ArticleArchiv der Pharmazie2025
Design, Synthesis, and Molecular Evaluation of S
Larissa N Ernst, Jason Stahlecker, Finn Mier, Ricardo A M Serafim, Valentin R Wydra, Benedikt Masberg, Simon J Jaag, Cornelius Knappe, Michael Lämmerhofer, Thilo Stehle and 2 more
Abstract read
In one paragraphArticle in Archiv der Pharmazie, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
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 registryThe 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 literatureWho cites it
0 citing papers in PubMed.
No citing paper in PubMed yet.
4 · The recordCorrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
5 · Who and what moneyAuthors and funding
12 authors.
Larissa N ErnstDepartment of Pharmacy and Biochemistry, Laboratory for Molecular Design & Pharmaceutical Biophysics, Institute of Pharmaceutical Sciences, Eberhard Karls Universität Tübingen, Tübingen, Germany.ORCID https://orcid.org/0000-0003-0014-4496 Jason StahleckerDepartment of Pharmacy and Biochemistry, Laboratory for Molecular Design & Pharmaceutical Biophysics, Institute of Pharmaceutical Sciences, Eberhard Karls Universität Tübingen, Tübingen, Germany.ORCID https://orcid.org/0000-0002-0044-4037 Finn MierDepartment of Pharmacy and Biochemistry, Laboratory for Molecular Design & Pharmaceutical Biophysics, Institute of Pharmaceutical Sciences, Eberhard Karls Universität Tübingen, Tübingen, Germany.ORCID https://orcid.org/0000-0003-3409-4626 Benedikt MasbergDepartment of Pharmacy and Biochemistry, Pharmaceutical (Bio-)Analysis, Institute of Pharmaceutical Sciences, Eberhard Karls Universität, Tübingen, Germany.ORCID https://orcid.org/0000-0003-2041-4983 Cornelius KnappeDepartment of Pharmacy and Biochemistry, Pharmaceutical (Bio-)Analysis, Institute of Pharmaceutical Sciences, Eberhard Karls Universität, Tübingen, Germany.ORCID https://orcid.org/0009-0009-4080-4410 Michael LämmerhoferDepartment of Pharmacy and Biochemistry, Pharmaceutical (Bio-)Analysis, Institute of Pharmaceutical Sciences, Eberhard Karls Universität, Tübingen, Germany.ORCID https://orcid.org/0000-0002-1318-0974 Frank M BoecklerDepartment of Pharmacy and Biochemistry, Laboratory for Molecular Design & Pharmaceutical Biophysics, Institute of Pharmaceutical Sciences, Eberhard Karls Universität Tübingen, Tübingen, Germany.ORCID https://orcid.org/0000-0001-8738-6716 Funding
M.G. gratefully acknowledges the Deutsche Forschungsgemeinschaft (DFG, German Research Foundation) under Germany's excellence strategy - EXC 2180 - 390900677 [Image Guided and Functionally Instructed Tumor Therapies' (iFIT)] and the Deutsche Forschungsgemeinschaft (DFG, German Research Foundation) - Project number 511101075 for funding. Funding by the Deutsche Krebshilfe (German Cancer Aid) - Dr. Mildred Scheel Stiftung für Krebsforschung is gratefully acknowledged by R.A.M.S. and M.G. The authors acknowledge support from the state of Baden-Württemberg through bwHPC and the German Research Foundation (DFG) through Grant No. INST 40/575-1 FUGG (JUSTUS 2 cluster). In addition, the authors acknowledge support by the High Performance and Cloud Computing Group at the Zentrum für Datenverarbeitung of the University of Tübingen, the state of Baden-Württemberg through bwHPC, and the German Research Foundation (DFG) through grant no. INST 37/935-1 FUGG (BinAC cluster).
6 · The paper itselfAbstract
The cysteine protease ubiquitin-specific protease 7 (USP7), also known as herpes-associated ubiquitin-specific protease (HAUSP), has gained increasing attention in recent years due to its proven overexpression in several cancer types and its role in tumorigenesis. Herein, after a design based on molecular docking experiments, we report the synthesis of a series of mildly electrophilic compounds that covalently modify the catalytic cysteine 223 in USP7 through a nucleophilic aromatic substitution (S
Indexed as
Drug DesignIsoquinolinesUbiquitin-Specific Peptidase 7Dose-Response Relationship, DrugHumansMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipIsoquinolinesUbiquitin-Specific Peptidase 7USP7 protein, humancovalent inhibitordifferential scanning fluorimetry (DSF)intact protein mass spectrometryUSP7X‐ray crystallography
Identifiers
PMID40785232
PMCPMC12336439
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