Zobrazeno 1 - 10
of 142
pro vyhledávání: '"Denise, Wootten"'
Autor:
Kaleeckal G. Harikumar, Sarah J. Piper, Arthur Christopoulos, Denise Wootten, Patrick M. Sexton, Laurence J. Miller
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-12 (2024)
Abstract Class B G protein-coupled receptors can form dimeric complexes important for high potency biological effects. Here, we apply pharmacological, biochemical, and biophysical techniques to cells and membranes expressing the prototypic secretin r
Externí odkaz:
https://doaj.org/article/03bd6139abd74708a85a68f98f562b73
Autor:
Kaleeckal G Harikumar, Peishen Zhao, Brian P Cary, Xiaomeng Xu, Aditya J Desai, Maoqing Dong, Jesse I Mobbs, Chirine Toufaily, Sebastian G B Furness, Arthur Christopoulos, Matthew J Belousoff, Denise Wootten, Patrick M Sexton, Laurence J Miller
Publikováno v:
PLoS Biology, Vol 22, Iss 7, p e3002673 (2024)
Development of optimal therapeutics for disease states that can be associated with increased membrane cholesterol requires better molecular understanding of lipid modulation of the drug target. Type 1 cholecystokinin receptor (CCK1R) agonist actions
Externí odkaz:
https://doaj.org/article/897ba52f46f9422aa4eba66be6e9d3a4
Autor:
Wessel A. C. Burger, Vi Pham, Ziva Vuckovic, Alexander S. Powers, Jesse I. Mobbs, Yianni Laloudakis, Alisa Glukhova, Denise Wootten, Andrew B. Tobin, Patrick M. Sexton, Steven M. Paul, Christian C. Felder, Radostin Danev, Ron O. Dror, Arthur Christopoulos, Celine Valant, David M. Thal
Publikováno v:
Nature Communications, Vol 14, Iss 1, Pp 1-11 (2023)
Abstract The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of high therapeutic interest due to its expression in regions of the brain involved in the regulation of psychosis, cognition, and addiction. The mAChR agonist,
Externí odkaz:
https://doaj.org/article/7484d1906038449ebf83ab0a1980953a
Autor:
Sarah J. Piper, Giuseppe Deganutti, Jessica Lu, Peishen Zhao, Yi-Lynn Liang, Yao Lu, Madeleine M. Fletcher, Mohammed Akhter Hossain, Arthur Christopoulos, Christopher A. Reynolds, Radostin Danev, Patrick M. Sexton, Denise Wootten
Publikováno v:
Nature Communications, Vol 13, Iss 1, Pp 1-20 (2022)
Previously, peptide selectivity in the VPAC receptor family of GPCRs was poorly understood. Here, authors combine cryo-EM and MD data to understand binding and selectivity of VPAC1R and PAC1R peptide agonists that can guide future drug development.
Externí odkaz:
https://doaj.org/article/f2ad6a82f21b446eaee66d37613979d6
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:
Giuseppe Deganutti, Yi-Lynn Liang, Xin Zhang, Maryam Khoshouei, Lachlan Clydesdale, Matthew J. Belousoff, Hari Venugopal, Tin T. Truong, Alisa Glukhova, Andrew N. Keller, Karen J. Gregory, Katie Leach, Arthur Christopoulos, Radostin Danev, Christopher A. Reynolds, Peishen Zhao, Patrick M. Sexton, Denise Wootten
Publikováno v:
Nature Communications, Vol 13, Iss 1, Pp 1-18 (2022)
The glucagon-like peptide-1 receptor (GLP-1R) can be targeted in the treatment of diabetes, obesity and other metabolic disorders. Here, the authors assess the molecular mechanisms of peptide agonists binding to GLP-1R and the responses elucidated by
Externí odkaz:
https://doaj.org/article/8f7e8894b23a4f8eb32f5d2c26ccefc6
Autor:
Radostin Danev, Matthew Belousoff, Yi-Lynn Liang, Xin Zhang, Fabian Eisenstein, Denise Wootten, Patrick M. Sexton
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-10 (2021)
There is a need to optimise cryo-EM data acquisition approaches to improve the resolution of GPCR cryo-EM structures to better than 2.5 Å, in order to use them for structure-based drug design purposes. Here, the authors present a systematic analysis
Externí odkaz:
https://doaj.org/article/4b98c85f04bd463f9b6c1fcd192b0ef8
Autor:
Maoqing Dong, Giuseppe Deganutti, Sarah J. Piper, Yi-Lynn Liang, Maryam Khoshouei, Matthew J. Belousoff, Kaleeckal G. Harikumar, Christopher A. Reynolds, Alisa Glukhova, Sebastian G. B. Furness, Arthur Christopoulos, Radostin Danev, Denise Wootten, Patrick M. Sexton, Laurence J. Miller
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-17 (2020)
The class B secretin GPCR (SecR) has broad physiological effects, with target potential for treatment of metabolic and cardiovascular disease. Here, authors present a cryo-EM structure and biochemical studies of secretin binding to the SecR:Gs comple
Externí odkaz:
https://doaj.org/article/35d3a9f45d2f49f5b92ff1e2f30c175a
Autor:
Kaleeckal G. Harikumar, Thomas Coudrat, Aditya J. Desai, Maoqing Dong, Daniela G. Dengler, Sebastian G. B. Furness, Arthur Christopoulos, Denise Wootten, Eduard A. Sergienko, Patrick M. Sexton, Laurence J. Miller
Publikováno v:
Frontiers in Endocrinology, Vol 12 (2021)
Drugs useful in prevention/treatment of obesity could improve health. Cholecystokinin (CCK) is a key regulator of appetite, working through the type 1 CCK receptor (CCK1R); however, full agonists have not stimulated more weight loss than dieting. We
Externí odkaz:
https://doaj.org/article/895703c860ab400c964a97eea810e55b
Autor:
Giuseppe Deganutti, Silvia Atanasio, Roxana-Maria Rujan, Patrick M. Sexton, Denise Wootten, Christopher A. Reynolds
Publikováno v:
Frontiers in Molecular Biosciences, Vol 8 (2021)
Class B1 G protein-coupled receptors (GPCRs) are important targets for many diseases, including cancer, diabetes, and heart disease. All the approved drugs for this receptor family are peptides that mimic the endogenous activating hormones. An unders
Externí odkaz:
https://doaj.org/article/d348c6f0e82d477487b7b314deab29b4