Evidence map›Paper›PMID 39312747›Full record

ArticleACS chemical biology2024

Next Generation SICLOPPS Screening for the Identification of Inhibitors of the HIF-1α/HIF-1β Protein-Protein Interaction.

Alexander McDermott, Leonie M Windeln, Jacob S D Valentine, Leonardo Baldassarre, Andrew D Foster, Ali Tavassoli

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Article in ACS chemical biology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

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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

6 citing papers in PubMed.

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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

6 authors.

Alexander McDermottSchool of Chemistry, University of Southampton, Southampton SO17 1BJ, U.K.
Leonie M WindelnSchool of Chemistry, University of Southampton, Southampton SO17 1BJ, U.K.
Jacob S D ValentineSchool of Chemistry, University of Southampton, Southampton SO17 1BJ, U.K.
Leonardo BaldassarreCurve Therapeutics, Delta House, Southampton Science Park, Southampton SO16 7NS, U.K.
Andrew D FosterSchool of Chemistry, University of Southampton, Southampton SO17 1BJ, U.K.
Ali TavassoliSchool of Chemistry, University of Southampton, Southampton SO17 1BJ, U.K.ORCID 0000-0002-7420-5063

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Split-intein circular ligation of proteins and peptides (SICLOPPS) is a method for generating intracellular libraries of cyclic peptides that has yielded several first-in-class inhibitors. Here, we detail a revised high-content, high-throughput SICLOPPS screening protocol that utilizes next-generation sequencing, biopanning, and computational tools to identify hits against a given protein-protein interaction. We used this platform for the identification of inhibitors of the HIF-1α/HIF-1β protein-protein interaction. The revised platform resulted in a significantly higher positive hit rate than that previously reported for SICLOPPS screens, and the identified cyclic peptides were more active in vitro and in cells than our previously reported inhibitors. The platform detailed here may be used for the identification of inhibitors of a wide range of other targets.

Indexed as

Hypoxia-Inducible Factor 1, alpha SubunitPeptides, CyclicAryl Hydrocarbon Receptor Nuclear TranslocatorHigh-Throughput Screening AssaysHumansPeptide LibraryProtein BindingARNT protein, humanAryl Hydrocarbon Receptor Nuclear TranslocatorHIF1A protein, humanHypoxia-Inducible Factor 1, alpha SubunitPeptide LibraryPeptides, Cyclic

Identifiers

PMID39312747
PMCPMC11494503

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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.