Structural Requirements for the Activation of the Human Growth Hormone Secretagogue Receptor by Peptide and Nonpeptide Secretagogues

Autor: Dennis C. Dean, Donna L. Hreniuk, Karen K. McKee, Carina P. Tan, Ravi P. Nargund, Lht Van der Ploeg, JR Tata, Kristine Prendergast, Andrew D. Howard, Scott D. Feighner, Arthur A. Patchett, Oksana C. Palyha, JW Woods, Roy G. Smith, D Underwood

Publikováno v: Molecular Endocrinology. 12:137-145

Antibodies raised against an intracellular and extracellular domain of the GH secretagogue receptor (GHS-R) confirmed that its topological orientation in the lipid bilayer is as predicted for G protein-coupled receptors with seven transmembrane domai

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56d56a687a83b3f530fe4e6240d6ee0c
https://doi.org/10.1210/mend.12.1.0051

Down-regulation of the Notch pathway mediated by a gamma-secretase inhibitor induces anti-tumour effects in mouse models of T-cell leukaemia

Autor: J, Tammam, C, Ware, C, Efferson, J, O'Neil, S, Rao, X, Qu, J, Gorenstein, M, Angagaw, H, Kim, C, Kenific, K, Kunii, K J, Leach, G, Nikov, J, Zhao, X, Dai, J, Hardwick, M, Scott, C, Winter, L, Bristow, C, Elbi, J F, Reilly, T, Look, G, Draetta, Lht, Van der Ploeg, N E, Kohl, P R, Strack, P K, Majumder

Publikováno v: British journal of pharmacology. 158(5)

gamma-Secretase inhibitors (GSIs) block NOTCH receptor cleavage and pathway activation and have been under clinical evaluation for the treatment of malignancies such as T-cell acute lymphoblastic leukaemia (T-ALL). The ability of GSIs to decrease T-A

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::3bda9111cf4fe1ceb0096775ff848449
https://pubmed.ncbi.nlm.nih.gov/19775282

Current Mechanistic and Pharmacodynamic Understanding of Melanocortin-4 Receptor Activation.

Autor: Sharma S; Rhythm Pharmaceuticals, Boston, MA 02116, USA. ssharma@rhythmtx.com., Garfield AS; Rhythm Pharmaceuticals, Boston, MA 02116, USA. agarfield@rhythmtx.com., Shah B; Rhythm Pharmaceuticals, Boston, MA 02116, USA. bshah@rhythmtx.com., Kleyn P; Rhythm Pharmaceuticals, Boston, MA 02116, USA. pkleyn@rhythmtx.com., Ichetovkin I; Rhythm Pharmaceuticals, Boston, MA 02116, USA. ichetov@rhythmtx.com., Moeller IH; Rhythm Pharmaceuticals, Boston, MA 02116, USA. imoeller@rhythmtx.com., Mowrey WR; Rhythm Pharmaceuticals, Boston, MA 02116, USA. bmowrey@rhythmtx.com., Van der Ploeg LHT; Rhythm Pharmaceuticals, Boston, MA 02116, USA. lvanderploeg@rhythmtx.com.

Publikováno v: Molecules (Basel, Switzerland) [Molecules] 2019 May 16; Vol. 24 (10). Date of Electronic Publication: 2019 May 16.

Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency.

Autor: Collet TH; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom; Service of Endocrinology, Diabetes and Metabolism, University Hospital of Lausanne, Lausanne, 1011, Switzerland., Dubern B; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France; Sorbonne Université, UPMC Univ Paris 06, UMR_S 1166, INSERM, F-75013, Paris, France., Mokrosinski J; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom., Connors H; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA., Keogh JM; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom., Mendes de Oliveira E; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom., Henning E; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom., Poitou-Bernert C; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France; Sorbonne Université, UPMC Univ Paris 06, UMR_S 1166, INSERM, F-75013, Paris, France., Oppert JM; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France; Sorbonne Université, UPMC Univ Paris 06, UMR_S 1166, INSERM, F-75013, Paris, France., Tounian P; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France; Sorbonne Université, UPMC Univ Paris 06, UMR_S 1166, INSERM, F-75013, Paris, France., Marchelli F; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France., Alili R; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France; Sorbonne Université, UPMC Univ Paris 06, UMR_S 1166, INSERM, F-75013, Paris, France., Le Beyec J; Assistance Publique, Hôpital Pitié-Salpêtrière-Charles Foix, Department of Endocrine and Oncological Biochemistry, F-75651, Paris, France; Sorbonne Université, UPMC Univ, Paris 06, France; Inserm UMR1149, F-75890, Paris, France., Pépin D; Assistance Publique, Hôpital Pitié-Salpêtrière-Charles Foix, Department of Endocrine and Oncological Biochemistry, F-75651, Paris, France., Lacorte JM; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France; Sorbonne Université, UPMC Univ Paris 06, UMR_S 1166, INSERM, F-75013, Paris, France; Assistance Publique, Hôpital Pitié-Salpêtrière-Charles Foix, Department of Endocrine and Oncological Biochemistry, F-75651, Paris, France., Gottesdiener A; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA., Bounds R; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom., Sharma S; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA., Folster C; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA., Henderson B; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA., O'Rahilly S; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom., Stoner E; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA., Gottesdiener K; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA., Panaro BL; Lunenfeld-Tanenbaum Research Institute, Department of Medicine, Mt. Sinai Hospital, University of Toronto, Toronto, Ontario, Canada; Vanderbilt University, Department of Molecular Physiology and Biophysics, Nashville, TN, 37235, USA., Cone RD; Vanderbilt University, Department of Molecular Physiology and Biophysics, Nashville, TN, 37235, USA; Life Sciences Institute and Department of Molecular and Integrative Physiology, University of Michigan, Ann Arbor, MI, 48105, USA., Clément K; Institute of Cardiometabolism and Nutrition (ICAN), Assistance Publique-Hôpitaux de Paris, Trousseau and Pitié-Salpêtrière Hospitals, F-75013, Paris, France; Sorbonne Université, UPMC Univ Paris 06, UMR_S 1166, INSERM, F-75013, Paris, France. Electronic address: karine.clement@aphp.fr., Farooqi IS; University of Cambridge Metabolic Research Laboratories and NIHR Cambridge Biomedical Research Centre, Wellcome Trust-MRC Institute of Metabolic Science, Box 289, Addenbrooke's Hospital, Hills Road, Cambridge, CB2 0QQ, United Kingdom. Electronic address: isf20@cam.ac.uk., Van der Ploeg LHT; Rhythm Pharmaceuticals, 500 Boylston Street, Boston, MA, 02116, USA. Electronic address: lvanderploeg@rhythmtx.com.

Publikováno v: Molecular metabolism [Mol Metab] 2017 Oct; Vol. 6 (10), pp. 1321-1329. Date of Electronic Publication: 2017 Jul 08.