Evidence map›Paper›PMID 36841432›Full record

ArticleSLAS discovery : advancing life sciences R & D2023

Fragment-based drug discovery of small molecule ligands for the human chemokine CCL28.

Angela L Zhou, Davin R Jensen, Francis C Peterson, Monica A Thomas, Roman R Schlimgen, Michael B Dwinell, Brian C Smith, Brian F Volkman

Open access · diamondAbstract read
In one paragraph

Article in SLAS discovery : advancing life sciences R & D, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.8field-weighted citation impact, top 28% 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

2 citing papers in PubMed, 5 citations in OpenAlex.

  1. Article
  2. 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 1 institution in 1 country.

Angela L ZhouDepartment of Biochemistry, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.
Davin R JensenDepartment of Biochemistry, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA; Program in Chemical Biology, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.
Francis C PetersonDepartment of Biochemistry, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA; Program in Chemical Biology, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.
Monica A ThomasDepartment of Biochemistry, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.
Roman R SchlimgenDepartment of Biochemistry, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.
Michael B DwinellDepartment of Microbiology and Immunology, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA; Center for Immunology, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.
Brian C SmithDepartment of Biochemistry, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA; Program in Chemical Biology, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.
Brian F VolkmanDepartment of Biochemistry, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA; Program in Chemical Biology, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA; Center for Immunology, Medical College of Wisconsin 8701 Watertown Plank Road, Milwaukee, WI 53226, USA. Electronic address: bvolkman@mcw.edu.
Medical College of Wisconsin · US

Funding

Medical Scientist Training ProgramT32GM080202 · NIGMS · MEDICAL COLLEGE OF WISCONSIN · PI BARBIERI, JOSEPH T, SALZMAN, NITA H · 2010 to 2024
$5.7M
Structural Basis for Chemokine FunctionR37AI058072 · NIAID · MEDICAL COLLEGE OF WISCONSIN · PI Brian F Volkman · 2020 to 2026
$2.8M
Discovering and Exploiting Selectivity within Tandem BromodomainsR35GM128840 · NIGMS · MEDICAL COLLEGE OF WISCONSIN · PI Brian Christopher Smith · 2018 to 2026
$2.7M
Structure-based inhibition of chemokine signaling in the inflamed pancreasR01DK133247 · NIDDK · MEDICAL COLLEGE OF WISCONSIN · PI Michael B Dwinell, Brian F Volkman · 2023 to 2026
$2.5M
Targeting CCL28 as therapy for obstructive lung diseaseR01AI120655 · NIAID · MEDICAL COLLEGE OF WISCONSIN · PI VOLKMAN, BRIAN F · 2015 to 2018
$1.5M
High Performance Digital Console and Sample JetS10OD020000 · OD · MEDICAL COLLEGE OF WISCONSIN · PI VOLKMAN, BRIAN F · 2015 to 2015
$600k
Evolution of fold-switching in the metamorphic chemokine XCL1R56AI155881 · NIAID · MEDICAL COLLEGE OF WISCONSIN · PI VOLKMAN, BRIAN F · 2021 to 2021
$390k
Validating CCL28 as a Target for Novel Asthma Therapies using NMR SpectroscopyF30HL134253 · NHLBI · MEDICAL COLLEGE OF WISCONSIN · PI THOMAS, MONICA A · 2017 to 2019
$140k
NHLBI NIH HHS F30 HL134253NIAID NIH HHS R01 AI120655NIAID NIH HHS R37 AI058072NIAID NIH HHS R56 AI155881NIDDK NIH HHS R01 DK133247NIGMS NIH HHS R35 GM128840NIGMS NIH HHS T32 GM080202NIH HHS S10 OD020000
6 · The paper itself

Abstract

The mucosal chemokine CCL28 is a promising target for immunotherapy drug development due to its elevated expression level in epithelial cells and critical role in creating and maintaining an immunosuppressive tumor microenvironment. Using sulfotyrosine as a probe, NMR chemical shift mapping identified a potential receptor-binding hotspot on the human CCL28 surface. CCL28 was screened against 2,678 commercially available chemical fragments by 2D NMR, yielding thirteen verified hits. Computational docking predicted that two fragments could occupy adjoining subsites within the sulfotyrosine recognition cleft. Dual NMR titrations confirmed their ability to bind CCL28 simultaneously, thereby validating an initial fragment pair for linking and merging strategies to design high-potency CCL28 inhibitors.

Indexed as

ChemokinesChemokines, CCDrug DiscoveryEpithelial CellsHumansLigandsCCL28 protein, humanChemokinesChemokines, CCLigandsCCL28ChemokineDrug discoveryFragmentNMRSulfotyrosine

Identifiers

PMID36841432
PMCPMC10339762
OpenAlexW4321602259

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.