000304282 001__ 304282 000304282 005__ 20251107154044.0 000304282 0247_ $$2doi$$a10.1016/j.ymthe.2025.08.031 000304282 0247_ $$2pmid$$apmid:40886048 000304282 0247_ $$2ISSN$$a1525-0016 000304282 0247_ $$2ISSN$$a1525-0024 000304282 0247_ $$2altmetric$$aaltmetric:180771333 000304282 037__ $$aDKFZ-2025-01822 000304282 041__ $$aEnglish 000304282 082__ $$a610 000304282 1001_ $$aUllrich, Timo$$b0 000304282 245__ $$aTuning of G-CSFR signaling by de novo designed agonists. 000304282 260__ $$aAmsterdam$$bElsevier$$c2025 000304282 3367_ $$2DRIVER$$aarticle 000304282 3367_ $$2DataCite$$aOutput Types/Journal article 000304282 3367_ $$0PUB:(DE-HGF)16$$2PUB:(DE-HGF)$$aJournal Article$$bjournal$$mjournal$$s1762526417_1834969 000304282 3367_ $$2BibTeX$$aARTICLE 000304282 3367_ $$2ORCID$$aJOURNAL_ARTICLE 000304282 3367_ $$00$$2EndNote$$aJournal Article 000304282 500__ $$a2025 Nov 5;33(11):5741-5759 000304282 520__ $$aEnhancing cytokine-based therapies by systematically tuning how an agonist associates its receptor is emerging as a powerful new concept in drug discovery. Here, we report the design and characterization of agonists that tune the granulocyte-colony stimulating factor receptor (G-CSFR) activity, which is central for the proliferation and granulocytic differentiation of hematopoietic stem cells. Using design agonists, we study the impact of varying the receptor-binding affinity and dimerization geometry on receptor association, downstream signaling, and cellular response. Hence, we achieved agonists with altered signaling specificities that are hyper-thermostable, can outcompete the native ligand (G-CSF), and bias cells toward granulopoietic differentiation over triggering proliferation. Furthermore, the design agonists differentially modulate the kinetics and amplitudes of signal transduction pathways, and gene expression patterns. In contrast to G-CSF, they achieve more selective activation of gene sets with hematopoietic functions with minimal unwanted effects on immunomodulatory signaling. These findings demonstrate the potential of dissecting the complex G-CSFR signaling, and open up ways for new therapeutic applications for designed cytokines. 000304282 536__ $$0G:(DE-HGF)POF4-899$$a899 - ohne Topic (POF4-899)$$cPOF4-899$$fPOF IV$$x0 000304282 588__ $$aDataset connected to CrossRef, PubMed, , Journals: inrepo02.dkfz.de 000304282 7001_ $$aPollmann, Christoph$$b1 000304282 7001_ $$aRitter, Malte$$b2 000304282 7001_ $$aHaaf, Jérémy$$b3 000304282 7001_ $$aAghaallaei, Narges$$b4 000304282 7001_ $$aTesakov, Ivan$$b5 000304282 7001_ $$aHatskovska, Valeriia$$b6 000304282 7001_ $$aEl-Riz, Maya$$b7 000304282 7001_ $$aMaksymenko, Kateryna$$b8 000304282 7001_ $$aKandabarau, Sergey$$b9 000304282 7001_ $$aKlimiankou, Maksim$$b10 000304282 7001_ $$0P:(DE-HGF)0$$aLengerke, Claudia$$b11 000304282 7001_ $$aWelte, Karl$$b12 000304282 7001_ $$aHernandez-Alvarez, Birte$$b13 000304282 7001_ $$aMüller, Patrick$$b14 000304282 7001_ $$aLupas, Andrei$$b15 000304282 7001_ $$aPiehler, Jacob$$b16 000304282 7001_ $$aSkokowa, Julia$$b17 000304282 7001_ $$aElGamacy, Mohammad$$b18 000304282 773__ $$0PERI:(DE-600)2001818-6$$a10.1016/j.ymthe.2025.08.031$$gp. 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