Evidence map›Paper›PMID 37392559›Full record

ArticleBioorganic chemistry2023

Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model.

Retheesh S Thankan, Elizabeth Thomas, Puranik Purushottamachar, David J Weber, Vincent C O Njar

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

Article in Bioorganic chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
2.2field-weighted citation impact, top 12% 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

4 citing papers in PubMed, 9 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. 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

5 authors at 1 institution in 1 country.

Retheesh S ThankanDepartment of Pharmacology, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; The Center for Biomolecular Therapeutics, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; Isoprene Pharmaceuticals, Inc. 801 West Baltimore Street, Suite 502J, Baltimore, MD 21201, USA. Electronic address: retheeshst@som.umaryland.edu.
Elizabeth ThomasDepartment of Pharmacology, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; The Center for Biomolecular Therapeutics, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA. Electronic address: elizabeththomas@som.umaryland.edu.
Puranik PurushottamacharDepartment of Pharmacology, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; The Center for Biomolecular Therapeutics, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; Isoprene Pharmaceuticals, Inc. 801 West Baltimore Street, Suite 502J, Baltimore, MD 21201, USA. Electronic address: PPuranik@som.umaryland.edu.
David J WeberThe Center for Biomolecular Therapeutics, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, Baltimore, MD 21201, USA; Marlene and Stewart Greenebaum Comprehensive Cancer Center, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; Isoprene Pharmaceuticals, Inc. 801 West Baltimore Street, Suite 502J, Baltimore, MD 21201, USA. Electronic address: DWeber@som.umaryland.edu.
Vincent C O NjarDepartment of Pharmacology, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; The Center for Biomolecular Therapeutics, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; Marlene and Stewart Greenebaum Comprehensive Cancer Center, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201, USA; Isoprene Pharmaceuticals, Inc. 801 West Baltimore Street, Suite 502J, Baltimore, MD 21201, USA. Electronic address: vnjar@som.umaryland.edu.
University of Maryland, Baltimore · US

Funding

Development of Next Generation Galeterone Analogs for Prostate Cancer TherapyR01CA224696 · NCI · UNIVERSITY OF MARYLAND BALTIMORE · PI NJAR, VINCENT COLLINS OFUKA · 2018 to 2022
$2.6M
NCI NIH HHS R01 CA224696
6 · The paper itself

Abstract

Galeterone, 3β-(hydroxy)-17-(1H-benzimidazole-1-yl)androsta-5,16-diene (Gal, 1) and VNPP433-3β, 3β-(1H-imidazole-1-yl-17-(1H-benzimidazole-1-yl)androsta-5,16-diene (2) are potent molecular glue degrader modulators of AR/AR-V7 and Mnk1/2-eIF4E signaling pathways, and are promising Phase 3 and Phase 1 drug candidates, respectively. Because appropriate salts can be utilized to create new chemical entities with enhanced aqueous solubility, in vivo pharmacokinetics, and enhanced in vitro and in vivo efficacies, the monohydrochloride salt of Gal (3) and the mono- and di-hydrochlorides salts of compound 2, compounds 4 and 5, respectively, were synthesized. The salts were characterized using

Indexed as

AndrostadienesBenzimidazolesProstatic Neoplasms, Castration-ResistantAnimalsBenzamidesCell Line, TumorDocetaxelHeterograftsHumansImidazolesMaleMiceNitrilesPhenylthiohydantoinReceptors, AndrogenSalts3beta-(1H-imidazole-1-yl-17-(1H-benzimidazole-1-yl)androsta-5,16-diene3-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-dieneAndrostadienesBenzamidesBenzimidazolesDocetaxelenzalutamideImidazolesNitrilesPhenylthiohydantoinReceptors, AndrogenSaltsVNPP433-3betaAntitumor efficacyAR/AR-V7 and Mnk1/2 Molecular Glue DegradersCastration-resistant prostate cancer (CRPC)Galeterone (Gal)HCl saltsProstate cancerVNPP433-3β

Identifiers

PMID37392559
PMCPMC10528634
OpenAlexW4381953306

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.