Evidence map›Paper›PMID 35164144›Full record

ArticleMolecules (Basel, Switzerland)2022

Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action.

Peter Jaein Choi, Petr Tomek, Moana Tercel, Jóhannes Reynisson, Thomas In Hyeup Park, Elizabeth Alexandra Cooper, William Alexander Denny, Jiney Jose, Euphemia Leung

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2022. 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
2.0field-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, 13 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Article
  6. 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

9 authors at 2 institutions in 2 countries.

Peter Jaein ChoiAuckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland 1023, New Zealand.ORCID 0000-0001-7195-3683
Petr TomekAuckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland 1023, New Zealand.ORCID 0000-0002-5490-6540
Moana TercelAuckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland 1023, New Zealand.
Jóhannes ReynissonSchool of Pharmacy and Bioengineering, Keele University, Hornbeam Building, Newcastle under Lyme, Staffordshire ST5 5BG, UK.ORCID 0000-0003-4174-9512
Thomas In Hyeup ParkNeurosurgical Research Unit & Department of Pharmacology, The Centre for Brain Research, University of Auckland, Private Bag 92019, Auckland 1023, New Zealand.ORCID 0000-0002-7995-8865
Elizabeth Alexandra CooperNeurosurgical Research Unit & Department of Pharmacology, The Centre for Brain Research, University of Auckland, Private Bag 92019, Auckland 1023, New Zealand.
William Alexander DennyAuckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland 1023, New Zealand.ORCID 0000-0001-7997-1843
Jiney JoseAuckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland 1023, New Zealand.
Euphemia LeungAuckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland 1023, New Zealand.ORCID 0000-0002-6932-3188
University of Auckland · NZKeele University · GB

Funding

Cancer Research Trust New Zealand CRTNZ 2013 RPGMaurice Phyllis Paykel Trust 203123
6 · The paper itself

Abstract

The CDK4/6 inhibitor palbociclib, combined with endocrine therapy, has been shown to be effective in postmenopausal women with estrogen receptor-positive, HER2-negative advanced or metastatic breast cancer. However, palbociclib is not as effective in the highly aggressive, triple-negative breast cancer that lacks sensitivity to chemotherapy or endocrine therapy. We hypothesized that conjugation of the near-infrared dye MHI-148 with palbociclib can produce a potential theranostic in triple-negative, as well as estrogen receptor-positive, breast cancer cells. In our study, the conjugate was found to have enhanced activity in all mammalian cell lines tested in vitro. However, the conjugate was cytotoxic and did not induce G1 cell cycle arrest in breast cancer cells, suggesting its mechanism of action differs from the parent compound palbociclib. The study highlights the importance of investigating the mechanism of conjugates of near-infrared dyes to therapeutic compounds, as conjugation can potentially result in a change of mechanism or target, with an enhanced cytotoxic effect in this case.

Indexed as

Antineoplastic AgentsCarbocyaninesCytotoxinsIndolesPiperazinesPyridinesAnimalsBreast NeoplasmsCHO CellsCricetulusFemaleHEK293 CellsHumansAntineoplastic AgentsCarbocyaninesCytotoxinsIndolesMHI-148palbociclibPiperazinesPyridinesbreast cancerCDK4/6 inhibitor palbociclibcell cycle arrestMHI-148near-infrared fluorescent (NIRF)

Identifiers

PMID35164144
PMCPMC8840619
OpenAlexW4226069373

What OpenQuestion holds

Textmetadata
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.