Evidence map›Paper›PMID 28385503›Full record

ArticleBioorganic & medicinal chemistry letters2017

Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.

Joseph M Salvino, Yellamelli V V Srikanth, Rongliang Lou, Halley M Oyer, Nan Chen, Felix J Kim

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Review
  2. 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

6 authors.

Joseph M SalvinoDepartment of Pharmacology and Physiology, Drexel University College of Medicine, 245 N 15th Street, Philadelphia, PA 19102-1101, USA. Electronic address: jsalvino@wistar.org.
Yellamelli V V SrikanthDepartment of Pharmacology and Physiology, Drexel University College of Medicine, 245 N 15th Street, Philadelphia, PA 19102-1101, USA.
Rongliang LouAstaTech, Inc., Keystone Business Park, 2525 Pearl Buck Road, Bristol, PA 19007, USA.
Halley M OyerDepartment of Pharmacology and Physiology, Drexel University College of Medicine, 245 N 15th Street, Philadelphia, PA 19102-1101, USA.
Nan ChenDepartment of Pharmacology and Physiology, Drexel University College of Medicine, 245 N 15th Street, Philadelphia, PA 19102-1101, USA.
Felix J KimDepartment of Pharmacology and Physiology, Drexel University College of Medicine, 245 N 15th Street, Philadelphia, PA 19102-1101, USA.

Funding

Tumor Microenvironment and MetastasisP30CA010815 · NCI · WISTAR INSTITUTE · PI Luis J Montaner · 1985 to 2026
$75.9M
Multifunctional Regulation of Prostate Cancer Metabolism by Sigma1 ModulatorsR01CA244749 · NCI · THOMAS JEFFERSON UNIVERSITY · PI KIM, FELIX JINHYUN · 2020 to 2024
$3.1M
A Potent Small Molecule Sigma1 Modulator Degrades Androgen Receptor In Castration Resistant Prostate CancerR43CA206691 · NCI · CONTEXT THERAPEUTICS, LLC · PI KIM, FELIX JINHYUN, LEHR, MARTIN · 2016 to 2016
$225k
NCI NIH HHS P30 CA010815NCI NIH HHS R01 CA244749NCI NIH HHS R43 CA206691
6 · The paper itself

Abstract

Prostate cancer is the most frequently diagnosed malignancy and the leading cause of cancer related death in men. First line therapy for disseminated disease relies on androgen deprivation, leveraging the addiction of these tumors on androgens for both growth and survival. Treatment typically involves antagonizing the androgen receptor (AR) or blocking the synthesis of androgens. Recurrence is common and within 2-3years patients develop castration resistant tumors that become unresponsive to AR-axis targeted therapies. In order to provide a more effective treatment, we are utilizing an approach that targets a key scaffolding protein, Sigma1 (also known as sigma-1 receptor), a unique 26-kilodalton integral membrane protein that is critical in stabilizing the AR. Herein we report on a new series of Sigma1 compounds for lead optimization derived from a hybrid pharmacophore approach.

Indexed as

AnimalsERG1 Potassium ChannelGuanidinesHalf-LifeHumansMaleMiceMicrosomes, LiverNeoplasm StagingProstatic NeoplasmsProtein BindingReceptors, sigmaSigma-1 ReceptorStructure-Activity RelationshipERG1 Potassium ChannelGuanidinesReceptors, sigmaSigma-1 ReceptorGuanidineProstate cancerSigma1Sigma-1 chaperoneSigma-1 receptorSmall molecule inhibitor

Identifiers

PMID28385503
PMCPMC5714280

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.