Výsledky vyhledávání - "Ariele P. Hanek"

Photochemical Proteolysis of an Unstructured Linker of the GABAAR Extracellular Domain Prevents GABA but Not Pentobarbital Activation

Autor: Dennis A. Dougherty, Henry A. Lester, Ariele P. Hanek

Publikováno v: Molecular Pharmacology. 78:29-35

The GABA type A receptor (GABA(A)R) is the major inhibitory receptor in the mammalian central nervous system and the target of numerous pharmaceuticals. The alpha-subunit of these pentameric Cys-loop neurotransmitter-gated ion channels contributes to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1650e27231e1cc1dd7af5dd2391f5834
https://doi.org/10.1124/mol.109.059832

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A Stereochemical Test of a Proposed Structural Feature of the Nicotinic Acetylcholine Receptor

Autor: Ariele P. Hanek, Henry A. Lester, Dennis A. Dougherty

Publikováno v: Journal of the American Chemical Society. 130:13216-13218

Understanding the gating mechanism of the nicotinic acetylcholine receptor (nAChR) and similar channels constitutes a significant challenge in chemical neurobiology. In the present work, we use a stereochemical probe to evaluate a proposed pin-into-h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::296c39f5465d26ac25fe989a163a0bc4
https://doi.org/10.1021/ja8015457

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A Cation-π Interaction at a Phenylalanine Residue in the Glycine Receptor Binding Site Is Conserved for Different Agonists

Autor: Henry A. Lester, Ariele P. Hanek, Joseph W. Lynch, Dennis A. Dougherty, Kerry L. Price, Sarah C. R. Lummis, Stephan A. Pless

Cation-π interactions have been demonstrated to play a major role in agonist-binding in Cys-loop receptors. However, neither the aromatic amino acid contributing to this interaction nor its location is conserved among Cys-loop receptors. Likewise, i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4c1a7a19587f7ff1b1b5b2f929dc5ce
https://europepmc.org/articles/PMC3063724/

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A Cation-π Interaction in the Binding Site of the Glycine Receptor Is Mediated by a Phenylalanine Residue

Autor: Henry A. Lester, Kat S. Millen, Ariele P. Hanek, Stephan A. Pless, Dennis A. Dougherty, Sarah C. R. Lummis, Joseph W. Lynch

Cys-loop receptor binding sites characteristically contain many aromatic amino acids. In nicotinic ACh and 5-HT3receptors, a Trp residue forms a cation-π interaction with the agonist, whereas in GABAAreceptors, a Tyr performs this role. The glycine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a6234451d89ca3fa63bc33eda537b87
https://europepmc.org/articles/PMC2649377/

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A unified view of the role of electrostatic interactions in modulating the gating of Cys loop receptors

Autor: Ariele P. Hanek, Xinan Xiu, Jinti Wang, Dennis A. Dougherty, Henry A. Lester

Publikováno v: The Journal of biological chemistry. 280(50)

In the Cys loop superfamily of ligand-gated ion channels, a global conformational change, initiated by agonist binding, results in channel opening and the passage of ions across the cell membrane. The detailed mechanism of channel gating is a subject

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3457679c4f472b60a18ff98d733984b4
https://pubmed.ncbi.nlm.nih.gov/16216879

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