Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation.


Journal

Nature communications
ISSN: 2041-1723
Titre abrégé: Nat Commun
Pays: England
ID NLM: 101528555

Informations de publication

Date de publication:
05 02 2021
Historique:
received: 30 07 2020
accepted: 05 01 2021
entrez: 6 2 2021
pubmed: 7 2 2021
medline: 18 2 2021
Statut: epublish

Résumé

Narcolepsy type 1 (NT1) is a chronic neurological disorder that impairs the brain's ability to control sleep-wake cycles. Current therapies are limited to the management of symptoms with modest effectiveness and substantial adverse effects. Agonists of the orexin receptor 2 (OX

Identifiants

pubmed: 33547286
doi: 10.1038/s41467-021-21087-6
pii: 10.1038/s41467-021-21087-6
pmc: PMC7864924
doi:

Substances chimiques

Aminopyridines 0
Azepines 0
HCRTR2 protein, human 0
N-ethyl-2-((6-methoxy-pyridin-3-yl)-(toluene-2-sulphonyl)amino)-N-pyridin-3-ylmethyl-acetamide 0
Orexin Receptor Antagonists 0
Orexin Receptors 0
Peptides 0
Recombinant Proteins 0
Sleep Aids, Pharmaceutical 0
Sulfonamides 0
Triazoles 0
suvorexant 081L192FO9

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

815

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Auteurs

Chuan Hong (C)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, Kenilworth, NJ, USA.

Noel J Byrne (NJ)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Beata Zamlynny (B)

Screening & Compound Profiling, MRL, Merck & Co., Inc, Kenilworth, NJ, USA.

Srivanya Tummala (S)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Li Xiao (L)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, Kenilworth, NJ, USA.

Jennifer M Shipman (JM)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Andrea T Partridge (AT)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Christina Minnick (C)

Quantitative Bioscience, MRL, Merck & Co., Inc, West Point, PA, USA.

Michael J Breslin (MJ)

Discovery Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Michael T Rudd (MT)

Discovery Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Shawn J Stachel (SJ)

Discovery Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Vanessa L Rada (VL)

Discovery Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Jeffrey C Kern (JC)

Discovery Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Kira A Armacost (KA)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Scott A Hollingsworth (SA)

Computational & Structural Chemistry, MRL, Merck & Co., Inc., South San Francisco, CA, USA.

Julie A O'Brien (JA)

Quantitative Bioscience, MRL, Merck & Co., Inc, West Point, PA, USA.

Dawn L Hall (DL)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Terrence P McDonald (TP)

Neuroscience, MRL, Merck & Co., Inc, West Point, PA, USA.

Corey Strickland (C)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, Kenilworth, NJ, USA.

Alexei Brooun (A)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA.

Stephen M Soisson (SM)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA. stephen_soisson@merck.com.

Kaspar Hollenstein (K)

Computational & Structural Chemistry, MRL, Merck & Co., Inc, West Point, PA, USA. kaspar.hollenstein@merck.com.

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Classifications MeSH