Evidence map›Paper›PMID 36812406›Full record

ArticleMolecular pharmaceutics2023

Unusually High Affinity of the PLK Inhibitors RO3280 and GSK461364 to HSA and Its Possible Pharmacokinetic Implications.

Jesús Fernández-Sainz, Pedro J Pacheco-Liñán, Consuelo Ripoll, Joaquín González-Fuentes, José Albaladejo, Iván Bravo, Andrés Garzón-Ruiz

Open access · hybridAbstract read
In one paragraph

Article in Molecular pharmaceutics, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.1field-weighted citation impact, top 23% 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

3 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
  2. Article
  3. PLK1 inhibition impairs erythroid differentiation.Frontiers in cell and developmental biology · 2024
    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

7 authors at 1 institution in 1 country.

Jesús Fernández-SainzDepartamento de Química Física, Facultad de Farmacia, Universidad de Castilla-La Mancha, Av. Dr. José María Sánchez Ibáñez, s/n, 02071 Albacete, Spain.ORCID 0000-0003-3417-8416
Pedro J Pacheco-LiñánDepartamento de Química Física, Facultad de Farmacia, Universidad de Castilla-La Mancha, Av. Dr. José María Sánchez Ibáñez, s/n, 02071 Albacete, Spain.ORCID 0000-0002-8591-0147
Consuelo RipollDepartamento de Química Física, Facultad de Farmacia, Universidad de Castilla-La Mancha, Av. Dr. José María Sánchez Ibáñez, s/n, 02071 Albacete, Spain.
Joaquín González-FuentesCentro Regional de Investigaciones Biomédicas (CRIB), Unidad Asociada de Biomedicina (UCLM-CSIC), C/ Almansa, 14, 02008 Albacete, Spain.
José AlbaladejoDepartamento de Química Física, Facultad de Ciencias y Tecnologías Químicas, Universidad de Castilla-La Mancha, Avenida Camilo José Cela, 10, 13071 Ciudad Real, Spain.
Iván BravoDepartamento de Química Física, Facultad de Farmacia, Universidad de Castilla-La Mancha, Av. Dr. José María Sánchez Ibáñez, s/n, 02071 Albacete, Spain.ORCID 0000-0003-1589-5399
Andrés Garzón-RuizDepartamento de Química Física, Facultad de Farmacia, Universidad de Castilla-La Mancha, Av. Dr. José María Sánchez Ibáñez, s/n, 02071 Albacete, Spain.ORCID 0000-0002-0077-4562
University of Castilla-La Mancha · ES

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The binding processes of two Polo-like kinase inhibitors, RO3280 and GSK461364, to the human serum albumin (HSA) protein as well as the protonation equilibria of both compounds have been studied combining absorbance and fluorescence spectroscopy experiments together with density functional theory calculations. We found that the charge states of RO3280 and GSK461364 are +2 and +1, respectively, at the physiological pH. Nevertheless, RO3280 binds to HSA in the charge state +1 prior to a deprotonation pre-equilibrium. Binding constants to site I of HSA of 2.23 × 10

Indexed as

Serum AlbuminSerum Albumin, HumanAzepinesBenzimidazolesBinding SitesHumansProtein BindingPyrimidinesSpectrometry, FluorescenceThermodynamicsThiophenesAzepinesBenzimidazolesGSK 461364PyrimidinesRO3280Serum AlbuminSerum Albumin, HumanThiophenesdrug−protein bindingfluorescence spectroscopyGSK461364human serum albuminRO3280

Identifiers

PMID36812406
PMCPMC9997069
OpenAlexW4321482401

What OpenQuestion holds

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LicenceCC BY
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.