Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors

Selectively inhibiting N-Methyl-D-aspartate receptors (NMDARs) containing the GluN2C/2D subunits has been challenging. Here, using electrophysiology and X-ray crystallography, authors show that compounds UBP791 and UBP1700 show over 40- and 50-fold selectivity for GluN2C/2D compared to GluN2A.

Guardado en:

Detalles Bibliográficos
Autores principales:	Jue Xiang Wang, Mark W. Irvine, Erica S. Burnell, Kiran Sapkota, Robert J. Thatcher, Minjun Li, Noriko Simorowski, Arturas Volianskis, Graham L. Collingridge, Daniel T. Monaghan, David E. Jane, Hiro Furukawa
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2020
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/9cf4ff26eb1b4740b5b19c5f54918691
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:9cf4ff26eb1b4740b5b19c5f54918691
record_format	dspace
spelling	oai:doaj.org-article:9cf4ff26eb1b4740b5b19c5f549186912021-12-02T14:42:12ZStructural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors10.1038/s41467-020-14321-02041-1723https://doaj.org/article/9cf4ff26eb1b4740b5b19c5f549186912020-01-01T00:00:00Zhttps://doi.org/10.1038/s41467-020-14321-0https://doaj.org/toc/2041-1723Selectively inhibiting N-Methyl-D-aspartate receptors (NMDARs) containing the GluN2C/2D subunits has been challenging. Here, using electrophysiology and X-ray crystallography, authors show that compounds UBP791 and UBP1700 show over 40- and 50-fold selectivity for GluN2C/2D compared to GluN2A.Jue Xiang WangMark W. IrvineErica S. BurnellKiran SapkotaRobert J. ThatcherMinjun LiNoriko SimorowskiArturas VolianskisGraham L. CollingridgeDaniel T. MonaghanDavid E. JaneHiro FurukawaNature PortfolioarticleScienceQENNature Communications, Vol 11, Iss 1, Pp 1-14 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Jue Xiang Wang Mark W. Irvine Erica S. Burnell Kiran Sapkota Robert J. Thatcher Minjun Li Noriko Simorowski Arturas Volianskis Graham L. Collingridge Daniel T. Monaghan David E. Jane Hiro Furukawa Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors
description	Selectively inhibiting N-Methyl-D-aspartate receptors (NMDARs) containing the GluN2C/2D subunits has been challenging. Here, using electrophysiology and X-ray crystallography, authors show that compounds UBP791 and UBP1700 show over 40- and 50-fold selectivity for GluN2C/2D compared to GluN2A.
format	article
author	Jue Xiang Wang Mark W. Irvine Erica S. Burnell Kiran Sapkota Robert J. Thatcher Minjun Li Noriko Simorowski Arturas Volianskis Graham L. Collingridge Daniel T. Monaghan David E. Jane Hiro Furukawa
author_facet	Jue Xiang Wang Mark W. Irvine Erica S. Burnell Kiran Sapkota Robert J. Thatcher Minjun Li Noriko Simorowski Arturas Volianskis Graham L. Collingridge Daniel T. Monaghan David E. Jane Hiro Furukawa
author_sort	Jue Xiang Wang
title	Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors
title_short	Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors
title_full	Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors
title_fullStr	Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors
title_full_unstemmed	Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors
title_sort	structural basis of subtype-selective competitive antagonism for glun2c/2d-containing nmda receptors
publisher	Nature Portfolio
publishDate	2020
url	https://doaj.org/article/9cf4ff26eb1b4740b5b19c5f54918691
work_keys_str_mv	AT juexiangwang structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT markwirvine structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT ericasburnell structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT kiransapkota structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT robertjthatcher structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT minjunli structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT norikosimorowski structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT arturasvolianskis structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT grahamlcollingridge structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT danieltmonaghan structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT davidejane structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors AT hirofurukawa structuralbasisofsubtypeselectivecompetitiveantagonismforglun2c2dcontainingnmdareceptors
_version_	1718389768223457280

Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors

Ejemplares similares