Evidence map›Paper›PMID 32410451›Full record

ArticleJournal of medicinal chemistry2020

A Platinum(IV) Prodrug-Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain.

Colin M Fadzen, Justin M Wolfe, Wen Zhou, Choi-Fong Cho, Niklas von Spreckelsen, Kathryn T Hutchinson, Yen-Chun Lee, E Antonio Chiocca, Sean E Lawler, Omer H Yilmaz and 2 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.8field-weighted citation impact, top 14% 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

13 citing papers in PubMed, 38 citations in OpenAlex.

  1. Article
  2. Peptide Multifunctionalization via Modular Construction of Trans-ABAdvanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025
    Article
  3. Article
  4. Article
  5. Article
  6. Review
  7. Article
  8. A Pt(IV)-conjugated brain penetrant macrocyclic peptide shows pre-clinical efficacy in glioblastoma.Journal of controlled release : official journal of the Controlled Release Society · 2022
    Article
  9. Article
  10. Review
  11. Review
  12. Article
  13. 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

12 authors at 2 institutions in 2 countries.

Colin M FadzenDepartment of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.ORCID 0000-0002-4139-9578
Justin M WolfeDepartment of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.ORCID 0000-0002-1003-6045
Wen ZhouDepartment of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.ORCID 0000-0001-8455-6011
Choi-Fong ChoHarvey Cushing Neuro-Oncology Laboratories, Department of Neurosurgery, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, United States.
Niklas von SpreckelsenHarvey Cushing Neuro-Oncology Laboratories, Department of Neurosurgery, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, United States.ORCID 0000-0002-9873-1711
Kathryn T HutchinsonHarvey Cushing Neuro-Oncology Laboratories, Department of Neurosurgery, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, United States.
Yen-Chun LeeDepartment of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.
E Antonio ChioccaHarvey Cushing Neuro-Oncology Laboratories, Department of Neurosurgery, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, United States.
Sean E LawlerHarvey Cushing Neuro-Oncology Laboratories, Department of Neurosurgery, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, United States.
Omer H YilmazThe Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.
Stephen J LippardDepartment of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.ORCID 0000-0002-2693-4982
Bradley L PenteluteDepartment of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.ORCID 0000-0002-7242-801X
Massachusetts Institute of Technology · USBrigham and Women's Hospital · US

Funding

VIRUS PRODUCTION COREP30CA014051 · NCI · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI Andreea O'Connell · 1985 to 2026
$93.9M
Understanding and Improving Platinum Anticancer DrugsR01CA034992 · NCI · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI YILMAZ, OMER · 1985 to 2018
$6.8M
CHEMISTRY AND BIOLOGY OF PLATINUM ANTICANCER DRUGSR37CA034992 · NCI · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI LIPPARD, STEPHEN J. · 1990 to 2008
$5.7M
Fluorinated macrocyclic peptides as BBB penetrating agent for improved GBM treatmentR01CA237063 · NCI · BROWN UNIVERSITY · PI LAWLER, SEAN EDWARD, PENTELUTE, BRADLEY LETHER · 2019 to 2023
$3.0M
Impact of fasting on intestinal stem cells and cancerR01CA245314 · NCI · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI Omer Yilmaz · 2020 to 2026
$2.3M
Dietary control of stem cells in physiology and cancerR01CA211184 · NCI · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI YILMAZ, OMER · 2017 to 2021
$2.0M
Cysteine ArylationR01GM110535 · NIGMS · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI PENTELUTE, BRADLEY LETHER · 2014 to 2018
$1.5M
Regulation of the Intestinal Stem Cell Niche in AgingR00AG045144 · NIA · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI YILMAZ, OMER · 2014 to 2016
$740k
Regulation of the Intestinal Stem Cell Niche in AgingK99AG045144 · NIA · WHITEHEAD INSTITUTE FOR BIOMEDICAL RES · PI YILMAZ, OMER · 2013 to 2014
$275k
Chemically Modified Peptide Agents for Next-Generation Conjugate Therapies to Treat Duchenne Muscular DystrophyF30HD093358 · NICHD · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI FADZEN, COLIN MACLAINE · 2017 to 2019
$142k
NCI NIH HHS P30 CA014051NCI NIH HHS R01 CA034992NCI NIH HHS R01 CA211184NCI NIH HHS R01 CA237063NCI NIH HHS R01 CA245314NCI NIH HHS R37 CA034992NIA NIH HHS K99 AG045144NIA NIH HHS R00 AG045144NICHD NIH HHS F30 HD093358NIGMS NIH HHS R01 GM110535
6 · The paper itself

Abstract

Effective delivery to the brain limits the development of novel glioblastoma therapies. Here, we introduce conjugation between platinum(IV) prodrugs of cisplatin and perfluoroaryl peptide macrocycles to increase brain uptake. We demonstrate that one such conjugate shows efficacy against glioma stem-like cells. We investigate the pharmacokinetics of this conjugate in mice and show that the amount of platinum in the brain after treatment with the conjugate is 15-fold greater than with cisplatin after 5 h.

Indexed as

Biological TransportBrainCell LineHumansMacrocyclic CompoundsPeptidesPlatinumProdrugsMacrocyclic CompoundsPeptidesPlatinumProdrugs

Identifiers

PMID32410451
PMCPMC7992430
OpenAlexW3024615820

What OpenQuestion holds

Textmetadata
LicenceTDM
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.