β-Arrestin-dependent and -independent endosomal G protein activation by the vasopressin type 2 receptor

Autor: Carole Daly, Akim Abdul Guseinov, Hyunggu Hahn, Adam Wright, Irina G Tikhonova, Alex Rojas Bie Thomsen, Bianca Plouffe

Publikováno v: eLife, Vol 12 (2023)

The vasopressin type 2 receptor (V2R) is an essential G protein-coupled receptor (GPCR) in renal regulation of water homeostasis. Upon stimulation, the V2R activates Gαs and Gαq/11, which is followed by robust recruitment of β-arrestins and recept

Externí odkaz: https://doaj.org/article/548a4b2b757c44c993214c3aaa268821

Steered molecular dynamics simulations reveal critical residues for (un)binding of substrates, inhibitors and a product to the malarial M1 aminopeptidase.

Autor: Daniel S Moore, Conor Brines, Heather Jewhurst, John P Dalton, Irina G Tikhonova

Publikováno v: PLoS Computational Biology, Vol 14, Iss 10, p e1006525 (2018)

Malaria is a life-threatening disease spread by mosquitoes. Plasmodium falciparum M1 alanyl aminopeptidase (PfM1-AAP) is a promising target for the treatment of malaria. The recently solved crystal structures of PfM1-AAP revealed that the buried acti

Externí odkaz: https://doaj.org/article/f9d92695a43c4582990a4c1205c5c535

Oxidation modulates LINGO2-induced inactivation of large conductance, Ca2+-activated potassium channels

Autor: Srikanth Dudem, Pei Xin Boon, Nicholas Mullins, Heather McClafferty, Michael J. Shipston, Richard D.A. Wilkinson, Ian Lobb, Gerard P. Sergeant, Keith D. Thornbury, Irina G. Tikhonova, Mark A. Hollywood

Publikováno v: Dudem, S, Boon, P X, Mullins, N, McClafferty, H, Shipston, M J, Wilkinson, R D A, Lobb, I, Sergeant, G P, Thornbury, K D, Tikhonova, I G & Hollywood, M A 2023, ' Oxidation modulates LINGO2-induced inactivation of large conductance, Ca2 +-activated potassium channels ', The Journal of Biological Chemistry, vol. 299, no. 3, 102975 . https://doi.org/10.1016/j.jbc.2023.102975

Ca 2+ and voltage-activated K + (BK) channels are ubiquitous ion channels that can be modulated by accessory proteins, including β, γ, and LINGO1 BK subunits. In this study, we utilized a combination of site-directed mutagenesis, patch clamp electr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1495f97e0c80f1b57baf1814ccbfd671
https://pure.qub.ac.uk/en/publications/5d33d0e5-f1db-494a-a1d1-cd824ca00826

Probe Confined Dynamic Mapping for G Protein-Coupled Receptor Allosteric Site Prediction

Autor: George Chalhoub, Amandeep Kaur Gill, Antonella Ciancetta, Tianyi Ding, Dmitry S. Karlov, Irina G. Tikhonova, Peter J. McCormick

Publikováno v: ACS Central Science
Ciancetta, A, Gill, A K, Ding, T, Karlov, D S, Chalhoub, G, McCormick, P J & Tikhonova, I G 2021, ' Probe Confined Dynamic Mapping for G Protein-Coupled Receptor Allosteric Site Prediction ', ACS Central Science . https://doi.org/10.1021/acscentsci.1c00802
ACS Central Science, Vol 7, Iss 11, Pp 1847-1862 (2021)

Targeting G protein-coupled receptors (GPCRs) through allosteric sites offers advantages over orthosteric sites in identifying drugs with increased selectivity and potentially reduced side effects. In this study, we developed a probe confined dynamic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a627d63429e88cc204d44ba72bde3d21
http://europepmc.org/articles/PMC8614102

Investigating the structure–activity relationship of 1,2,4-triazine G-protein-coupled receptor 84 (GPR84) antagonists

Autor: Amit Mahindra, Laura Jenkins, Sara Marsango, Mark Huggett, Margaret Huggett, Lindsay Robinson, Jonathan Gillespie, Muralikrishnan Rajamanickam, Angus Morrison, Stuart McElroy, Irina G. Tikhonova, Graeme Milligan, Andrew G. Jamieson

Publikováno v: Mahindra, A, Jenkins, L, Marsango, S, Huggett, M, Huggett, M, Robinson, L, Gillespie, J, Rajamanickam, M, Morrison, A, McElroy, S, Tikhonova, I G, Milligan, G & Jamieson, A G 2022, ' Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists ', Journal of Medicinal Chemistry, vol. 65, no. 16, pp. 11270–11290 . https://doi.org/10.1021/acs.jmedchem.2c00804

G-protein-coupled receptor 84 (GPR84) is a proinflammatory orphan G-protein-coupled receptor implicated in several inflammatory and fibrotic diseases. Several agonist and antagonist ligands have been developed that target GPR84; however, a noncompeti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f04505f33b851dac9c2727e94441dc5
https://eprints.gla.ac.uk/275398/1/275398.pdf