Photoswitchable ORG25543 Congener Enables Optical Control of Glycine Transporter 2.

Mostyn, SN; Sarker, S; Muthuraman, P; Raja, A; Shimmon, S; Rawling, T; Cioffi, CL; Vandenberg, RJ

Photoswitchable ORG25543 Congener Enables Optical Control of Glycine Transporter 2.

Mostyn, SN Sarker, S Muthuraman, P Raja, A Shimmon, S Rawling, T

Cioffi, CL Vandenberg, RJ

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Publisher:: AMER CHEMICAL SOC
Publication Type:: Journal Article
Citation:: ACS chemical neuroscience, 2020, 11, (9), pp. 1250-1258
Issue Date:: 2020-05

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Field	Value	Language
dc.contributor.author	Mostyn, SN
dc.contributor.author	Sarker, S
dc.contributor.author	Muthuraman, P
dc.contributor.author	Raja, A
dc.contributor.author	Shimmon, S
dc.contributor.author	Rawling, T https://orcid.org/0000-0002-6624-6586
dc.contributor.author	Cioffi, CL
dc.contributor.author	Vandenberg, RJ
dc.date.accessioned	2021-01-12T05:06:58Z
dc.date.available	2021-01-12T05:06:58Z
dc.date.issued	2020-05
dc.identifier.citation	ACS chemical neuroscience, 2020, 11, (9), pp. 1250-1258
dc.identifier.issn	1948-7193
dc.identifier.issn	1948-7193
dc.identifier.uri	http://hdl.handle.net/10453/145337
dc.description.abstract	Glycine neurotransmission in the dorsal horn of the spinal cord plays a key role in regulating nociceptive signaling, but in chronic pain states reduced glycine neurotransmission is associated with the development of allodynia and hypersensitivity to painful stimuli. This suggests that restoration of glycine neurotransmission may be therapeutic for the treatment of chronic pain. Glycine transporter 2 inhibitors have been demonstrated to enhance glycine neurotransmission and provide relief from allodynia in rodent models of chronic pain. In recent years, photoswitchable compounds have been developed to provide the possibility of controlling the activity of target proteins using light. In this study we have developed a photoswitchable noncompetitive inhibitor of glycine transporter 2 that has different affinities for the transporter at 365 nm compared to 470 nm light.
dc.format	Print-Electronic
dc.language	eng
dc.publisher	AMER CHEMICAL SOC
dc.relation.ispartof	ACS chemical neuroscience
dc.relation.isbasedon	10.1021/acschemneuro.9b00655
dc.rights	info:eu-repo/semantics/restrictedAccess
dc.subject	0304 Medicinal and Biomolecular Chemistry
dc.title	Photoswitchable ORG25543 Congener Enables Optical Control of Glycine Transporter 2.
dc.type	Journal Article
utslib.citation.volume	11
utslib.location.activity	United States
utslib.for	0304 Medicinal and Biomolecular Chemistry
pubs.organisational-group	/University of Technology Sydney/Faculty of Science
pubs.organisational-group	/University of Technology Sydney/Faculty of Science/School of Mathematical and Physical Sciences
pubs.organisational-group	/University of Technology Sydney
utslib.copyright.status	closed_access	*
pubs.consider-herdc	false
dc.date.updated	2021-01-12T05:06:48Z
pubs.issue	9
pubs.publication-status	Published
pubs.volume	11
utslib.citation.issue	9

Abstract:

Glycine neurotransmission in the dorsal horn of the spinal cord plays a key role in regulating nociceptive signaling, but in chronic pain states reduced glycine neurotransmission is associated with the development of allodynia and hypersensitivity to painful stimuli. This suggests that restoration of glycine neurotransmission may be therapeutic for the treatment of chronic pain. Glycine transporter 2 inhibitors have been demonstrated to enhance glycine neurotransmission and provide relief from allodynia in rodent models of chronic pain. In recent years, photoswitchable compounds have been developed to provide the possibility of controlling the activity of target proteins using light. In this study we have developed a photoswitchable noncompetitive inhibitor of glycine transporter 2 that has different affinities for the transporter at 365 nm compared to 470 nm light.

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http://hdl.handle.net/10453/145337