Evidence map›Paper›PMID 38958364›Full record

ArticleBrazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologica2024

FRAX486, a PAK inhibitor, overcomes ABCB1-mediated multidrug resistance in breast cancer cells.

Meng Zhang, Xiaoqi Zeng, Meiling She, Xingduo Dong, Jun Chen, Qingquan Xiong, Guobin Qiu, Shuyi Yang, Xiangqi Li, Guanghui Ren

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologica, 2024. 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

10 authors.

Meng ZhangDepartment of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.ORCID http://orcid.org/0009-0005-2664-6701
Xiaoqi ZengDepartment of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.ORCID http://orcid.org/0009-0004-0618-9534
Meiling SheSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong, China.ORCID http://orcid.org/0000-0002-8425-8652
Xingduo DongDepartment of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, New York, USA.ORCID http://orcid.org/0009-0004-4467-2842
Jun ChenDepartment of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.ORCID http://orcid.org/0009-0000-6066-0199
Qingquan XiongDepartment of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.ORCID http://orcid.org/0009-0004-2107-8840
Guobin QiuDepartment of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.ORCID http://orcid.org/0009-0003-3603-9935
Shuyi YangDepartment of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.ORCID http://orcid.org/0009-0005-5756-1313
Xiangqi LiDepartment of Breast Surgery, The Second Affiliated Hospital of Shandong First Medical University, Tai'an, Shandong, China.ORCID http://orcid.org/0009-0008-5589-9806
Guanghui RenDepartment of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.ORCID http://orcid.org/0009-0009-6044-2373

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The overexpression of P-glycoprotein (P-gp/ABCB1) is a leading cause of multidrug resistance (MDR). Hence, it is crucial to discover effective pharmaceuticals that counteract ABCB1-mediated multidrug resistance. FRAX486 is a p21-activated kinase (PAK) inhibitor. The objective of this study was to investigate whether FRAX486 can reverse ABCB1-mediated multidrug resistance, while also exploring its mechanism of action. The CCK8 assay demonstrated that FRAX486 significantly reversed ABCB1-mediated multidrug resistance. Furthermore, western blotting and immunofluorescence experiments revealed that FRAX486 had no impact on expression level and intracellular localization of ABCB1. Notably, FRAX486 was found to enhance intracellular drug accumulation and reduce efflux, resulting in the reversal of multidrug resistance. Docking analysis also indicated a strong affinity between FRAX486 and ABCB1. This study highlights the ability of FRAX486 to reverse ABCB1-mediated multidrug resistance and provides valuable insights for its clinical application.

Indexed as

ATP Binding Cassette Transporter, Subfamily BBreast NeoplasmsDrug Resistance, MultipleDrug Resistance, NeoplasmBlotting, WesternCell Line, TumorFemaleHumansp21-Activated KinasesABCB1 protein, humanATP Binding Cassette Transporter, Subfamily Bp21-Activated Kinases

Identifiers

PMID38958364
PMCPMC11221864

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Registered trials

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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.