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Pregled bibliografske jedinice broj: 1263949

Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode

Southall, Stacey, M.; Banerjee, Joydeep; Brown, Jason; Butkovic, Kristina; Cansfield, Andrew D.; Cansfield, Julie, E.; Congreve, Miles S.; Cseke, Gabriella; Deflorian, Franceska; Petrovic Hunjadi, Martina et al.
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode // ACS Medicinal Chemistry Letters, 13 (2022), 11; 1776-1782 doi:10.1021/acsmedchemlett.2c00400 (međunarodna recenzija, članak, znanstveni)

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Naslov
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode

Autori
Southall, Stacey, M. ; Banerjee, Joydeep ; Brown, Jason ; Butkovic, Kristina ; Cansfield, Andrew D. ; Cansfield, Julie, E. ; Congreve, Miles S. ; Cseke, Gabriella ; Deflorian, Franceska ; Petrovic Hunjadi, Martina ; Hutinec, Antun ; Kumar Inturi, Trinadh ; Rupcic, Renata ; Saxty, Gordon ; Watson, Stephen P.

Izvornik
ACS Medicinal Chemistry Letters (1948-5875) 13 (2022), 11; 1776-1782

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

Ključne riječi
GPCR, CGRP, CGRPR, Macrocycle, Macrocyclic, Antagonist

Sažetak
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.

Izvorni jezik
Engleski



POVEZANOST RADA

Ustanove:
Fidelta d.o.o.

Profili:

Avatar Url Kristina Butković (autor)

Avatar Url Antun Hutinec (autor)

Avatar Url Renata Rupčić (autor)

Poveznice na cjeloviti tekst rada:

doi

Citiraj ovu publikaciju:

Southall, Stacey, M.; Banerjee, Joydeep; Brown, Jason; Butkovic, Kristina; Cansfield, Andrew D.; Cansfield, Julie, E.; Congreve, Miles S.; Cseke, Gabriella; Deflorian, Franceska; Petrovic Hunjadi, Martina et al.
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode // ACS Medicinal Chemistry Letters, 13 (2022), 11; 1776-1782 doi:10.1021/acsmedchemlett.2c00400 (međunarodna recenzija, članak, znanstveni)
Southall, Stacey, M., Banerjee, J., Brown, J., Butkovic, K., Cansfield, A., Cansfield, Julie, E., Congreve, M., Cseke, G., Deflorian, F. & Petrovic Hunjadi, M. (2022) Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode. ACS Medicinal Chemistry Letters, 13 (11), 1776-1782 doi:10.1021/acsmedchemlett.2c00400.
@article{article, author = {Banerjee, Joydeep and Brown, Jason and Butkovic, Kristina and Cansfield, Andrew D. and Congreve, Miles S. and Cseke, Gabriella and Deflorian, Franceska and Petrovic Hunjadi, Martina and Hutinec, Antun and Kumar Inturi, Trinadh and Rupcic, Renata and Saxty, Gordon and Watson, Stephen P.}, year = {2022}, pages = {1776-1782}, DOI = {10.1021/acsmedchemlett.2c00400}, keywords = {GPCR, CGRP, CGRPR, Macrocycle, Macrocyclic, Antagonist}, journal = {ACS Medicinal Chemistry Letters}, doi = {10.1021/acsmedchemlett.2c00400}, volume = {13}, number = {11}, issn = {1948-5875}, title = {Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode}, keyword = {GPCR, CGRP, CGRPR, Macrocycle, Macrocyclic, Antagonist} }
@article{article, author = {Banerjee, Joydeep and Brown, Jason and Butkovic, Kristina and Cansfield, Andrew D. and Congreve, Miles S. and Cseke, Gabriella and Deflorian, Franceska and Petrovic Hunjadi, Martina and Hutinec, Antun and Kumar Inturi, Trinadh and Rupcic, Renata and Saxty, Gordon and Watson, Stephen P.}, year = {2022}, pages = {1776-1782}, DOI = {10.1021/acsmedchemlett.2c00400}, keywords = {GPCR, CGRP, CGRPR, Macrocycle, Macrocyclic, Antagonist}, journal = {ACS Medicinal Chemistry Letters}, doi = {10.1021/acsmedchemlett.2c00400}, volume = {13}, number = {11}, issn = {1948-5875}, title = {Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode}, keyword = {GPCR, CGRP, CGRPR, Macrocycle, Macrocyclic, Antagonist} }

Časopis indeksira:


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

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