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Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.

Autor: Southall SM; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom., Banerjee J; Syngene International, Biocon Park, Bommasandra, Bangalore, Karnataka 560099, India., Brown J; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom., Butkovic K; Selvita d.o.o., Prilaz aruna Filipovića 29, 10000 Zagreb, Croatia., Cansfield AD; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom., Cansfield JE; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom., Congreve MS; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom., Cseke G; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom., Deflorian F; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom., Hunjadi MP; Selvita d.o.o., Prilaz aruna Filipovića 29, 10000 Zagreb, Croatia., Hutinec A; Selvita d.o.o., Prilaz aruna Filipovića 29, 10000 Zagreb, Croatia., Inturi TK; Syngene International, Biocon Park, Bommasandra, Bangalore, Karnataka 560099, India., Rupcic R; Selvita d.o.o., Prilaz aruna Filipovića 29, 10000 Zagreb, Croatia., Saxty G; Selvita d.o.o., Prilaz aruna Filipovića 29, 10000 Zagreb, Croatia., Watson SP; Sosei Heptares, Steinmetz Building, Granta Park, Great Abington, Cambridge CB21 6DG, United Kingdom.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2022 Oct 19; Vol. 13 (11), pp. 1776-1782. Date of Electronic Publication: 2022 Oct 19 (Print Publication: 2022).

From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.

Autor: Brown AJH; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Bradley SJ; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK; The Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, UK., Marshall FH; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Brown GA; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Bennett KA; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Brown J; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Cansfield JE; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Cross DM; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK; Cross Pharma Consulting Ltd, 20-22 Wenlock Road, London, N17GU, UK., de Graaf C; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Hudson BD; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Dwomoh L; The Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, UK., Dias JM; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Errey JC; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Hurrell E; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Liptrot J; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Mattedi G; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Molloy C; The Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, UK., Nathan PJ; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK; Brain Mapping Unit, University of Cambridge, Department of Psychiatry, Herchel Smith Building, Cambridge, CB20SZ, UK., Okrasa K; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Osborne G; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Patel JC; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Pickworth M; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Robertson N; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Shahabi S; Eli Lilly & Co, Neuroscience Discovery, Erl Wood Manor, Windlesham, Surrey, GU20 6PH, UK., Bundgaard C; Eli Lilly & Co, Neuroscience Discovery, Erl Wood Manor, Windlesham, Surrey, GU20 6PH, UK; H. Lundbeck A/S, Neuroscience Research, Ottiliavej 9, 2500 Valby, Copenhagen, Denmark., Phillips K; Eli Lilly & Co, Neuroscience Discovery, Erl Wood Manor, Windlesham, Surrey, GU20 6PH, UK., Broad LM; Eli Lilly & Co, Neuroscience Discovery, Erl Wood Manor, Windlesham, Surrey, GU20 6PH, UK., Goonawardena AV; Center for Neuroscience, Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA., Morairty SR; Center for Neuroscience, Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA., Browning M; University Department of Psychiatry, University of Oxford, Warneford Hospital, Oxford, OX12JD, UK; P1vital, Manor house, Howbery Buisness Park, Wallingford, OX108BA, UK., Perini F; Centre for Cognitive Neuroscience - Duke-NUS Medical School, 8 College Road, 169857, Singapore., Dawson GR; University Department of Psychiatry, University of Oxford, Warneford Hospital, Oxford, OX12JD, UK., Deakin JFW; Neuroscience and Psychiatry Unit, University of Manchester, Manchester, M139PT UK., Smith RT; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Sexton PM; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville 3052, Victoria, Australia; ARC Centre for Cryo-electron Microscopy of Membrane Proteins, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville 3052, Victoria, Australia., Warneck J; Protogenia Consulting Ltd, PO-Box 289, Ely, CB79DR, UK., Vinson M; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Tasker T; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Tehan BG; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Teobald B; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Christopoulos A; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville 3052, Victoria, Australia., Langmead CJ; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville 3052, Victoria, Australia., Jazayeri A; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Cooke RM; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Rucktooa P; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Congreve MS; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK., Weir M; Sosei-Heptares, Steinmetz Building, Granta Park, Cambridge, CB21 6DG, UK. Electronic address: malcolm.weir@soseiheptares.com., Tobin AB; The Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, UK. Electronic address: andrew.tobin@glasgow.ac.uk.

Publikováno v: Cell [Cell] 2021 Nov 24; Vol. 184 (24), pp. 5886-5901.e22.

NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis.

Autor: Eccles SA; Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, United Kingdom. Sue.Eccles@icr.ac.uk, Massey A, Raynaud FI, Sharp SY, Box G, Valenti M, Patterson L, de Haven Brandon A, Gowan S, Boxall F, Aherne W, Rowlands M, Hayes A, Martins V, Urban F, Boxall K, Prodromou C, Pearl L, James K, Matthews TP, Cheung KM, Kalusa A, Jones K, McDonald E, Barril X, Brough PA, Cansfield JE, Dymock B, Drysdale MJ, Finch H, Howes R, Hubbard RE, Surgenor A, Webb P, Wood M, Wright L, Workman P

Publikováno v: Cancer research [Cancer Res] 2008 Apr 15; Vol. 68 (8), pp. 2850-60.

Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues.

Autor: Sharp SY; Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, United Kingdom., Prodromou C, Boxall K, Powers MV, Holmes JL, Box G, Matthews TP, Cheung KM, Kalusa A, James K, Hayes A, Hardcastle A, Dymock B, Brough PA, Barril X, Cansfield JE, Wright L, Surgenor A, Foloppe N, Hubbard RE, Aherne W, Pearl L, Jones K, McDonald E, Raynaud F, Eccles S, Drysdale M, Workman P

Publikováno v: Molecular cancer therapeutics [Mol Cancer Ther] 2007 Apr; Vol. 6 (4), pp. 1198-211.