Proposed mechanism of receptor-dependent activity of bitopic ligands. Structures of PTHR1 and A2AR used in this panel were generated using Alphafold2.

Bitopic ligands comprise a #pharmacophore & a linked moiety that bind to separate sites. @rche54.bsky.social &co show that #GPCRs that bind small molecules can be potently activated by #bitopic #nanobody -ligand conjugates to selectively target pairs of GPCRs @plosbiology.org 🧪 plos.io/4p3VOyH

Proposed mechanism of receptor-dependent activity of bitopic ligands. Structures of PTHR1 and A2AR used in this panel were generated using Alphafold2.

Bitopic ligands comprise a #pharmacophore & a linked moiety that bind to separate sites. @rche54.bsky.social &co show that #GPCRs that bind small molecules can be potently activated by #bitopic #nanobody -ligand conjugates to selectively target pairs of GPCRs @plosbiology.org 🧪 plos.io/4p3VOyH

Proposed mechanism of receptor-dependent activity of bitopic ligands. Structures of PTHR1 and A2AR used in this panel were generated using Alphafold2.

Bitopic ligands comprise a #pharmacophore & a linked moiety that bind to separate sites. @rche54.bsky.social &co show that #GPCRs that bind small molecules can be potently activated by #bitopic #nanobody -ligand conjugates to selectively target pairs of GPCRs @plosbiology.org 🧪 plos.io/4p3VOyH