Evidence mapPaperPMID 38847394Full record

ArticleeLife2024

Targeted protein degradation systems to enhance Wnt signaling.

Parthasarathy Sampathkumar, Heekyung Jung, Hui Chen, Zhengjian Zhang, Nicholas Suen, Yiran Yang, Zhong Huang, Tom Lopez, Robert Benisch, Sung-Jin Lee and 3 more

Abstract read
In one paragraph

Article in eLife, 2024. 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
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

3 citing papers in PubMed.

  1. Review
  2. Induced proximity at the cell surface.Nature biotechnology · 2025
    Review
  3. 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

13 authors.

Parthasarathy Sampathkumar *Surrozen, Inc, South San Francisco, United States.
Heekyung Jung *Surrozen, Inc, South San Francisco, United States.
Hui ChenSurrozen, Inc, South San Francisco, United States.
Zhengjian ZhangSurrozen, Inc, South San Francisco, United States.
Nicholas SuenSurrozen, Inc, South San Francisco, United States.ORCID https://orcid.org/0000-0002-6388-024X
Yiran YangSurrozen, Inc, South San Francisco, United States.
Zhong HuangSurrozen, Inc, South San Francisco, United States.
Tom LopezSurrozen, Inc, South San Francisco, United States.
Robert BenischSurrozen, Inc, South San Francisco, United States.ORCID https://orcid.org/0000-0002-0612-7606
Sung-Jin LeeSurrozen, Inc, South San Francisco, United States.
Jay YeSurrozen, Inc, South San Francisco, United States.
Wen-Chen YehSurrozen, Inc, South San Francisco, United States.
Yang LiSurrozen, Inc, South San Francisco, United States.ORCID https://orcid.org/0000-0002-7134-5685

Funding

User Training and OutreachP30GM124169 · NIGMS · UNIVERSITY OF CALIF-LAWRENC BERKELEY LAB · PI Gregory L Hura · 2017 to 2026
$28.6M
NIGMS NIH HHS P30 GM124169
6 · The paper itself

Abstract

Molecules that facilitate targeted protein degradation (TPD) offer great promise as novel therapeutics. The human hepatic lectin asialoglycoprotein receptor (ASGR) is selectively expressed on hepatocytes. We have previously engineered an anti-ASGR1 antibody-mutant RSPO2 (RSPO2RA) fusion protein (called SWEETS) to drive tissue-specific degradation of ZNRF3/RNF43 E3 ubiquitin ligases, which achieved hepatocyte-specific enhanced Wnt signaling, proliferation, and restored liver function in mouse models, and an antibody-RSPO2RA fusion molecule is currently in human clinical trials. In the current study, we identified two new ASGR1- and ASGR1/2-specific antibodies, 8M24 and 8G8. High-resolution crystal structures of ASGR1:8M24 and ASGR2:8G8 complexes revealed that these antibodies bind to distinct epitopes on opposing sides of ASGR, away from the substrate-binding site. Both antibodies enhanced Wnt activity when assembled as SWEETS molecules with RSPO2RA through specific effects sequestering E3 ligases. In addition, 8M24-RSPO2RA and 8G8-RSPO2RA efficiently downregulate ASGR1 through TPD mechanisms. These results demonstrate the possibility of combining different therapeutic effects and degradation mechanisms in a single molecule.

Indexed as

Asialoglycoprotein ReceptorProteolysisUbiquitin-Protein LigasesWnt Signaling PathwayAnimalsCrystallography, X-RayHepatocytesHumansIntercellular Signaling Peptides and ProteinsMiceRecombinant Fusion ProteinsR-SpondinsAsialoglycoprotein ReceptorIntercellular Signaling Peptides and ProteinsRecombinant Fusion ProteinsRNF43 protein, humanRspo2 protein, humanR-SpondinsUbiquitin-Protein LigasesZNRF3 protein, humanASGR1biochemistrychemical biologyLYTACnonePROTACregenerative medicineR-spondinstem cellsSWEETSWnt

Identifiers

PMID38847394
PMCPMC11161174

What Socratic 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 Socratic graph.