Identification of an allosteric binding site on the human glycine transporter, GlyT2, for bioactive lipid analgesics
SN Mostyn, KA Wilson, A Schumann-Gillett, ZJ Frangos… - Elife, 2019 - elifesciences.org
10.7554/eLife.47150.001 The treatment of chronic pain is poorly managed by current
analgesics, and there is a need for new classes of drugs. We recently developed a series of …
analgesics, and there is a need for new classes of drugs. We recently developed a series of …
Development of an N-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 To Produce Analgesia in a Rat Model of Chronic Pain
…, S Mohammadi, S Shimmon, ZJ Frangos… - Journal of medicinal …, 2019 - ACS Publications
Inhibitors that target the glycine transporter 2, GlyT2, show promise as analgesics, but may
be limited by their toxicity through complete or irreversible binding. Acyl-glycine inhibitors, …
be limited by their toxicity through complete or irreversible binding. Acyl-glycine inhibitors, …
Membrane cholesterol regulates inhibition and substrate transport by the glycine transporter, GlyT2
Membrane cholesterol binds to and modulates the function of various SLC6 neurotransmitter
transporters, including stabilizing the outward-facing conformation of the dopamine and …
transporters, including stabilizing the outward-facing conformation of the dopamine and …
Novel Phenylene Lipids That Are Positive Allosteric Modulators of Glycine Receptors and Inhibitors of Glycine Transporter 2
CI Gallagher, ZJ Frangos, D Sheipouri… - ACS Chemical …, 2023 - ACS Publications
Chronic pain is a complex condition that remains resistant to current therapeutics. We previously
synthesized a series of N-acyl amino acids (NAAAs) that inhibit the glycine transporter, …
synthesized a series of N-acyl amino acids (NAAAs) that inhibit the glycine transporter, …
The efficacy of the analgesic GlyT2 inhibitor, ORG25543, is determined by two connected allosteric sites
Glycine Transporter 2 (GlyT2) inhibitors have shown considerable potential as analgesics for
the treatment of neuropathic pain but also display considerable side effects. One potential …
the treatment of neuropathic pain but also display considerable side effects. One potential …
[HTML][HTML] The allosteric inhibition of glycine transporter 2 by bioactive lipid analgesics is controlled by penetration into a deep lipid cavity
KA Wilson, SN Mostyn, ZJ Frangos, S Shimmon… - Journal of Biological …, 2021 - ASBMB
The role of lipids in modulating membrane protein function is an emerging and rapidly
growing area of research. The rational design of lipids that target membrane proteins for the …
growing area of research. The rational design of lipids that target membrane proteins for the …
[HTML][HTML] Glycine transporter 2: Mechanism and allosteric modulation
ZJ Frangos, RP Cantwell Chater… - Frontiers in Molecular …, 2021 - frontiersin.org
Neurotransmitter sodium symporters (NSS) are a subfamily of SLC6 transporters responsible
for regulating neurotransmitter signalling. They are a major target for psychoactive …
for regulating neurotransmitter signalling. They are a major target for psychoactive …
Investigating the molecular mechanism of bioactive lipid inhibitors of GlyT2
ZJ Frangos - 2022 - ses.library.usyd.edu.au
Lipid modulation of glycine transport has attracted significant attention as a potential analgesic
pathway for neuropathic pain conditions. An array of bioactive lipids that potently inhibit …
pathway for neuropathic pain conditions. An array of bioactive lipids that potently inhibit …
The inhibitory activity of glycine transporter 2 targeting bioactive lipid analgesics are influenced by formation of a deep lipid cavity
KA Wilson, SN Mostyn, ZJ Frangos, S Shimmon… - bioRxiv, 2020 - biorxiv.org
The human glycine transporter 2 (GlyT2 or SLC6A5) has emerged as a promising drug target
for the development of new analgesics to manage chronic pain. N-acyl amino acids inhibit …
for the development of new analgesics to manage chronic pain. N-acyl amino acids inhibit …
Successful Treatment of Recalcitrant Mpox Lesions With Intralesional Cidofovir in a Patient With HIV/AIDS
CR Buechler, ZJ Anderson, SA Kullberg… - JAMA …, 2024 - jamanetwork.com
… Correction: This article was corrected on January 24, 2024, to correct the name and
credential of the second author, Zachary J. Anderson. Conflict of Interest Disclosures: Dr Hylwa …
credential of the second author, Zachary J. Anderson. Conflict of Interest Disclosures: Dr Hylwa …