Evidence map›Paper›PMID 31720502›Full record

ArticleACS omega2019

Pharmacokinetics of the Rac/Cdc42 Inhibitor MBQ-167 in Mice by Supercritical Fluid Chromatography-Tandem Mass Spectrometry.

María Del Mar Maldonado, Gabriela Rosado-González, Joseph Bloom, Jorge Duconge, Jean F Ruiz-Calderón, Eliud Hernández-O'Farrill, Cornelis Vlaar, José F Rodríguez-Orengo, Suranganie Dharmawardhane

Abstract read
In one paragraph

Article in ACS omega, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing 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

10 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Polymorphism in early development: The account of MBQ-167.International journal of pharmaceutics · 2021
    Article
  9. Progress in the therapeutic inhibition of Cdc42 signalling.Biochemical Society transactions · 2021
    Review
  10. 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

9 authors.

María Del Mar MaldonadoDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
Gabriela Rosado-GonzálezDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
Joseph BloomDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
Jorge DucongeDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
Jean F Ruiz-CalderónDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
Eliud Hernández-O'FarrillDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
Cornelis VlaarDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
José F Rodríguez-OrengoDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.
Suranganie DharmawardhaneDepartment of Biochemistry and Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico Medical Sciences Campus, PO Box 365067, San Juan, Puerto Rico 00936-5067, United States.

Funding

SCIENCE AND TECHNOLOGY COMPETENCY & EDUCATION CORE (STCE)P20GM103475 · NIGMS · UNIVERSITY OF PUERTO RICO MED SCIENCES · PI Jose R. Rodriguez-Medina · 2012 to 2026
$52.9M
Upstream Regulation and Downstream effectors of c-MYC in Ovarian CancerU54MD007600 · NIMHD · UNIVERSITY OF PUERTO RICO MED SCIENCES · PI Emma Fernandez-Repollet · 2017 to 2026
$35.8M
RISE Option III: MBRS RISE at the UPR Medical Sciences CampusR25GM061838 · NIGMS · UNIVERSITY OF PUERTO RICO MED SCIENCES · PI CADILLA, CARMEN LYDIA · 2000 to 2021
$25.5M
Targeting breast cancer progressionSC3GM084824 · NIGMS · UNIVERSITY OF PUERTO RICO MED SCIENCES · PI DHARMAWARDHANE, SURANGANIE · 2008 to 2021
$1.6M
Towards the Development of Novel Vav-Rac InhibitorsSC3GM116713 · NIGMS · UNIVERSITY OF PUERTO RICO MED SCIENCES · PI VLAAR, CORNELIS P · 2016 to 2019
$450k
NIGMS NIH HHS P20 GM103475NIGMS NIH HHS R25 GM061838NIGMS NIH HHS SC3 GM084824NIGMS NIH HHS SC3 GM116713NIMHD NIH HHS U54 MD007600
6 · The paper itself

Abstract

The Rho GTPases Rac and Cdc42 are potential targets against metastatic diseases. We characterized the small molecule MBQ-167 as an effective dual Rac/Cdc42 inhibitor that reduces HER2-type tumor growth and metastasis in mice by ∼90%. This study reports the pharmacokinetics and tissue distribution of MBQ-167 following intraperitoneal and oral single-dose administrations. We first developed and validated a bioanalytical method for the quantitation of MBQ-167 in mouse plasma and tissues by supercritical fluid chromatography coupled with electrospray ionization tandem mass spectrometry. MBQ-167 was rapidly distributed into the kidneys after intraperitoneal dosing, whereas oral administration resulted in higher distribution to lungs. The elimination half-lives were 2.17 and 2.6 h for the intraperitoneal and oral dosing, respectively. The relative bioavailability of MBQ-167 after oral administration was 35%. This investigation presents the first analysis of the pharmacokinetics of MBQ-167 and supports further preclinical evaluation of this drug as a potential anticancer therapeutic.

Identifiers

PMID31720502
PMCPMC6843717

What OpenQuestion holds

Textmetadata
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.