Evidence map›Paper›PMID 34288674›Full record

ArticleJournal of medicinal chemistry2021

Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.

Linfeng Li, Bala C Chenna, Kai S Yang, Taylor R Cole, Zachary T Goodall, Miriam Giardini, Zahra Moghadamchargari, Elizabeth A Hernandez, Jana Gomez, Claudia M Calvet and 14 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
4.2field-weighted citation impact, top 5% 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

19 citing papers in PubMed, 32 citations in OpenAlex.

  1. α-C(spOrganic letters · 2026
    Article
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  7. Review
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  9. Review
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  11. PRSC chemical biology · 2023
    Review
  12. Article
  13. Advances in research on 3C-like protease (3CLRSC medicinal chemistry · 2023
    Review
  14. Article
  15. Review
  16. Article
  17. Article
  18. Insights into the structural properties of SARS-CoV-2 main protease.Current research in structural biology · 2022
    Article
  19. 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

24 authors at 3 institutions in 1 country.

Linfeng LiDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.ORCID 0000-0001-6185-4999
Bala C ChennaDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.ORCID 0000-0002-2660-5302
Kai S YangDepartment of Chemistry, Texas A&M University, 580 Ross Street, College Station, Texas 77843, United States.ORCID 0000-0002-1890-4169
Taylor R ColeDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
Zachary T GoodallDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
Miriam GiardiniSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Dr, La Jolla, California 92093, United States.
Zahra MoghadamchargariDepartment of Chemistry, Texas A&M University, 580 Ross Street, College Station, Texas 77843, United States.
Elizabeth A HernandezDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
Jana GomezDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
Claudia M CalvetSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Dr, La Jolla, California 92093, United States.
Jean A BernatchezSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Dr, La Jolla, California 92093, United States.ORCID 0000-0002-8309-1627
Drake M MellottDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.ORCID 0000-0002-8043-8170
Jiyun ZhuDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
Andrew RademacherDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
Diane ThomasSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Dr, La Jolla, California 92093, United States.
Lauren R BlankenshipDepartment of Chemistry, Texas A&M University, 580 Ross Street, College Station, Texas 77843, United States.
Aleksandra DrelichDepartment of Microbiology and Immunology, University of Texas Medical Branch, 301 University Blvd, Galveston, Texas 77555, United States.
Arthur LaganowskyDepartment of Chemistry, Texas A&M University, 580 Ross Street, College Station, Texas 77843, United States.ORCID 0000-0001-5012-5547
Chien-Te K TsengDepartment of Microbiology and Immunology, University of Texas Medical Branch, 301 University Blvd, Galveston, Texas 77555, United States.
Wenshe R LiuDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
A Joshua WandDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.ORCID 0000-0001-8341-0782
Jorge Cruz-ReyesDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.
Jair L Siqueira-NetoSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Dr, La Jolla, California 92093, United States.ORCID 0000-0001-9574-8174
Thomas D MeekDepartment of Biochemistry and Biophysics, Texas A&M University, 300 Olsen Blvd, College Station, Texas 77843, United States.ORCID 0000-0002-1931-8073
Texas A&M University · USUniversity of California San Diego · USThe University of Texas Medical Branch at Galveston · US

Funding

The role of the free energy landscape in Parkin's function and dysfunction in health and diseaseR01GM129076 · NIGMS · TEXAS A&M AGRILIFE RESEARCH · PI WAND, A. JOSHUA · 2020 to 2023
$1.6M
SELF-MASKED ALDEHYDES AS INHIBITORS OF THE CYSTEINE PROTEASES 3CL PROTEASE, CATHEPSIN L, AND CRUZAINR21AI166624 · NIAID · TEXAS A&M AGRILIFE RESEARCH · PI MEEK, THOMAS · 2022 to 2023
$430k
Novel Inhibitors of Cruzain and Trypanosoma brucei Cathpesin B as Potential Drug Candidates for the Treatment of African Trypanosomiasis and Chagas DiseaseR21AI127634 · NIAID · TEXAS A&M AGRILIFE RESEARCH · PI MEEK, THOMAS · 2017 to 2018
$396k
NIAID NIH HHS R21 AI127634NIAID NIH HHS R21 AI166624NIGMS NIH HHS R01 GM129076
6 · The paper itself

Abstract

Cysteine proteases comprise an important class of drug targets, especially for infectious diseases such as Chagas disease (cruzain) and COVID-19 (3CL protease, cathepsin L). Peptide aldehydes have proven to be potent inhibitors for all of these proteases. However, the intrinsic, high electrophilicity of the aldehyde group is associated with safety concerns and metabolic instability, limiting the use of aldehyde inhibitors as drugs. We have developed a novel class of self-masked aldehyde inhibitors (SMAIs) for cruzain, the major cysteine protease of the causative agent of Chagas disease-

Indexed as

COVID-19 Drug TreatmentAldehydesCathepsin LChagas DiseaseCysteine EndopeptidasesCysteine ProteasesCysteine Proteinase InhibitorsDrug DesignHumansKineticsModels, MolecularMolecular StructureProtozoan ProteinsSARS-CoV-2Structure-Activity RelationshipTrypanosoma cruziAldehydesCathepsin LcruzipainCysteine EndopeptidasesCysteine ProteasesCysteine Proteinase InhibitorsProtozoan Proteins

Identifiers

PMID34288674
PMCPMC10504874
OpenAlexW3184905337

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.