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Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
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; Hunjadi, Martina Petrovic; Hutinec, Antun; Inturi, Trinadh Kumar; Landek, Goran; Mason, Jonathan; O'Brien, Alistair; Ott, Gregory R; Rupcic, Renata; Saxty, Gordon; Southall, Stacey M; Zadravec, Rahela; Watson, Stephen P.
Afiliación
  • Cansfield AD; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Ator MA; Teva Pharmaceuticals, 145 Brandywine Parkway, West Chester, Pennsylvania 19380, United States.
  • Banerjee J; Syngene International, Biocon Park, Bommasandra, Bangalore 560099, India.
  • Bestwick M; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Bortolato A; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Brown GA; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Brown J; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Butkovic K; Fidelta d.o.o., Prilaz Baruna Filipovica 29, 10000 Zagreb, Croatia.
  • Cansfield JE; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Christopher JA; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Congreve M; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Cseke G; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Deflorian F; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Dugan B; Teva Pharmaceuticals, 145 Brandywine Parkway, West Chester, Pennsylvania 19380, United States.
  • Hunjadi MP; Fidelta d.o.o., Prilaz Baruna Filipovica 29, 10000 Zagreb, Croatia.
  • Hutinec A; Fidelta d.o.o., Prilaz Baruna Filipovica 29, 10000 Zagreb, Croatia.
  • Inturi TK; Syngene International, Biocon Park, Bommasandra, Bangalore 560099, India.
  • Landek G; Fidelta d.o.o., Prilaz Baruna Filipovica 29, 10000 Zagreb, Croatia.
  • Mason J; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • O'Brien A; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Ott GR; Teva Pharmaceuticals, 145 Brandywine Parkway, West Chester, Pennsylvania 19380, United States.
  • Rupcic R; Fidelta d.o.o., Prilaz Baruna Filipovica 29, 10000 Zagreb, Croatia.
  • Saxty G; Fidelta d.o.o., Prilaz Baruna Filipovica 29, 10000 Zagreb, Croatia.
  • Southall SM; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
  • Zadravec R; Fidelta d.o.o., Prilaz Baruna Filipovica 29, 10000 Zagreb, Croatia.
  • Watson SP; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, U.K.
ACS Chem Neurosci ; 13(6): 751-765, 2022 03 16.
Article en En | MEDLINE | ID: mdl-35245037
ABSTRACT
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Péptido Relacionado con el Gen de Calcitonina / Receptores Acoplados a Proteínas G Idioma: En Revista: ACS Chem Neurosci Año: 2022 Tipo del documento: Article País de afiliación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Péptido Relacionado con el Gen de Calcitonina / Receptores Acoplados a Proteínas G Idioma: En Revista: ACS Chem Neurosci Año: 2022 Tipo del documento: Article País de afiliación: Reino Unido