Evidence map›Paper›PMID 38628795›Full record

ArticleACS medicinal chemistry letters2024

Macrocyclic Oxindole Peptide Epoxyketones-A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome.

Marion G Götz, Kacey Godwin, Rachel Price, Robert Dorn, Gabriel Merrill-Steskal, William Klemmer, Hunter Hansen, Gautam Produturi, Megan Rocha, Mathias Palmer and 3 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS medicinal chemistry letters, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.7field-weighted citation impact, top 32% 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

0 citing papers in PubMed, 3 citations in OpenAlex.

No citing paper in PubMed yet.

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

13 authors at 2 institutions in 2 countries.

Marion G GötzDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.ORCID https://orcid.org/0000-0003-4831-0537
Kacey GodwinDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Rachel PriceDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Robert DornDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Gabriel Merrill-SteskalDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
William KlemmerDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Hunter HansenDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Gautam ProduturiDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Megan RochaDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Mathias PalmerDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Lea MolacekDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Zack StraterDepartment of Chemistry, Whitman College, Walla Walla, Washington 99362, United States.
Michael GrollTechnical University of Munich, TUM School of Natural Sciences, Department of Bioscience, Center for Protein Assemblies (CPA), Ernst-Otto-Fischer Strasse 8, 85748 Garching, Germany.ORCID https://orcid.org/0000-0002-1660-340X
Whitman College · USTechnical University of Munich · DE

Funding

TMC-95 derived peptide macrocycles as inhibitors of the proteasomeR15GM113198 · NIGMS · WHITMAN COLLEGE · PI GOTZ, MARION GABRIELE · 2015 to 2015
$261k
NIGMS NIH HHS R15 GM113198
6 · The paper itself

Abstract

Peptide macrocycles have recently gained attention as protease inhibitors due to their metabolic stability and specificity. However, the development of peptide macrocycles with improved binding potency has so far been challenging. Here we present macrocyclic peptides derived from the clinically applied proteasome inhibitor carfilzomib with an oxindole group that mimics the natural product TMC-95A. Fluorescence kinetic activity assays reveal a high potency of the oxindole group (IC

Identifiers

PMID38628795
PMCPMC11017298
OpenAlexW4393233387

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.