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TitleEpitope-directed selection of GPCR nanobody ligands with evolvable function.
Journal, issue, pagesProc Natl Acad Sci U S A, Vol. 122, Issue 11, Page e2423931122, Year 2025
Publish dateMar 18, 2025
AuthorsMeredith A Skiba / Clare Canavan / Genevieve R Nemeth / Jinghan Liu / Ali Kanso / Andrew C Kruse /
PubMed AbstractAntibodies have the potential to target G protein-coupled receptors (GPCRs) with high receptor, cellular, and tissue selectivity; however, few antibody ligands for GPCRs exist. Here, we describe a ...Antibodies have the potential to target G protein-coupled receptors (GPCRs) with high receptor, cellular, and tissue selectivity; however, few antibody ligands for GPCRs exist. Here, we describe a generalizable selection method to enrich for GPCR ligands from a synthetic camelid antibody fragment (nanobody) library. Our strategy yielded multiple nanobody ligands for the angiotensin II type I receptor (AT1R), a prototypical GPCR and important drug target. We found that nanobodies readily act as allosteric modulators, encoding selectivity for both the receptor and chemical features of GPCR ligands. We then used structure-guided design to convert two nanobodies from allosteric ligands to competitive AT1R inhibitors through simple mutations. This work demonstrates that nanobodies can encode multiple pharmacological behaviors and have great potential as evolvable scaffolds for the development of next-generation GPCR therapeutics.
External linksProc Natl Acad Sci U S A / PubMed:40067891 / PubMed Central
MethodsEM (single particle)
Resolution3.1 - 3.2 Å
Structure data

47831

9eah

EMDB-47831, PDB-9eah:
Structure of nanobody AT209 in complex with the olmesartan-bound angiotensin II type I receptor (AT1R)
Method: EM (single particle) / Resolution: 3.1 Å

47832

9eai

EMDB-47832, PDB-9eai:
Structure of nanobody AT206 in complex with the losartan-bound angiotensin II type I receptor (AT1R)
Method: EM (single particle) / Resolution: 3.1 Å

47833

9eaj

EMDB-47833, PDB-9eaj:
Structure of nanobody AT206 in complex with the angiotensin II type I receptor (AT1R)
Method: EM (single particle) / Resolution: 3.2 Å

Chemicals

ChemComp-OLM:
Olmesartan

ChemComp-CLR:
CHOLESTEROL

ChemComp-LSN:
[2-butyl-5-chloranyl-3-[[4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol

ChemComp-Y01:
CHOLESTEROL HEMISUCCINATE

Source
  • homo sapiens (human)
  • synthetic construct (others)
  • camelidae (mammal)
  • escherichia coli (E. coli)
KeywordsMEMBRANE PROTEIN / GPCR / AT1R / nanobody

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