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Items: 1 to 20 of 77

1.

Serial millisecond crystallography for routine room-temperature structure determination at synchrotrons.

Weinert T, Olieric N, Cheng R, Brünle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Doré AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J.

Nat Commun. 2017 Sep 14;8(1):542. doi: 10.1038/s41467-017-00630-4.

2.

BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease.

Prati F, Bottegoni G, Bolognesi ML, Cavalli A.

J Med Chem. 2017 Aug 8. doi: 10.1021/acs.jmedchem.7b00393. [Epub ahead of print]

PMID:
28749667
3.

Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity.

Cheng RKY, Segala E, Robertson N, Deflorian F, Doré AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM.

Structure. 2017 Aug 1;25(8):1275-1285.e4. doi: 10.1016/j.str.2017.06.012. Epub 2017 Jul 14.

PMID:
28712806
4.

Opportunities for therapeutic antibodies directed at G-protein-coupled receptors.

Hutchings CJ, Koglin M, Olson WC, Marshall FH.

Nat Rev Drug Discov. 2017 Sep;16(9):1-24. doi: 10.1038/nrd.2017.91. Epub 2017 Jul 14. Review.

PMID:
28706220
5.

Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs.

Congreve M, Oswald C, Marshall FH.

Trends Pharmacol Sci. 2017 Sep;38(9):837-847. doi: 10.1016/j.tips.2017.05.010. Epub 2017 Jun 22. Review.

PMID:
28648526
6.

Crystal structure of the GLP-1 receptor bound to a peptide agonist.

Jazayeri A, Rappas M, Brown AJH, Kean J, Errey JC, Robertson NJ, Fiez-Vandal C, Andrews SP, Congreve M, Bortolato A, Mason JS, Baig AH, Teobald I, Doré AS, Weir M, Cooke RM, Marshall FH.

Nature. 2017 Jun 8;546(7657):254-258. doi: 10.1038/nature22800. Epub 2017 May 31. Erratum in: Nature. 2017 Jul 12;:.

PMID:
28562585
7.

Structural insight into allosteric modulation of protease-activated receptor 2.

Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N.

Nature. 2017 May 4;545(7652):112-115. doi: 10.1038/nature22309. Epub 2017 Apr 26.

PMID:
28445455
8.

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time.

Schuetz DA, de Witte WEA, Wong YC, Knasmueller B, Richter L, Kokh DB, Sadiq SK, Bosma R, Nederpelt I, Heitman LH, Segala E, Amaral M, Guo D, Andres D, Georgi V, Stoddart LA, Hill S, Cooke RM, De Graaf C, Leurs R, Frech M, Wade RC, de Lange ECM, IJzerman AP, Müller-Fahrnow A, Ecker GF.

Drug Discov Today. 2017 Jun;22(6):896-911. doi: 10.1016/j.drudis.2017.02.002. Epub 2017 Apr 13. Review.

PMID:
28412474
9.

Residues W320 and Y328 within the binding site of the μ-opioid receptor influence opiate ligand bias.

Hothersall JD, Torella R, Humphreys S, Hooley M, Brown A, McMurray G, Nickolls SA.

Neuropharmacology. 2017 May 15;118:46-58. doi: 10.1016/j.neuropharm.2017.03.007. Epub 2017 Mar 7.

10.
11.

Association between CSF biomarkers, hippocampal volume and cognitive function in patients with amnestic mild cognitive impairment (MCI).

Nathan PJ, Lim YY, Abbott R, Galluzzi S, Marizzoni M, Babiloni C, Albani D, Bartres-Faz D, Didic M, Farotti L, Parnetti L, Salvadori N, Müller BW, Forloni G, Girtler N, Hensch T, Jovicich J, Leeuwis A, Marra C, Molinuevo JL, Nobili F, Pariente J, Payoux P, Ranjeva JP, Rolandi E, Rossini PM, Schönknecht P, Soricelli A, Tsolaki M, Visser PJ, Wiltfang J, Richardson JC, Bordet R, Blin O, Frisoni GB; PharmaCog Consortium.

Neurobiol Aging. 2017 May;53:1-10. doi: 10.1016/j.neurobiolaging.2017.01.013. Epub 2017 Jan 18.

PMID:
28189924
12.

Decoding Corticotropin-Releasing Factor Receptor Type 1 Crystal Structures.

Dore AS, Bortolato A, Hollenstein K, Cheng RKY, Read RJ, Marshall FH.

Curr Mol Pharmacol. 2017;10(4):334-344. doi: 10.2174/1874467210666170110114727.

PMID:
28183242
13.

Perspective in Medicinal Chemistry: Structure-Based Drug Design.

Congreve M, Andrews S.

Curr Top Med Chem. 2017;17(2):93-94. No abstract available.

PMID:
28093978
14.

Editorial (Thematic Issue: New Targets for Structure-Based Drug Discovery).

Andrews S, Congreve M.

Curr Top Med Chem. 2017;17(1):2-3. No abstract available.

PMID:
28029086
15.

Intracellular allosteric antagonism of the CCR9 receptor.

Oswald C, Rappas M, Kean J, Doré AS, Errey JC, Bennett K, Deflorian F, Christopher JA, Jazayeri A, Mason JS, Congreve M, Cooke RM, Marshall FH.

Nature. 2016 Dec 15;540(7633):462-465. doi: 10.1038/nature20606. Epub 2016 Dec 7.

PMID:
27926729
16.

Visualizing GPCR 'Megaplexes' Which Enable Sustained Intracellular Signaling.

Marshall FH.

Trends Biochem Sci. 2016 Dec;41(12):985-986. doi: 10.1016/j.tibs.2016.10.006. Epub 2016 Nov 4.

PMID:
27825513
17.

Real time monitoring of membrane GPCR reconstitution by plasmon waveguide resonance: on the role of lipids.

Calmet P, De Maria M, Harté E, Lamb D, Serrano-Vega M, Jazayeri A, Tschammer N, Alves ID.

Sci Rep. 2016 Nov 8;6:36181. doi: 10.1038/srep36181.

18.

How Do Short Chain Nonionic Detergents Destabilize G-Protein-Coupled Receptors?

Lee S, Mao A, Bhattacharya S, Robertson N, Grisshammer R, Tate CG, Vaidehi N.

J Am Chem Soc. 2016 Nov 30;138(47):15425-15433. Epub 2016 Nov 15.

19.

The use of conformationally thermostabilised GPCRs in drug discovery: application to fragment, structure and biophysical techniques.

Tehan BG, Christopher JA.

Curr Opin Pharmacol. 2016 Oct;30:8-13. doi: 10.1016/j.coph.2016.06.010. Epub 2016 Jul 9. Review.

PMID:
27400445
20.

Allosteric binding: structures reveal new ways to tame G protein-coupled receptors.

Cooke R, Congreve M.

Future Med Chem. 2016 Oct 14. [Epub ahead of print] No abstract available.

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