Structure-Based Design of Potent TLR7/8/9 Triple Antagonists: Overcoming High Tissue Distribution and Reactive Metabolite Liabilities
, demonstrated robust dose-dependent inhibition of TLR7 and TLR9 pathways in mouse challenging models, supporting the potential of a TLR7/8/9 triple antagonist for treating autoimmune diseases.
Authors
- Lue Dai (ORCID: https://orcid.org/0000-0002-1513-2503)
- M.G. Rudolph (ORCID: https://orcid.org/0000-0003-0447-1101)
- Buyu Kou
- Kristin Sokoll
- Daniel Schlatter
- Kara G. Lassen (ORCID: https://orcid.org/0000-0001-7023-461X)
- Bernard Gsell
- Jieyu Dai
- Tina Kaiser (ORCID: https://orcid.org/0000-0001-6890-678X)
- A. Ehler
- Xin Yu (ORCID: https://orcid.org/0000-0001-7713-2106)
- Fabian Dey (ORCID: https://orcid.org/0000-0002-4903-2869)
- Hong C. Shen (ORCID: https://orcid.org/0000-0002-3477-8932)
- Haiyuan Ding
- H Liu (ORCID: https://orcid.org/0009-0004-7817-5203)
- Zhisen Zhang (ORCID: https://orcid.org/0000-0002-8638-0993)
- Zhiwei Zhang (ORCID: https://orcid.org/0000-0002-6131-3233)
- Wei Zhang (ORCID: https://orcid.org/0000-0001-7800-3189)
- Xiaoqing Wang (ORCID: https://orcid.org/0000-0001-7476-8889)
- Wei Zhu (ORCID: https://orcid.org/0000-0003-4701-2474)
- Liu Y (ORCID: https://orcid.org/0009-0004-3901-1652)
- Zhaohu Lin
- Taishan Hu
- Hong-Xia Qiu
- Jörg Benz
- Ge Zou
- Jianquan Wu
- Fang Shen
- Tianyi Jiang
- Lina Zhu
Institutions
- Roche (Switzerland) (CH)
- Roche (China) (CN)
- Institute for Computer Aided Design (RU)
- Institute of Medicinal Plant Development (CN)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2026-07-22
- DOI
- https://doi.org/10.1021/acs.jmedchem.6c00993
- Primary Topic
- Immune Response and Inflammation
- Type
- article
- Field-Weighted Citation Impact
- 0.00