% IMPORTANT: The following is UTF-8 encoded. This means that in the presence % of non-ASCII characters, it will not work with BibTeX 0.99 or older. % Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or % “biber”. @ARTICLE{Ullrich:304282, author = {T. Ullrich and C. Pollmann and M. Ritter and J. Haaf and N. Aghaallaei and I. Tesakov and V. Hatskovska and M. El-Riz and K. Maksymenko and S. Kandabarau and M. Klimiankou and C. Lengerke$^*$ and K. Welte and B. Hernandez-Alvarez and P. Müller and A. Lupas and J. Piehler and J. Skokowa and M. ElGamacy}, title = {{T}uning of {G}-{CSFR} signaling by de novo designed agonists.}, journal = {Molecular therapy}, volume = {nn}, issn = {1525-0016}, address = {Amsterdam}, publisher = {Elsevier}, reportid = {DKFZ-2025-01822}, pages = {nn}, year = {2025}, note = {epub}, abstract = {Enhancing 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.}, cin = {TU01}, ddc = {610}, cid = {I:(DE-He78)TU01-20160331}, pnm = {899 - ohne Topic (POF4-899)}, pid = {G:(DE-HGF)POF4-899}, typ = {PUB:(DE-HGF)16}, pubmed = {pmid:40886048}, doi = {10.1016/j.ymthe.2025.08.031}, url = {https://inrepo02.dkfz.de/record/304282}, }