＞＞Heptares has solved the crystal structures of multiple class B GPCRs in complex with low molecular weight ligands. From these a highly optimised GLP-1 receptor homology model was developed and used for peptide design. Specifically, we targeted peptides with reduced size and improved physicochemical properties with the aim of controlling clearance, volume of distribution and plasma half-life properties. Lead peptides were tested across a range of in vitro assay formats in which they demonstrated high affinity and efficacy comparable to full-length GLP-1. Pharmacokinetic analysis demonstrated profiles consistent with their physicochemical properties and supported testing in vivo: the lead peptide demonstrated positive efficacy similar to exendin-4 in a mouse OGTT.
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＞＞Heptares has solved the crystal structures of multiple class B GPCRs in complex with low molecular weight ligands. From these a highly optimised GLP-1 receptor homology model was developed and used for peptide design. Specifically, we targeted peptides with reduced size and improved physicochemical properties with the aim of controlling clearance, volume of distribution and plasma half-life properties. Lead peptides were tested across a range of in vitro assay formats in which they demonstrated high affinity and efficacy comparable to full-length GLP-1. Pharmacokinetic analysis demonstrated profiles consistent with their physicochemical properties and supported testing in vivo: the lead peptide demonstrated positive efficacy similar to exendin-4 in a mouse OGTT.
GLP-1アゴニストは市場規模が大きいので期待大