| Autor: |
Stacey M. Southall, Joydeep Banerjee, Jason Brown, Kristina Butkovic, Andrew D. Cansfield, Julie E. Cansfield, Miles S. Congreve, Gabriella Cseke, Francesca Deflorian, Martina Petrovic Hunjadi, Antun Hutinec, Trinadh Kumar Inturi, Renata Rupcic, Gordon Saxty, Stephen P. Watson |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 13:1776-1782 |
| ISSN: |
1948-5875 |
| Popis: |
The diastereomeric macrocyclic calcitonin generelated peptide (CGRP) antagonists HTL0029881 (3) and HTL0029882 (4), in which the stereochemistry of a spiro center is reversed, surprisingly demonstrate comparable potency. X-ray crystallographic characterization demonstrates that 3 binds to the CGRP receptor in a precedented manner but that 4 binds in an unprecedented, unexpected, and radically different manner. The observation of this phenomenon is noteworthy and may open novel avenues for CGRP receptor antagonist design. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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