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Pregled bibliografske jedinice broj: 1263956

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. et al.
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes // ACS Chemical Neuroscience, 13 (2022), 6; 751-765 doi:10.1021/acschemneuro.1c00696 (međunarodna recenzija, članak, znanstveni)

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Naslov
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes

Autori
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.

Izvornik
ACS Chemical Neuroscience (1948-7193) 13 (2022), 6; 751-765

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
GPCR CGRP CGRPR macrocycle macrocyclic antagonist

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA

Ustanove:
Fidelta d.o.o.

Profili:

Avatar Url Goran Landek (autor)

Avatar Url Renata Rupčić (autor)

Avatar Url Kristina Butković (autor)

Avatar Url Antun Hutinec (autor)

Poveznice na cjeloviti tekst rada:

doi

Citiraj ovu publikaciju:

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. et al.
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes // ACS Chemical Neuroscience, 13 (2022), 6; 751-765 doi:10.1021/acschemneuro.1c00696 (međunarodna recenzija, članak, znanstveni)
Cansfield, Andrew, D., Ator, M., Banerjee, J., Bestwick, M., Bortolato, A., Brown, G., Brown, J., Butkovic, K., Cansfield, J. & Christopher, J. (2022) Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes. ACS Chemical Neuroscience, 13 (6), 751-765 doi:10.1021/acschemneuro.1c00696.
@article{article, author = {Ator, Mark A. and Banerjee, Joydeep and Bestwick, Michael and Bortolato, Andrea and Brown, Giles A. and Brown, Jason and Butkovic, Kristina and Cansfield, Julie E. and Christopher, John A. and Congreve, Miles and Cseke, Gabriella and Deflorian, Francesca and Dugan, Benjamin and Petrovic Hunjadi, Martina and Hutinec, Antun and Kumar Inturi, Trinadh and Landek, Goran and Mason, Jonathan and O’Brien, Alistair and Ott, Gregory R. and Rupcic, Renata and Saxty, Gordon and Southall, Stacey M. and Zadravec, Rahela and Watson, Stephen P.}, year = {2022}, pages = {751-765}, DOI = {10.1021/acschemneuro.1c00696}, keywords = {GPCR CGRP CGRPR macrocycle macrocyclic antagonist}, journal = {ACS Chemical Neuroscience}, doi = {10.1021/acschemneuro.1c00696}, volume = {13}, number = {6}, issn = {1948-7193}, title = {Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes}, keyword = {GPCR CGRP CGRPR macrocycle macrocyclic antagonist} }
@article{article, author = {Ator, Mark A. and Banerjee, Joydeep and Bestwick, Michael and Bortolato, Andrea and Brown, Giles A. and Brown, Jason and Butkovic, Kristina and Cansfield, Julie E. and Christopher, John A. and Congreve, Miles and Cseke, Gabriella and Deflorian, Francesca and Dugan, Benjamin and Petrovic Hunjadi, Martina and Hutinec, Antun and Kumar Inturi, Trinadh and Landek, Goran and Mason, Jonathan and O’Brien, Alistair and Ott, Gregory R. and Rupcic, Renata and Saxty, Gordon and Southall, Stacey M. and Zadravec, Rahela and Watson, Stephen P.}, year = {2022}, pages = {751-765}, DOI = {10.1021/acschemneuro.1c00696}, keywords = {GPCR CGRP CGRPR macrocycle macrocyclic antagonist}, journal = {ACS Chemical Neuroscience}, doi = {10.1021/acschemneuro.1c00696}, volume = {13}, number = {6}, issn = {1948-7193}, title = {Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein−Ligand Complexes}, keyword = {GPCR CGRP CGRPR macrocycle macrocyclic antagonist} }

Časopis indeksira:


  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE

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