| Autor: |
Andrew D. Cansfield, Mark A. Ator, Joydeep Banerjee, Michael Bestwick, Andrea Bortolato, Giles A. Brown, Jason Brown, Kristina Butkovic, Julie E. Cansfield, John A. Christopher, Miles Congreve, Gabriella Cseke, Francesca Deflorian, Benjamin Dugan, Martina Petrovic Hunjadi, Antun Hutinec, Trinadh Kumar Inturi, Goran Landek, Jonathan Mason, Alistair O’Brien, Gregory R. Ott, Renata Rupcic, Gordon Saxty, Stacey M. Southall, Rahela Zadravec, Stephen P. Watson |
| Rok vydání: |
2022 |
| Předmět: |
|
| Zdroj: |
ACS Chemical Neuroscience. 13:751-765 |
| ISSN: |
1948-7193 |
| Popis: |
A series of macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonists identified using structure-based design principles, exemplified by HTL0028016 (1) and HTL0028125 (2), is described. Structural characterization by X-ray crystallography of the interaction of two of the macrocycle antagonists with the CGRP receptor ectodomain is described, along with structure– activity relationships associated with point changes to the macrocyclic antagonists. The identification of non-peptidic/natural product- derived, macrocyclic ligands for a G protein coupled receptor (GPCR) is noteworthy. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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