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• W2912690805 abstract "Adrenomedullin (ADM) is a vasoactive peptide hormone of 52 amino acids and belongs to the calcitonin peptide superfamily. Its vasodilative effects are mediated by the interaction with the calcitonin receptor‐like receptor (CLR), a class B G protein‐coupled receptor (GPCR), associated with the receptor activity modifying protein 2 (RAMP2) and functionally described as AM‐1 receptor (AM 1 R). A disulfide‐bonded ring structure consisting of six amino acids between Cys 16 and Cys 21 has been shown to be a key motif for receptor activation. However, the specific structural requirements remain to be elucidated. To investigate the influence of ring size and position of additional functional groups that replace the native disulfide bond, we generated ADM analogs containing thioether, thioacetal, alkane, and lactam bonds between amino acids 16 and 21 by Fmoc/ t‐ Bu solid phase peptide synthesis. Activity studies of the ADM disulfide bond mimetics (DSBM) revealed a strong impact of structural parameters. Interestingly, an increased ring size was tolerated but the activity of lactam‐based mimetics depended on its position within the bridging structure. Furthermore, we found the thioacetal as well as the thioether‐based mimetics to be well accepted with full AM 1 R activity. While a reduced selectivity over the calcitonin gene‐related peptide receptor (CGRPR) was observed for the thioethers, the thioacetal was able to retain a wild–type‐like selectivity profile. The carbon analog in contrast displayed weak antagonistic properties. These results provide insight into the structural requirements for AM 1 R activation as well as new possibilities for the development of metabolically stabilized analogs for therapeutic applications of ADM." @default.
• W2912690805 created "2019-02-21" @default.
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• W2912690805 date "2019-01-24" @default.
• W2912690805 modified "2023-09-24" @default.
• W2912690805 title "Adrenomedullin disulfide bond mimetics uncover structural requirements for AM₁receptor activation" @default.
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• W2912690805 doi "https://doi.org/10.1002/psc.3147" @default.
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• W2912690805 hasPublicationYear "2019" @default.
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