Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Emma T. van der Westhuizen"'
Autor:
Emma T. van der Westhuizen, K. H. Christopher Choy, Celine Valant, Simon McKenzie-Nickson, Sophie J. Bradley, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos
Publikováno v:
Frontiers in Pharmacology, Vol 11 (2021)
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia. Due to high sequence homology, selective targeting of any of the M1-M5 mAC
Externí odkaz:
https://doaj.org/article/d28372b23be44dbb9a54b7ed9c514464
Autor:
Ziva Vuckovic, Jinan Wang, Vi Pham, Jesse I Mobbs, Matthew J Belousoff, Apurba Bhattarai, Wessel AC Burger, Geoff Thompson, Mahmuda Yeasmin, Vindhya Nawaratne, Katie Leach, Emma T van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W Lindsley, Andrew Tobin, Patrick Sexton, Radostin Danev, Celine Valant, Yinglong Miao, Arthur Christopoulos, David M Thal
Publikováno v:
eLife, Vol 12 (2023)
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR
Externí odkaz:
https://doaj.org/article/7f71dbdee2334fc988c8a96b377f0938
Autor:
Jesse I Mobbs, Vi Pham, Jinan Wang, Ziva Vuckovic, Matthew J Belousoff, Apurba Bhattarai, Wessel AC Burger, Geoff Thompson, Mahmuda Yeasmin, Vindhya Nawaratne, Katie Leach, Emma T van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W Lindsley, Andrew Tobin, Patrick Sexton, Radostin Danev, Celine Valant, Yinglong Miao, Arthur Christopoulos, David M Thal
Publikováno v:
eLife. 12
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6a3f8c39932d4142cae5d5abc25a4480
https://doi.org/10.7554/elife.83477
https://doi.org/10.7554/elife.83477
Autor:
Jack K. McDonald, Emma T. van der Westhuizen, Vi Pham, Geoff Thompson, Christian C. Felder, Steven M. Paul, David M. Thal, Arthur Christopoulos, Celine Valant
Publikováno v:
ACS Chemical Neuroscience. 13:1206-1218
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a0896bb8e581162bb30dc8d61f3362f1
https://doi.org/10.1021/acschemneuro.1c00827
https://doi.org/10.1021/acschemneuro.1c00827
Autor:
Manuela Jörg, Emma T. van der Westhuizen, Yao Lu, K. H. Christopher Choy, David M. Shackleford, Elham Khajehali, Andrew Tobin, David Thal, Ben Capuano, Arthur Christopoulos, Celine Valant, Peter Scammells
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b15a8d7eea63a48c1a2875d38a584ede
https://doi.org/10.2139/ssrn.4432468
https://doi.org/10.2139/ssrn.4432468
Autor:
Huong T. M. Nguyen, Emma T. van der Westhuizen, Christopher J. Langmead, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos, Celine Valant
Publikováno v:
British Journal of Pharmacology.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::71ae10831c70acc83a25c4f6be125d79
https://doi.org/10.1111/bph.15982
https://doi.org/10.1111/bph.15982
Autor:
Ziva Vuckovic, Jinan Wang, Vi Pham, Jesse I. Mobbs, Matthew J. Belousoff, Apurba Bhattarai, Wessel A.C. Burger, Geoff Thompson, Mahmuda Yeasmin, Katie Leach, Emma T. van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W. Lindsley, Andrew B. Tobin, Patrick M. Sexton, Radostin Danev, Celine Valant, Yinglong Miao, Arthur Christopoulos, David M. Thal
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular level understanding of the general principals that govern the myriad pharmacological effects exerted by GPCR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c582d2c3aeeced33d04530cd651f1edd
https://doi.org/10.1101/2022.09.27.509640
https://doi.org/10.1101/2022.09.27.509640
Autor:
Christopher J. Langmead, Mahmuda Yeasmin, Arthur Christopoulos, Geoff Thompson, Alice E. Berizzi, Emma T van der Westhuizen, Celine Valant, David M. Thal, Andrew B. Tobin, Patrick M. Sexton, Ziva Vuckovic, Wessel A.C. Burger, Patrick R. Gentry, Craig W. Lindsley
Publikováno v:
ACS Chemical Neuroscience. 12:3112-3123
The M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders. This has been in part due to promising preclinical studies with the M5 mAChR selective negative al
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::17d27430845c5e76182dde2cd731a4f1
https://doi.org/10.1021/acschemneuro.1c00383
https://doi.org/10.1021/acschemneuro.1c00383
Autor:
Arthur Christopoulos, Colin Molloy, Lisa Finlayson, Emma T van der Westhuizen, Celine Valant, Craig W. Lindsley, Sophie J. Bradley, Patrick M. Sexton, Elham Khajehali, Andrew B. Tobin
Publikováno v:
ACS Chemical Neuroscience. 11:4270-4279
Designer receptors exclusively activated by designer drugs (DREADDs) have been successfully employed to activate signaling pathways associated with specific muscarinic acetylcholine receptor (mAChR) subtypes. The M1 DREADD mAChR displays minimal resp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3f08b271a3fe2e2704c93343fc1cc1a1
https://doi.org/10.1021/acschemneuro.0c00540
https://doi.org/10.1021/acschemneuro.0c00540
Autor:
Celine Valant, Peter J. Scammells, Arthur Christopoulos, Ben Capuano, Manuela Jörg, Patrick M. Sexton, Elham Khajehali, David M. Shackleford, Kwok Ho Christopher Choy, Andrew B. Tobin, Emma T van der Westhuizen
Publikováno v:
ChemMedChem. 16:216-233
This study investigated the structure-activity relationships of 4-phenylpyridin-2-one and 6-phenylpyrimidin-4-one M1 muscarinic acetylcholine receptor (M1 mAChRs) positive allosteric modulators (PAMs). The presented series focuses on modifications to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4c2a8709f5b47591f003a0e2e8c6a516
https://doi.org/10.1002/cmdc.202000540
https://doi.org/10.1002/cmdc.202000540