Search Results - "Furness, G"

Phase-plate cryo-EM structure of a class B GPCR–G-protein complex by Liang, Yi-Lynn, Khoshouei, Maryam, Radjainia, Mazdak, Zhang, Yan, Glukhova, Alisa, Tarrasch, Jeffrey, Thal, David M., Furness, Sebastian G. B., Christopoulos, George, Coudrat, Thomas, Danev, Radostin, Baumeister, Wolfgang, Miller, Laurence J., Christopoulos, Arthur, Kobilka, Brian K., Wootten, Denise, Skiniotis, Georgios, Sexton, Patrick M.

“…Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases, such as osteoporosis, diabetes and obesity. Here we report the…”
Get full text

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex by Liang, Yi-Lynn, Khoshouei, Maryam, Glukhova, Alisa, Furness, Sebastian G. B., Zhao, Peishen, Clydesdale, Lachlan, Koole, Cassandra, Truong, Tin T., Thal, David M., Lei, Saifei, Radjainia, Mazdak, Danev, Radostin, Baumeister, Wolfgang, Wang, Ming-Wei, Miller, Laurence J., Christopoulos, Arthur, Sexton, Patrick M., Wootten, Denise

“…The structure of the glucagon-like peptide 1 receptor (GLP-1R) with its biased agonist exendin-P5 sheds light on both receptor activation and the mechanism of…”
Get full text

Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity by Mobbs, Jesse I, Belousoff, Matthew J, Harikumar, Kaleeckal G, Piper, Sarah J, Xu, Xiaomeng, Furness, Sebastian G B, Venugopal, Hari, Christopoulos, Arthur, Danev, Radostin, Wootten, Denise, Thal, David M, Miller, Laurence J, Sexton, Patrick M

“…G protein-coupled receptors (GPCRs) are critical regulators of cellular function acting via heterotrimeric G proteins as their primary transducers with…”
Get full text

Activation of the GLP-1 receptor by a non-peptidic agonist by Zhao, Peishen, Liang, Yi-Lynn, Belousoff, Matthew J., Deganutti, Giuseppe, Fletcher, Madeleine M., Willard, Francis S., Bell, Michael G., Christe, Michael E., Sloop, Kyle W., Inoue, Asuka, Truong, Tin T., Clydesdale, Lachlan, Furness, Sebastian G. B., Christopoulos, Arthur, Wang, Ming-Wei, Miller, Laurence J., Reynolds, Christopher A., Danev, Radostin, Sexton, Patrick M., Wootten, Denise

“…Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases, including diabetes and obesity 1 . Structures of active receptors…”
Get full text

Structure and dynamics of the active Gs-coupled human secretin receptor by Dong, Maoqing, Deganutti, Giuseppe, Piper, Sarah J., Liang, Yi-Lynn, Khoshouei, Maryam, Belousoff, Matthew J., Harikumar, Kaleeckal G., Reynolds, Christopher A., Glukhova, Alisa, Furness, Sebastian G. B., Christopoulos, Arthur, Danev, Radostin, Wootten, Denise, Sexton, Patrick M., Miller, Laurence J.

“…The class B secretin GPCR (SecR) has broad physiological effects, with target potential for treatment of metabolic and cardiovascular disease. Molecular…”
Get full text

Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling by Harikumar, Kaleeckal G, Zhao, Peishen, Cary, Brian P, Xu, Xiaomeng, Desai, Aditya J, Dong, Maoqing, Mobbs, Jesse I, Toufaily, Chirine, Furness, Sebastian G B, Christopoulos, Arthur, Belousoff, Matthew J, Wootten, Denise, Sexton, Patrick M, Miller, Laurence J

“…Development of optimal therapeutics for disease states that can be associated with increased membrane cholesterol requires better molecular understanding of…”
Get full text

Prolonged calcitonin receptor signaling by salmon, but not human calcitonin, reveals ligand bias by Andreassen, Kim Vietz, Hjuler, Sara Toftegaard, Furness, Sebastian G, Sexton, Patrick M, Christopoulos, Arthur, Nosjean, Olivier, Karsdal, Morten Asser, Henriksen, Kim

“…Salmon calcitonin (sCT) and human calcitonin (hCT) are pharmacologically distinct. However, the reason for the differences is unclear. Here we analyze the…”
Get full text

Structure and Dynamics of Adrenomedullin Receptors AM1 and AM2 Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins by Liang, Yi-Lynn, Belousoff, Matthew J, Fletcher, Madeleine M, Zhang, Xin, Khoshouei, Maryam, Deganutti, Giuseppe, Koole, Cassandra, Furness, Sebastian G. B, Miller, Laurence J, Hay, Debbie L, Christopoulos, Arthur, Reynolds, Christopher A, Danev, Radostin, Wootten, Denise, Sexton, Patrick M

“…Adrenomedullin (AM) and calcitonin gene-related peptide (CGRP) receptors are critically important for metabolism, vascular tone, and inflammatory response. AM…”
Get full text

Expression and activity of the calcitonin receptor family in a sample of primary human high-grade gliomas by Ostrovskaya, Anna, Hick, Caroline, Hutchinson, Dana S, Stringer, Brett W, Wookey, Peter J, Wootten, Denise, Sexton, Patrick M, Furness, Sebastian G B

“…Glioblastoma (GBM) is the most common and aggressive type of primary brain cancer. With median survival of less than 15 months, identification and validation…”
Get full text

Dominant Negative G Proteins Enhance Formation and Purification of Agonist-GPCR‑G Protein Complexes for Structure Determination by Liang, Yi-Lynn, Zhao, Peishen, Draper-Joyce, Christopher, Baltos, Jo-Anne, Glukhova, Alisa, Truong, Tin T, May, Lauren T, Christopoulos, Arthur, Wootten, Denise, Sexton, Patrick M, Furness, Sebastian G. B

“…Advances in structural biology have yielded exponential growth in G protein-coupled receptor (GPCR) structure solution. Nonetheless, the instability of fully…”
Get full text

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics by Cook, A E, Mistry, S N, Gregory, K J, Furness, S G B, Sexton, P M, Scammells, P J, Conigrave, A D, Christopoulos, A, Leach, K

“…Background and Purpose Clinical use of cinacalcet in hyperparathyroidism is complicated by its tendency to induce hypocalcaemia, arising partly from activation…”
Get full text

Receptor Activity-Modifying Proteins Differentially Modulate the G Protein-Coupling Efficiency of Amylin Receptors by Morfis, Maria, Tilakaratne, Nanda, Furness, Sebastian G. B, Christopoulos, George, Werry, Tim D, Christopoulos, Arthur, Sexton, Patrick M

“…Receptor activity-modifying proteins (RAMPs) 1, 2, and 3 are prototypic G protein-coupled receptor accessory proteins that can alter not only receptor…”
Get full text

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery by Harikumar, Kaleeckal G, Wootten, Denise, Pinon, Delia I, Koole, Cassandra, Ball, Alicja M, Furness, Sebastian G. B, Graham, Bim, Dong, Maoqing, Christopoulos, Arthur, Miller, Laurence J, Sexton, Patrick M

“…The glucagon-like peptide-1 receptor (GLP-1R) is a family B G protein-coupled receptor and an important drug target for the treatment of type II diabetes, with…”
Get full text

Dopamine and ghrelin receptor co‐expression and interaction in the spinal defecation centers by Furness, John B., Pustovit, Ruslan V., Syder, Andrew J., Ringuet, Mitchell T., Yoo, Eun Ji, Fanjul, Andrea, Wykosky, Jill, Fothergill, Linda J., Whitfield, Emily A., Furness, Sebastian G. B.

“…Background Dopamine receptor 2 (DRD2) and ghrelin receptor (GHSR1a) agonists both stimulate defecation by actions at the lumbosacral defecation center…”
Get full text

Dianthin-30 or gelonin versus monomethyl auristatin E, each configured with an anti-calcitonin receptor antibody, are differentially potent in vitro in high-grade glioma cell lines derived from glioblastoma by Gilabert-Oriol, Roger, Furness, Sebastian G. B., Stringer, Brett W., Weng, Alexander, Fuchs, Hendrik, Day, Bryan W., Kourakis, Angela, Boyd, Andrew W., Hare, David L., Thakur, Mayank, Johns, Terrance G., Wookey, Peter J.

“…We have reported that calcitonin receptor (CTR) is widely expressed in biopsies from the lethal brain tumour glioblastoma by malignant glioma and brain…”
Get full text

TrkB Agonist LM22A-4 Increases Oligodendroglial Populations During Myelin Repair in the Corpus Callosum by Nguyen, Huynh T H, Wood, Rhiannon J, Prawdiuk, Alexa R, Furness, Sebastian G B, Xiao, Junhua, Murray, Simon S, Fletcher, Jessica L

“…The neurotrophin, brain-derived neurotrophic factor (BDNF) promotes central nervous system (CNS) myelination during development and after injury. This is…”
Get full text

The Molecular Control of Calcitonin Receptor Signaling by dal Maso, Emma, Glukhova, Alisa, Zhu, Yue, Garcia-Nafria, Javier, Tate, Christopher G, Atanasio, Silvia, Reynolds, Christopher A, Ramírez-Aportela, Erney, Carazo, Jose-Maria, Hick, Caroline A, Furness, Sebastian G. B, Hay, Debbie L, Liang, Yi-Lynn, Miller, Laurence J, Christopoulos, Arthur, Wang, Ming-Wei, Wootten, Denise, Sexton, Patrick M

“…The calcitonin receptor (CTR) is a class B G protein-coupled receptor (GPCR) that responds to the peptide hormone calcitonin (CT). CTs are clinically approved…”
Get full text

Antibiotic or induction agent? Another problem from a possible solution by Quinn, L., Furness, G.

Get full text

Building the case for the calcitonin receptor as a viable target for the treatment of glioblastoma by Gupta, Pragya, Furness, Sebastian G. B., Bittencourt, Lucas, Hare, David L., Wookey, Peter J.

“…Researchers are actively seeking novel targeted therapies for the brain tumour glioblastoma (GBM) as the mean survival is less than 15 months. Here we discuss…”
Get full text

Discovery of a Positive Allosteric Modulator of Cholecystokinin Action at CCK1R in Normal and Elevated Cholesterol by Harikumar, Kaleeckal G, Coudrat, Thomas, Desai, Aditya J, Dong, Maoqing, Dengler, Daniela G, Furness, Sebastian G B, Christopoulos, Arthur, Wootten, Denise, Sergienko, Eduard A, Sexton, Patrick M, Miller, Laurence J

“…Drugs useful in prevention/treatment of obesity could improve health. Cholecystokinin (CCK) is a key regulator of appetite, working through the type 1 CCK…”
Get full text