Evidence map›Paper›PMID 37238630›Full record

ArticleBiomolecules2023

Homogeneous, Synthetic, Non-Saccharide Glycosaminoglycan Mimetics as Potent Inhibitors of Human Cathepsin G.

Daniel K Afosah, Rawan M Fayyad, Valerie R Puliafico, Spencer Merrell, Eltice K Langmia, Sophie R Diagne, Rami A Al-Horani, Umesh R Desai

Open access · goldAbstract read
In one paragraph

Article in Biomolecules, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.0field-weighted citation impact, top 22% 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

3 citing papers in PubMed, 4 citations in OpenAlex.

  1. Article
  2. Article
  3. Substituted 4H-3,1-benzoxazine-4-one Derivatives as Inhibitors of Cathepsin G.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2024
    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

8 authors at 3 institutions in 1 country.

Daniel K AfosahDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA.ORCID 0000-0001-5675-1127
Rawan M FayyadDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA.
Valerie R PuliaficoDepartment of Chemistry and Biochemistry, Washington and Lee University, Lexington, VA 24450, USA.
Spencer MerrellDepartment of Chemistry and Biochemistry, Washington and Lee University, Lexington, VA 24450, USA.
Eltice K LangmiaDepartment of Chemistry and Biochemistry, Washington and Lee University, Lexington, VA 24450, USA.
Sophie R DiagneDepartment of Chemistry, Virginia Commonwealth University, Richmond, VA 23298, USA.
Rami A Al-HoraniDivision of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA.ORCID 0000-0001-9146-2662
Umesh R DesaiDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA.ORCID 0000-0002-1976-6597
Virginia Commonwealth University · USWashington and Lee University · USXavier University of Louisiana · US

Funding

Project 3: Role of Glycosaminoglycans in HematopoiesisP01HL151333 · NHLBI · VERSITI WISCONSIN, INC. · PI LAU, JOSEPH TY · 2021 to 2025
$12.3M
Lead identification and pre-clinical studies on allosteric inhibitors of coagulation factor XIaR61HL161813 · NHLBI · VIRGINIA COMMONWEALTH UNIVERSITY · PI DESAI, UMESH RAMANLAL · 2022 to 2023
$1.1M
Lead identification and pre-clinical studies on allosteric inhibitors of coagulation factor XIaR33HL161813 · NHLBI · VIRGINIA COMMONWEALTH UNIVERSITY · PI DESAI, UMESH RAMANLAL · 2024 to 2024
$489k
Synthetic glycosaminoglycan mimetics as regulators of megakaryopoiesis and thrombopoiesisK99HL161423 · NHLBI · VIRGINIA COMMONWEALTH UNIVERSITY · PI AFOSAH, DANIEL KWAME · 2022 to 2023
$359k
NHLBI NIH HHS K99 HL161423NHLBI NIH HHS P01 HL151333NHLBI NIH HHS R33 HL161813NHLBI NIH HHS R61 HL161813NIH HHS K99 HL161423NIH HHS P01 HL151333NIH HHS R61 HL161813
6 · The paper itself

Abstract

Cathepsin G (CatG) is a pro-inflammatory neutrophil serine protease that is important for host defense, and has been implicated in several inflammatory disorders. Hence, inhibition of CatG holds much therapeutic potential; however, only a few inhibitors have been identified to date, and none have reached clinical trials. Of these, heparin is a well-known inhibitor of CatG, but its heterogeneity and bleeding risk reduce its clinical potential. We reasoned that synthetic small mimetics of heparin, labeled as non-saccharide glycosaminoglycan mimetics (NSGMs), would exhibit potent CatG inhibition while being devoid of bleeding risks associated with heparin. Hence, we screened a focused library of 30 NSGMs for CatG inhibition using a chromogenic substrate hydrolysis assay and identified nano- to micro-molar inhibitors with varying levels of efficacy. Of these, a structurally-defined, octasulfated di-quercetin NSGM

Indexed as

Cathepsin GGlycosaminoglycansHeparinEndopeptidasesHumansPeptide HydrolasesCathepsin GEndopeptidasesGlycosaminoglycansHeparinPeptide Hydrolasesallosterismcathepsin Gglycosaminoglycansinflammationmimetics

Identifiers

PMID37238630
PMCPMC10216581
OpenAlexW4367315452

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.