MET-Activating Ubiquitin Multimers.


Journal

Angewandte Chemie (International ed. in English)
ISSN: 1521-3773
Titre abrégé: Angew Chem Int Ed Engl
Pays: Germany
ID NLM: 0370543

Informations de publication

Date de publication:
04 09 2023
Historique:
received: 22 05 2023
medline: 31 8 2023
pubmed: 14 7 2023
entrez: 14 7 2023
Statut: ppublish

Résumé

Receptor tyrosine kinases (RTKs) are generally activated through their dimerization and/or oligomerization induced by their cognate ligands, and one such RTK hepatocyte growth factor (HGF) receptor, known as MET, plays an important role in tissue regeneration. Here we show the development of ubiquitin (Ub)-based protein ligand multimers, referred to as U-bodies, which act as surrogate agonists for MET and are derived from MET-binding macrocyclic peptides. Monomeric Ub constructs (U-body) were first generated by genetic implantation of a macrocyclic peptide pharmacophore into a structural loop of Ub (lasso-grafting) and subsequent optimization of its flanking spacer sequences via mRNA display. Such U-body constructs exhibit potent binding affinity to MET, thermal stability, and proteolytic stability. The U-body constructs also partially/fully inhibited or enhanced HGF-induced MET-phosphorylation. Their multimerization to dimeric, tetrameric, and octameric U-bodies linked by an appropriate peptide linker yielded potent MET activation activity and downstream cell proliferation-promoting activity. This work suggests that lasso-grafting of macrocycles to Ub is an effective approach to devising protein-based artificial RTK agonists and it can be useful in the development of a new class of biologics for various therapeutic applications.

Identifiants

pubmed: 37450419
doi: 10.1002/anie.202307157
doi:

Substances chimiques

Hepatocyte Growth Factor 67256-21-7
Ubiquitin 0
Proto-Oncogene Proteins c-met EC 2.7.10.1
Peptides 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

e202307157

Informations de copyright

© 2023 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.

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Auteurs

Naoya Kawakami (N)

Department of Chemistry, Graduate School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan.

Hiroki Sato (H)

Division of Tumor Dynamics and Regulation, Cancer Research Institute, Kanazawa University Kakuma-machi, Kanazawa City, Ishikawa, 920-1192, Japan.
WPI-Nano Life Science Institute (WPI-NanoLSI), Kanazawa University Kakuma-machi, Kanazawa City, Ishikawa, 920-1192, Japan.

Naohiro Terasaka (N)

Department of Chemistry, Graduate School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan.
Earth-Life Science Institute, Tokyo Institute of Technology, 2-12-1 Ookayama, Meguro-ku, Tokyo, 152-8550, Japan.

Kunio Matsumoto (K)

Division of Tumor Dynamics and Regulation, Cancer Research Institute, Kanazawa University Kakuma-machi, Kanazawa City, Ishikawa, 920-1192, Japan.
WPI-Nano Life Science Institute (WPI-NanoLSI), Kanazawa University Kakuma-machi, Kanazawa City, Ishikawa, 920-1192, Japan.

Hiroaki Suga (H)

Department of Chemistry, Graduate School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan.

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