HHS R01 CA244571NIAMS NIH HHS P30 AR075047
6 · The paper itself

Abstract

We previously reported trisubstituted pyrimidine lead compounds, namely, ARN22089 and ARN25062, which block the interaction between CDC42 with its specific downstream effector, a PAK protein. This interaction is crucial for the progression of multiple tumor types. Such inhibitors showed anticancer efficacy in vivo. Here, we describe a second class of CDC42 inhibitors with favorable drug-like properties. Out of the 25 compounds here reported, compound

Indexed as

Antineoplastic Agentscdc42 GTP-Binding ProteinAnimalsCell Line, TumorDrug DiscoveryFemaleHumansMicePyrimidinesStructure-Activity RelationshipXenograft Model Antitumor AssaysAntineoplastic Agentscdc42 GTP-Binding ProteinPyrimidines

Identifiers

PMID38866385
PMCPMC11215724

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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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.