STABILISING G PROTEIN-COUPLED RECEPTORS FOR DRUG DISCOVERY

High yield expression and purification of full-length Neurotensin with pyroglutamate modification

Kazem Asadollahi, Katherine Huang, Fei Yan, Lazarus A de Zhang, Daniel J Scott, Paul R Gooley

2022-12-28

Neurotensin (NT) is a 13-residue endogenous peptide found in mammals, with neurotransmission and hormonal roles in the central ner..

Crystal structure of the alpha(1B)-adrenergic receptor reveals molecular determinants of selective ligand recognition

Mattia Deluigi, Lena Morstein, Matthias Schuster, Christoph Klenk, Lisa Merklinger, Riley R Cridge, Lazarus A de Zhang, Alexander Klipp, Santiago Vacca, Tasneem M Vaid, Peer RE Mittl, Pascal Egloff, Stefanie A Eberle, Oliver Zerbe, David K Chalmers, Daniel J Scott, Andreas Pluckthun

2022-01-19

α-adrenergic receptors (αARs) are G protein-coupled receptors that regulate vital functions of the cardiovascular and nervous syst..

INPHARMA-Based Determination of Ligand Binding Modes at alpha(1)-Adrenergic Receptors Explains the Molecular Basis of Subtype Selectivity

Tasneem M Vaid, David K Chalmers, Daniel J Scott, Paul R Gooley

2020-08-18

The structural poses of ligands that bind weakly to protein receptors are challenging to define. In this work we have studied liga..

Probing the correlation between ligand efficacy and conformational diversity at the ?(1A)-adrenoreceptor reveals allosteric coupling of its microswitches

Feng-Jie Wu, Lisa M Williams, Alaa Abdul-Ridha, Avanka Gunatilaka, Tasneem M Vaid, Martina Kocan, Alice R Whitehead, Michael DW Griffin, Ross AD Bathgate, Daniel J Scott, Paul R Gooley

2020-05-22

G protein–coupled receptors (GPCRs) use a series of conserved microswitches to transmit signals across the cell membrane via an al..

α_1A-adrenoceptor inverse agonists and agonists modulate receptor signalling through a conformational selection mechanism

Feng-Jie Wu, Lisa M Williams, Alaa Abdul-Ridha, Avanka Gunatilaka, Tasneem M Vaid, Martina Kocan, Alice R Whitehead, Michael DW Griffin, Ross AD Bathgate, Daniel J Scott, Paul R Gooley

2019-12-07

<jats:title>Abstract</jats:title><jats:p>G-Protein Coupled Receptors (GPCRs) transmit signals across the cell membrane via an allo..

Diazepam is not a direct allosteric modulator of alpha(1)-adrenoceptors, but modulates receptor signaling by inhibiting phosphodiesterase-4

Lisa M Williams, Xiaoji He, Tasneem M Vaid, Alaa Abdul-Ridha, Alice R Whitehead, Paul R Gooley, Ross AD Bathgate, Spencer J Williams, Daniel J Scott

2019-02-01

α1A- and α1B-adrenoceptors (ARs) are G protein-coupled receptors (GPCRs) that are activated by adrenaline and noradrenaline to mod..

Expression and Purification of a Functional E. coli (CH3)-C-13-Methionine-Labeled Thermostable Neurotensin Receptor 1 Variant for Solution NMR Studies

Fabian Bumbak, Ross AD Bathgate, Daniel J Scott, Paul R Gooley

2019-01-01

Escherichia coli (E. coli) is the most widely used expression host for recombinant proteins due to high expression yields and stra..

Optimization and (CH3)-C-13 methionine labeling of a signaling competent neurotensin receptor 1 variant for NMR studies

Fabian Bumbak, Alastair C Keen, Natalie J Gunn, Paul R Gooley, Ross AD Bathgate, Daniel J Scott

2018-06-01

Neurotensin is a 13-residue peptide that acts as a neuromodulator of classical neurotransmitters such as dopamine and glutamate in..

Determinants of Ligand Subtype-Selectivity at alpha(1A)-Adrenoceptor Revealed Using Saturation Transfer Difference (STD) NMR

Kelvin J Yong, Tasneem M Vaid, Patrick J Shilling, Feng-Jie Wu, Lisa M Williams, Mattia Deluig, Andreas Plueckthun, Ross AD Bathgate, Paul R Gooley, Daniel J Scott

2018-04-01

α1A- and α1B-adrenoceptors (α1A-AR and α1B-AR) are closely related G protein-coupled receptors (GPCRs) that modulate the cardiovas..