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@ARTICLE{Rettie:1051977,
author = {Rettie, Stephen A. and Juergens, David and Adebomi, Victor
and Bueso, Yensi Flores and Zhao, Qinqin and Leveille,
Alexandria N. and Liu, Andi and Bera, Asim K. and Wilms,
Joana A. and Üffing, Alina and Kang, Alex and
Brackenbrough, Evans and Lamb, Mila and Gerben, Stacey R.
and Murray, Analisa and Levine, Paul M. and Schneider, Maika
and Vasireddy, Vibha and Ovchinnikov, Sergey and
Weiergräber, Oliver H. and Willbold, Dieter and Kritzer,
Joshua A. and Mougous, Joseph D. and Baker, David and
DiMaio, Frank and Bhardwaj, Gaurav},
title = {{A}ccurate de novo design of high-affinity protein-binding
macrocycles using deep learning},
journal = {Nature chemical biology},
volume = {21},
number = {12},
issn = {1552-4450},
address = {Basingstoke},
publisher = {Nature Publishing Group},
reportid = {FZJ-2026-00658},
pages = {1948 - 1956},
year = {2025},
abstract = {Developing macrocyclic binders to therapeutic proteins
typically relies on large-scale screening methods that are
resource intensive and provide little control over binding
mode. Despite progress in protein design, there are
currently no robust approaches for de novo design of
protein-binding macrocycles. Here we introduce RFpeptides, a
denoising diffusion-based pipeline for designing macrocyclic
binders against protein targets of interest. We tested 20 or
fewer designed macrocycles against each of four diverse
proteins and obtained binders with medium to high affinity
against all targets. For one of the targets, Rhombotarget A
(RbtA), we designed a high-affinity binder
(Kd < 10 nM) despite starting from the predicted
target structure. X-ray structures for macrocycle-bound
myeloid cell leukemia 1, γ-aminobutyric acid type A
receptor-associated protein and RbtA complexes match closely
with the computational models, with a Cα root-mean-square
deviation < 1.5 Å to the design models. RFpeptides
provides a framework for rapid and custom design of
macrocyclic peptides for diagnostic and therapeutic
applications.},
cin = {IBI-7},
ddc = {570},
cid = {I:(DE-Juel1)IBI-7-20200312},
pnm = {5241 - Molecular Information Processing in Cellular Systems
(POF4-524)},
pid = {G:(DE-HGF)POF4-5241},
typ = {PUB:(DE-HGF)16},
doi = {10.1038/s41589-025-01929-w},
url = {https://juser.fz-juelich.de/record/1051977},
}