Evidence map›Paper›PMID 39764864›Full record

ArticleBioorganic & medicinal chemistry2025

Fine-tuning probes for fluorescence polarization binding assays of bivalent ligands against polo-like kinase 1 using full-length protein.

Kohei Tsuji, Hirokazu Tamamura, Terrence R Burke

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

3 authors.

Kohei TsujiDepartment of Medicinal Chemistry, Laboratory for Biomaterials and Bioengineering, Institute of Integrated Research, Institute of Science Tokyo, 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan; Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, 1050 Boyles St., Frederick, MD 21702, USA. Electronic address: ktsuji.mr@tmd.ac.jp.
Hirokazu TamamuraDepartment of Medicinal Chemistry, Laboratory for Biomaterials and Bioengineering, Institute of Integrated Research, Institute of Science Tokyo, 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
Terrence R BurkeChemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, 1050 Boyles St., Frederick, MD 21702, USA.

Funding

INHIBITORS OF TYROSINE-SPECIFIC PROTEIN KINASES AS ANTICANCER AGENTSZ01BC006198 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BURKE, TERRENCE · 1996 to 2008
$1.6M
Intramural NIH HHS Z01 BC006198
6 · The paper itself

Abstract

Polo-like kinase 1 (Plk1) is an important cell cycle regulator that is a recognized target for development of anti-cancer therapeutics. Plk1 is composed of a catalytic kinase domain (KD), a flexible interdomain linker and a polo-box domain (PBD). Intramolecular protein-protein interactions (PPIs) between the PBD and KD result in "auto-inhibition" that is an essential component of proper Plk1 function. Recently, we developed high-affinity PBD-binding inhibitors using a bivalent approach. These ligands contain the low-nanomolar affinity Plk1 KD-binding inhibitors BI2536 or Wortmannin tethered to the PBD-binding peptide, PLH*SpT (H* represents a -(CH

Indexed as

Cell Cycle ProteinsFluorescence PolarizationPolo-Like Kinase 1Protein Kinase InhibitorsProtein Serine-Threonine KinasesProto-Oncogene ProteinsBinding SitesFluorescent DyesHumansLigandsMolecular StructureProtein BindingStructure-Activity RelationshipCell Cycle ProteinsFluorescent DyesLigandsPolo-Like Kinase 1Protein Kinase InhibitorsProtein Serine-Threonine KinasesProto-Oncogene ProteinsBivalent inhibitorFluorescence Polarization (FP) assayPhosphorylated threonine (pT)Polo-box domain (PBD)Polo-like kinase 1 (Plk1)

Identifiers

PMID39764864
PMCPMC12349915

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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.