Author

P. M. Sexton

Listed by name: these papers carry no ORCID for this author, so different people with the same name may be mixed together.

Biology Disciplines

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Pharmacology & Toxicology· 6 Biochemistry· 4 Biophysics· 1

Signature Assays, Organisms & Methods

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Approach:experimental assay· 10 Assay:cryo-EM· 7 Research Focus:host-pathogen & immune response· 5 Organism:human· 4 Research Focus:protein structure prediction· 4 Research Focus:drug response / drug discovery· 3 Research Focus:cell signaling & trafficking· 2 Research Focus:development & morphogenesis· 2

Frequent Co-Authors

D. Wootten· 8 shared M. J. Belousoff· 7 shared R. Danev· 7 shared A. Christopoulos· 5 shared X. Zhang· 5 shared P. Zhao· 4 shared T. T. truong· 4 shared Y.-L. Liang· 4 shared

Activity by Year

2019-2022 · peak 6/yr

Co-Author Collaboration Network

10 top collaborators · 45 mutual co-author links

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8 shared papersPharmacology & Toxicology

D. Wootten

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11 papers

Recent·Most cited

Molecular insights into peptide agonist engagement with the PTH1 receptor

B. P. Cary, E. J. Gerrard, M. J. Belousoff, M. M. Fletcher, Y. Jiang, I. C. Russell, S. J. Piper, D. Wootten, P. M. Sexton

This study presents cryo-EM structures of the PTH1R bound to various agonists, revealing how different peptides engage the receptor and providing insights for drug design.

bioRxiv · Sep 4, 2022 · PreprintBiochemistry

Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins: insight into mechanisms of G protein selectivity

J. Mobbs, M. J. Belousoff, K. G. Harikumar, S. J. Piper, X. Xu, S. G. B. Furness, H. Venugopal, A. Christopoulos, R. Danev, D. Wootten, D. M. Thal, L. J. Miller, P. M. Sexton

The paper determines cryo-EM structures of the CCK1R bound to Gs and Gq proteins, revealing conformational changes that enable promiscuous G protein coupling.

bioRxiv · May 6, 2021Pharmacology & Toxicology

RAMPs regulate signalling bias and internalisation of the GIPR

M. Harris, D. I. Mackie, J. B. Pawlak, S. Carvalho, T. T. truong, D. Safitri, H. Y. Yeung, S. Routledge, M. T. Harper, B. Al-Zaid, M. Soave, S. Al-Sabah, A. Inoue, D. R. Poyner, S. J. Hill, , G. Ladds

This study shows RAMPs modulate GIPR signaling and internalization, with RAMP3 reducing cAMP production and promoting surface retention, while RAMP1/2 decrease Gq/11/15 activation, and RAMP1 is essential for normal glucose regulation.

bioRxiv · Apr 8, 2021 · PreprintPharmacology & Toxicology

Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation

G. Deganutti, Y.-L. Liang, X. Zhang, M. Khoshouei, L. Clydesdale, M. J. Belousoff, H. Venugopal, T. T. Truong, A. Glukhova, A. N. Keller, K. J. Gregory, K. Leach, A. Christopoulos, R. Danev, C. A. Reynolds, , D. M. Wootten

The paper investigates how different GLP-1R agonists affect G protein activation kinetics through structural and functional analyses.

bioRxiv · Mar 10, 2021Biochemistry

Structural and Functional Diversity among Agonist-Bound States of the GLP-1 Receptor

B. P. Cary, P. Zhao, T. T. Truong, S. J. Piper, M. J. Belousoff, R. Danev, P. M. Sexton, D. Wootten, S. H. Gellman

This study investigates how peptide agonist conformational plasticity influences GLP-1R activation through structural and functional analysis.

bioRxiv · Feb 24, 2021Pharmacology & Toxicology

Structure and dynamics of semaglutide and taspoglutide bound GLP-1R-Gs complexes

X. Zhang, M. J. Belousoff, Y.-L. Liang, R. Danev, P. M. Sexton, D. Wootten

This study determines cryo-EM structures of GLP-1R-Gs complexes bound with semaglutide and taspoglutide, revealing similar peptide binding modes but distinct 3D motions compared to GLP-1.

bioRxiv · Jan 12, 2021Biochemistry

Evolving cryo-EM structural approaches for GPCR drug discovery

X. Zhang, R. M. Johnson, I. Drulyte, L. Yu, A. Kotecha, R. Danev, D. Wootten, P. M. Sexton, M. J. Belousoff

This study validates stable GPCR:Gs complexes without Nb35 stabilizers and evaluates 200kV vs 300kV cryo-EM imaging for drug discovery.

bioRxiv · Jan 11, 2021Biochemistry

Routine sub-2.5 A cryo-EM structure determination of B-family G protein-coupled receptors

R. Danev, M. Belousoff, Y.-L. Liang, X. Zhang, D. Wootten, P. M. Sexton

This study systematically optimizes cryo-EM parameters to routinely determine class B1 GPCR structures at better than 2.5 Å resolution.

bioRxiv · Aug 21, 2020Biophysics

Differential GLP-1R binding and activation by peptide and non-peptide agonists

X. Zhang, M. J. Belousoff, P. Zhao, A. J. Kooistra, T. T. Truong, S. Y. Ang, C. R. Underwood, T. Egebjerg, P. Senel, G. D. Stewart, Y.-L. Liang, A. Glukhova, H. Venugopal, A. Christopoulos, S. G. Furness, , D. Wootten

The paper compares the binding and activation of the GLP-1 receptor by peptide and non-peptide agonists, revealing structural and functional differences that inform drug design.

bioRxiv · Aug 16, 2020Pharmacology & Toxicology

Pharmacological insights into safety and efficacy determinants for the development of adenosine receptor biased agonists in the treatment of heart failure

P. Rueda, J. Merlin, S. Chimenti, M. Feletou, J. Paysant, P. J. White, A. Christopoulos, P. M. Sexton, R. J. Summers, W. N. Charman, L. T. May, C. J. Langmead

This study compares the safety and efficacy of A1R agonists, showing that biased agonism away from Ca2+ influx relative to cAMP improves safety but may not guarantee efficacy in heart failure.

bioRxiv · Jul 22, 2020Pharmacology & Toxicology

Crystal structure of the M5 muscarinic acetylcholine receptor

Z. Vuckovic, P. R. Gentry, A. E. Berizzi, K. Hirata, S. Varghese, G. Thompson, E. T. van der Westhuizen, W. A. C. Burger, R. Rahmani, C. Valant, C. J. Langmead, C. W. Lindsley, J. Baell, A. B. Tobin, P. M. Sexton, , D. M. Thal

The paper reports the crystal structure of the human M5 muscarinic acetylcholine receptor bound to tiotropium, revealing structural differences that inform ligand selectivity design.

bioRxiv · Aug 14, 2019Pharmacology & Toxicology