Patrick Sexton

Restoring Agonist Function at a Chemogenetically Modified M-1 Muscarinic Acetylcholine Receptor

Elham Khajehali, Sophie Bradley, Emma T van der Westhuizen, Colin Molloy, Celine Valant, Lisa Finlayson, Craig W Lindsley, Patrick M Sexton, Andrew B Tobin, Arthur Christopoulos

Journal article  |  2020  |  ACS CHEMICAL NEUROSCIENCE

Designer receptors exclusively activated by designer drugs (DREADDs) have been successfully employed to activate signaling pathway..

Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.

Xin Zhang, Matthew J Belousoff, Peishen Zhao, Albert J Kooistra, Tin T Truong, Sheng Yu Ang, Christina Rye Underwood, Thomas Egebjerg, Petr Šenel, Gregory D Stewart, Yi-Lynn Liang, Alisa Glukhova, Hari Venugopal, Arthur Christopoulos, Sebastian GB Furness, Laurence J Miller, Steffen Reedtz-Runge, Christopher J Langmead, David E Gloriam, Radostin Danev, et al.

Journal article  |  2020  |  Mol Cell

Peptide drugs targeting class B1 G-protein-coupled receptors (GPCRs) can treat multiple diseases; however, there remains substanti..

Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M(1)Muscarinic Acetylcholine Receptor

Manuela Jorg, Elham Khajehali, Emma T van der Westhuizen, KH C. Choy, David M Shackleford, Andrew B Tobin, Patrick M Sexton, Celine Valant, Ben Capuano, Arthur Christopoulos, Peter J Scammells

Journal article  |  2020  |  CHEMMEDCHEM

This study investigated the structure-activity relationships of 4-phenylpyridin-2-one and 6-phenylpyrimidin-4-one M1 muscarinic ac..

Structure and dynamics of the active Gs-coupled human secretin receptor.

Maoqing Dong, Giuseppe Deganutti, Sarah J Piper, Yi-Lynn Liang, Maryam Khoshouei, Matthew J Belousoff, Kaleeckal G Harikumar, Christopher A Reynolds, Alisa Glukhova, Sebastian GB Furness, Arthur Christopoulos, Radostin Danev, Denise Wootten, Patrick M Sexton, Laurence J Miller

Journal article  |  2020  |  Nat Commun

The class B secretin GPCR (SecR) has broad physiological effects, with target potential for treatment of metabolic and cardiovascu..

In the Loop: Extrastriatal Regulation of Spiny Projection Neurons by GPR52

Daisy L Spark, Miaomiao Mao, Sherie Ma, Mohsin Sarwar, Cameron J Nowell, David M Shackleford, Patrick M Sexton, Jess Nithianantharajah, Gregory D Stewart, Christopher J Langmead

Journal article  |  2020  |  ACS CHEMICAL NEUROSCIENCE

GPR52 is a Gαs-coupled orphan receptor identified as a putative target for the treatment of schizophrenia. The unique expression a..

Automatic local resolution-based sharpening of cryo-EM maps

Erney Ramirez-Aportela, Jose Luis Vilas, Alisa Glukhova, Roberto Melero, Pablo Conesa, Marta Martinez, David Maluenda, Javier Mota, Amaya Jimenez, Javier Vargas, Roberto Marabini, Patrick M Sexton, Jose Maria Carazo, Carlos Oscar S Sorzano

Journal article  |  2020  |  BIOINFORMATICS

MOTIVATION: Recent technological advances and computational developments have allowed the reconstruction of Cryo-Electron Microsco..

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M-1 mAChR: The Determinants of Allosteric Activity

Manuela Jorg, Emma T van der Westhuizen, Elham Khajehali, Wessel AC Burger, Jonathan M White, Kwok HC Choy, Andrew B Tobin, Patrick M Sexton, Celine Valant, Ben Capuano, Arthur Christopoulos, Peter J Scammells

Journal article  |  2019  |  ACS CHEMICAL NEUROSCIENCE

Targeting allosteric sites of the M1 muscarinic acetylcholine receptor (mAChR) is an enticing approach to overcome the lack of rec..

Expression and activity of the calcitonin receptor family in a sample of primary human high-grade gliomas

Anna Ostrovskaya, Caroline Hick, Dana S Hutchinson, Brett W Stringer, Peter J Wookey, Denise Wootten, Patrick M Sexton, Sebastian GB Furness

Journal article  |  2019  |  BMC CANCER

BACKGROUND: Glioblastoma (GBM) is the most common and aggressive type of primary brain cancer. With median survival of less than 1..

Rules of Engagement: GPCRs and G Proteins

Alisa Glukhova, Christopher J Draper-Joyce, Roger K Sunahara, Arthur Christopoulos, Denise Wootten, Patrick M Sexton

Journal article  |  2018  |  ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE

G protein-coupled receptors (GPCRs) are a key drug target class. They account for over one-third of current pharmaceuticals, and b..

Dominant Negative G Proteins Enhance Formation and Purification of Agonist-GPCR-G Protein Complexes for Structure Determination

Yi-Lynn Liang, Peishen Zhao, Christopher Draper-Joyce, Jo-Anne Baltos, Alisa Glukhova, Tin T Truong, Lauren T May, Arthur Christopoulos, Denise Wootten, Patrick M Sexton, Sebastian GB Furness

Journal article  |  2018  |  ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE

Advances in structural biology have yielded exponential growth in G protein-coupled receptor (GPCR) structure solution. Nonetheles..