Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes (CROSBI ID 323834)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Cansfield, Andrew, D. ; Ator, Mark A. ; Banerjee, Joydeep ; Bestwick, Michael ; Bortolato, Andrea ; Brown, Giles A. ; Brown, Jason ; Butkovic, Kristina ; Cansfield, Julie E. ; Christopher, John A. ; Congreve, Miles ; Cseke, Gabriella ; Deflorian, Francesca ; Dugan, Benjamin ; Petrovic Hunjadi, Martina ; Hutinec, Antun ; Kumar Inturi, Trinadh ; Landek, Goran ; Mason, Jonathan ; O’Brien, Alistair ; Ott, Gregory R. ; Rupcic, Renata ; Saxty, Gordon ; Southall, Stacey M. ; Zadravec, Rahela ; Watson, Stephen P.
engleski
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes
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.
GPCR CGRP CGRPR macrocycle macrocyclic antagonist
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