Evidence map›Paper›PMID 25956413›Full record

ArticleBioorganic & medicinal chemistry letters2015

Synthesis and evaluation of constrained phosphoramidate inhibitors of prostate-specific membrane antigen.

Corinne R Ley, Nathan R Beattie, Shorouk Dannoon, Melanie Regan, Henry VanBrocklin, Clifford E Berkman

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

Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
2.2field-weighted citation impact, top 13% 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

6 citing papers in PubMed, 14 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Metal-Based PSMA Radioligands.Molecules (Basel, Switzerland) · 2017
    Review
  6. Prostate-specific membrane antigen as a target for cancer imaging and therapy.The quarterly journal of nuclear medicine and molecular imaging : official publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR), [and] Section of the Society of... · 2015
    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

6 authors at 2 institutions in 1 country.

Corinne R LeyDepartment of Chemistry, Washington State University, Pullman, WA 99164-4630, USA.
Nathan R BeattieDepartment of Chemistry, Washington State University, Pullman, WA 99164-4630, USA.
Shorouk DannoonDepartment of Radiology and Biomedical Imaging, University of California, San Francisco, CA 94158, USA.
Melanie ReganDepartment of Radiology and Biomedical Imaging, University of California, San Francisco, CA 94158, USA.
Henry VanBrocklinDepartment of Radiology and Biomedical Imaging, University of California, San Francisco, CA 94158, USA.
Clifford E BerkmanDepartment of Chemistry, Washington State University, Pullman, WA 99164-4630, USA. Electronic address: cberkman@wsu.edu.
University of California, San Francisco · USWashington State University · US

Funding

Probe Optimization for Prostate Cancer DetectionR01CA140617 · NCI · WASHINGTON STATE UNIVERSITY · PI BERKMAN, CLIFFORD · 2010 to 2013
$1.8M
NCI NIH HHS R01 CA140617NCI NIH HHS R01CA140617
6 · The paper itself

Abstract

Prostate-specific membrane antigen (PSMA) is a cell-surface enzyme-biomarker that is actively pursued for targeted delivery of imaging and therapeutic agents for prostate cancer. Our lab has developed PSMA inhibitors based on a phosphoramidate scaffold, which has shown both high selectivity for PSMA-positive tumors and rapid clearance in vivo when radiolabeled with (18)F. However, this scaffold exhibits hydrolytic instability under low pH and high temperature conditions, barring the use of other imaging or therapeutic radionuclides such as (68)Ga or (177)Lu. Previous studies in our lab have shown a trend in increasing acid stability as the distance between the phosphoramidate core and the α-carboxylate of the P1 residue is increased. Therefore, a new generation of phosphoramidate inhibitors was developed based on trans-4-hydroxyproline as the P1 residue to restrict the interaction of the α-carboxylate to the phosphoramidate core. These hydroxyproline inhibitors demonstrated comparable IC50 values to earlier generations as well as enhanced thermal and acid stability.

Indexed as

AmidesAnimalsAntigens, SurfaceCell Line, TumorContrast MediaDrug Evaluation, PreclinicalGlutamate Carboxypeptidase IIHumansMaleMiceMice, NudePhosphoric AcidsPositron-Emission TomographyProstatic NeoplasmsProtein BindingRadiopharmaceuticalsAmidesAntigens, SurfaceContrast MediaFOLH1 protein, humanGlutamate Carboxypeptidase IIphosphoramidic acidPhosphoric AcidsRadiopharmaceuticals4-HydroxyprolineInhibitorPhosphoramidateProstate cancerProstate-specific membrane antigen

Identifiers

PMID25956413
PMCPMC7588815
OpenAlexW2046612580

What OpenQuestion holds

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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.