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TitleMultiscale biased chemical space remodeling for developing APLNR agonists with anti-HFpEF efficacy.
Journal, issue, pagesProc Natl Acad Sci U S A, Vol. 122, Issue 18, Page e2423432122, Year 2025
Publish dateMay 6, 2025
AuthorsQiu Sun / Xiaowen Tian / Lun Tan / Yan Deng / Sicen Liu / Yixiao Xiong / Yuying Feng / Yujia Wang / Lele Zhang / Jiayi Zhu / Huan Xiao / Zhenhua Shao / Yingqiang Guo / Wei Yan / Tao Li / Liang Ouyang /
PubMed AbstractHeart failure with preserved ejection fraction (HFpEF) represents a significant global health burden, yet effective pharmacotherapies remain elusive. The angiotensin-like 1 receptor, also known as ...Heart failure with preserved ejection fraction (HFpEF) represents a significant global health burden, yet effective pharmacotherapies remain elusive. The angiotensin-like 1 receptor, also known as the apelin receptor (APLNR), is a promising target for treating HFpEF due to its role in modulating cardiovascular function. Despite the cardioprotective effects of endogenous ligand, apelin, achieving G-protein-biased agonism for therapeutic benefit poses a significant challenge. In this study, we unravel the biased signal transduction pathway mediated by a reported partial G-protein-biased APLNR agonist CMF-019 and developed a biased chemical space remodeling approach to identify exclusive G-protein-biased agonists targeting APLNR. These agonists exhibited enhanced Gi-protein-biased function and protective effects in both in vitro and in vivo. Our findings not only enhance comprehension of APLNR-biased agonism but also establish drug design strategies for modifying and reshaping biased chemical landscapes in other G-protein-coupled receptors (GPCRs).
External linksProc Natl Acad Sci U S A / PubMed:40314976 / PubMed Central
MethodsEM (single particle)
Resolution2.93 Å
Structure data

61470

9jh3

EMDB-61470, PDB-9jh3:
CMF-019 with APLNR-Gi complex
Method: EM (single particle) / Resolution: 2.93 Å

Chemicals

PDB-1d5n:
CRYSTAL STRUCTURE OF E. COLI MNSOD AT 100K

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN/IMMUNE SYSTEM / Complex / Agonist / MEMBRANE PROTEIN / MEMBRANE PROTEIN-IMMUNE SYSTEM complex

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