Geoff Thompson
Monash University
5 Papers
6 Citations
Geoff Thompson is an academic researcher from Monash University. The author has contributed to research in topics: Allosteric regulation & Allosteric modulator. The author has an hindex of 2, co-authored 5 publications.
Chat about Author
Papers
Crystal structure of the M5 muscarinic acetylcholine receptor
Ziva Vuckovic,Patrick R. Gentry,Alice E. Berizzi,Kunio Hirata,Swapna Varghese,Geoff Thompson,Emma T van der Westhuizen,Wessel A.C. Burger,Raphaël Rahmani,Celine Valant,Christopher J. Langmead,Craig W. Lindsley,Jonathan B. Baell,Andrew B. Tobin,Patrick M. Sexton,Patrick M. Sexton,Arthur Christopoulos,David M. Thal +17 more
TL;DR: This study reports a high-resolution crystal structure of the human M5 mAChR bound to the clinically used inverse agonist, tiotropium, which provides important insights into the nature of orthosteric and allosteric ligand interaction across the mAchR family that could be exploited for the design of selective drugs.
71
Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs
Scott A. Hollingsworth,Scott A. Hollingsworth,Brendan Kelly,Celine Valant,Jordan Arthur Michaelis,Olivia Mastromihalis,Geoff Thompson,AJ Venkatakrishnan,Samuel Hertig,Peter J. Scammells,Patrick M. Sexton,Christian C. Felder,Arthur Christopoulos,Ron O. Dror +13 more
TL;DR: It is shown that positive allosteric modulators of the M1 muscarinic acetylcholine receptor (mAChR) achieve exquisite selectivity by occupying a dynamic pocket absent in existing crystal structures, identified using molecular dynamics simulations.
Crystal structure of the M5muscarinic acetylcholine receptor.
Ziva Vuckovic,Patrick R. Gentry,Alice E. Berizzi,Kunio Hirata,Swapna Varghese,Geoff Thompson,E.T. van der Westhuizen,Wessel A.C. Burger,Raphaël Rahmani,Celine Valant,Christopher J. Langmead,Craig W. Lindsley,Jonathan B. Baell,Andrew B. Tobin,Patrick M. Sexton,Arthur Christopoulos,David M. Thal +16 more
13
Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor.
Wessel A.C. Burger,Patrick R. Gentry,Alice E. Berizzi,Ziva Vuckovic,Emma T van der Westhuizen,Geoff Thompson,Mahmuda Yeasmin,Craig W. Lindsley,Patrick M. Sexton,Christopher J. Langmead,Andrew B. Tobin,Arthur Christopoulos,Celine Valant,David M. Thal +13 more
TL;DR: In this article, the M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders.
7
Crystal structure of the M5 muscarinic acetylcholine receptor
Ziva Vuckovic,Patrick R. Gentry,Alice E. Berizzi,Kunio Hirata,Swapna Varghese,Geoff Thompson,Emma T van der Westhuizen,Wessel A.C. Burger,Raphaël Rahmani,Celine Valant,Christopher J. Langmead,Craig W. Lindsley,Jonathan B. Baell,Andrew B. Tobin,Patrick M. Sexton,Patrick M. Sexton,Arthur Christopoulos,David M. Thal +17 more
TL;DR: A high-resolution crystal structure of the human M5 mAChR bound to the clinically used inverse agonist, tiotropium is determined and reveals subtle differences in the extracellular loop (ECL) regions of the receptor that mediate orthosteric and allosteric ligand selectivity.
1