Christopher Draper-Joyce

Structural Insights into the Unique Modes of Relaxin-Binding and Tethered-Agonist Mediated Activation of RXFP1 and RXFP2

Ashish Sethi, Shoni Bruell, Tim Ryan, Fei Yan, Mohammad Hossein Tanipour, Yee-Foong Mok, Chris Draper-Joyce, Yogesh Khandokar, Riley D Metcalfe, Michael DW Griffin, Daniel J Scott, Mohammad Akhter Hossain, Emma J Petrie, Ross AD Bathgate, Paul R Gooley

Journal article  |  2021  |  JOURNAL OF MOLECULAR BIOLOGY

Our poor understanding of the mechanism by which the peptide-hormone H2 relaxin activates its G protein coupled receptor, RXFP1 an..

Positive allosteric mechanisms of adenosine A(1) receptor-mediated analgesia

Christopher J Draper-Joyce, Rebecca Bhola, Jinan Wang, Apurba Bhattarai, Anh TN Nguyen, India Cowie-Kent, Kelly O'Sullivan, Ling Yeong Chia, Hariprasad Venugopal, Celine Valant, David M Thal, Denise Wootten, Nicolas Panel, Jens Carlsson, Macdonald J Christie, Paul J White, Peter Scammells, Lauren T May, Patrick M Sexton, Radostin Danev, et al.

Journal article  |  2021  |  NATURE

The adenosine A1 receptor (A1R) is a promising therapeutic target for non-opioid analgesic agents to treat neuropathic pain1,2. Ho..

Conformational Transitions and the Activation of Heterotrimeric G Proteins by G Protein-Coupled Receptors

Christopher Draper-Joyce, Sebastian George Barton Furness

Journal article  |  2019  |  ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE

G protein-coupled receptors (GPCRs) are particularly attractive targets for therapeutic pharmaceuticals. This is because they are ..

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole

Carmen Klein Herenbrink, Ravi Verma, Herman D Lim, Anitha Kopinathan, Alastair Keen, Jerem Y Shonberg, Christopher JD Raper-Joyce, Peter J Scammells, Arthur Christopoulos, Jonathan A Javitch, Ben Capuancy, Lei Shi, J Robert Lane

Journal article  |  2019  |  ACS CHEMICAL BIOLOGY

Partial agonists of the dopamine D2 receptor (D2R) have been developed to treat the symptoms of schizophrenia without causing the ..

Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-((trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity at the Dopamine D-2 Receptor

Anitha Kopinathan, Christopher Draper-Joyce, Monika Szabo, Arthur Christopoulos, Peter J Scammells, J Robert Lane, Ben Capuano

Journal article  |  2019  |  JOURNAL OF MEDICINAL CHEMISTRY

SB269652 (1) is a negative allosteric modulator of the dopamine D2 receptor. Herein, we present the design, synthesis, and pharmac..

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..

Recent advances in the determination of G protein-coupled receptor structures

David M Thal, Ziva Vuckovic, Christopher J Draper-Joyce, Yi-Lynn Liang, Alisa Glukhova, Arthur Christopoulos, Patrick M Sexton

Journal article  |  2018  |  CURRENT OPINION IN STRUCTURAL BIOLOGY

G protein-coupled receptors (GPCRs) are the largest superfamily of cell surface receptor proteins and are important drug targets f..

Structure of the adenosine-bound human adenosine A(1) receptor-G(i) complex

Christopher J Draper-Joyce, Maryam Khoshouei, David M Thal, Yi-Lynn Liang, Anh TN Nguyen, Sebastian GB Furness, Hariprasad Venugopal, Jo-Anne Baltos, Juergen M Plitzko, Radostin Danev, Wolfgang Baumeister, Lauren T May, Denise Wootten, Patrick M Sexton, Alisa Glukhova, Arthur Christopoulos

Journal article  |  2018  |  NATURE

The class A adenosine A1 receptor (A1R) is a G-protein-coupled receptor that preferentially couples to inhibitory Gi/o heterotrime..

Strength in numbers-an arrestin interaction code

Christopher J Draper-Joyce, Arthur Christopoulos

Journal article  |  2018  |  NATURE STRUCTURAL & MOLECULAR BIOLOGY

Activation signals from GPCRs, the largest receptor family, are transmitted to heterotrimeric G proteins and arrestins, and can be..