Evidence map›Paper›PMID 41099163›Full record

ArticleFuture medicinal chemistry2025

Aza-peptide aldehydes and ketones: synthesis and evaluation as human 20S proteasome inhibitors.

Thomas S Corrigan, Sarah E Border, Leilani M Lotti Diaz, Kayla Q Kasper, Abigail M Noonchester, Rasmiah Amer, Kayla S Kucway, Michael Fleisher, Joseph P Fernandez, Alex R Lovins and 6 more

Abstract read
In one paragraph

Article in Future medicinal chemistry, 2025. 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
–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

0 citing papers in PubMed.

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

16 authors.

Thomas S CorriganDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0000-0001-5113-9406
Sarah E BorderDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0000-0001-5739-3093
Leilani M Lotti DiazDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0000-0001-5955-9595
Kayla Q KasperDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0009-0004-7651-892X
Abigail M NoonchesterDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0009-0007-2302-635X
Rasmiah AmerDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0009-0000-7821-6520
Kayla S KucwayDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0009-0004-1078-1389
Michael FleisherDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0009-0009-1015-1551
Joseph P FernandezDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0000-0002-3744-3206
Alex R LovinsDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0009-0002-5850-1708
Ana K SerranoSkaggs School of Pharmacy and Pharmaceutical Sciences, Center for Discovery and Innovation in Parasitic Diseases, University of California San Diego, La Jolla, CA, USA.ORCID 0009-0006-8928-4135
Conor R CaffreySkaggs School of Pharmacy and Pharmaceutical Sciences, Center for Discovery and Innovation in Parasitic Diseases, University of California San Diego, La Jolla, CA, USA.ORCID 0000-0003-3048-8572
Anthony J O'DonoghueSkaggs School of Pharmacy and Pharmaceutical Sciences, Center for Discovery and Innovation in Parasitic Diseases, University of California San Diego, La Jolla, CA, USA.ORCID 0000-0001-5695-0409
Don M BensonDepartment of Internal Medicine, Division of Hematology, The Ohio State University Medical Center, Columbus, OH, USA.ORCID 0000-0001-8837-0548
Christopher M HadadDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0000-0003-1211-4315
Özlem Doğan EkiciDepartment of Chemistry and Biochemistry, The Ohio State University, Columbus, OH, USA.ORCID 0000-0002-1237-1269

Funding

Proteasome inhibitors against mucosal protozoan pathogensR01AI158612 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI ECKMANN, LARS, O'DONOGHUE, ANTHONY JOHN · 2021 to 2025
$3.2M
The catalytic core of the proteasome as a drug target to treat Human African TrypanosomiasisR21AI171824 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI CAFFREY, CONOR, O'DONOGHUE, ANTHONY JOHN · 2022 to 2023
$435k
NIAID NIH HHS R01 AI158612NIAID NIH HHS R21 AI171824
6 · The paper itself

Abstract

aimsAza-peptide aldehydes and ketones were developed as a new class of peptidyl analogues to inhibit the human constitutive (c)20S proteasome as alternative therapeutics to treat multiple myeloma (MM). MATERIAL AND

methodsEleven new aza-peptide aldehydes and ketones were designed based on their preference to bind at the ß5 catalytic subunit of c20S proteasome with benzyloxycarbonyl(Cbz)-Leu-Leu-Leu (MG132-like) and morpholinyl(Mp)-Homophenylalanyl(HPh)-Leu-Phe-Leu (Carfilzomib-like) sequences, synthesized, structurally characterized and evaluated for their inhibitory potency in competitive kinetic assays in vitro. Additionally, cell viability assays and molecular modeling experiments were designed and performed in support.

resultsAza-peptide aldehydes and ketones generated inhibitory activity with IC

conclusionsOverall, aza-peptide aldehydes and ketones are a new class of selective human c20S proteasome inhibitors with the potential for further development as alternative therapeutics for multiple myeloma.

Indexed as

Antineoplastic AgentsProteasome InhibitorsAldehydesAza CompoundsCell LineCell SurvivalDrug Screening Assays, AntitumorKetonesMolecular StructureMultiple MyelomaPeptidesAldehydesAntineoplastic AgentsAza CompoundsKetonesPeptidesProteasome Inhibitorsanticanceraza-peptide aldehydesaza-peptide ketonesmultiple myelomaProteasome inhibitor

Identifiers

PMID41099163
PMCPMC12536793

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.