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Items: 35

1.

Methodologies for the Examination of Water in GPCRs.

Bortolato A, Tehan BG, Smith RT, Mason JS.

Methods Mol Biol. 2018;1705:207-232. doi: 10.1007/978-1-4939-7465-8_10.

PMID:
29188565
2.

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
3.

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
4.

Potential for the Rational Design of Allosteric Modulators of Class C GPCRs.

Christopher JA, Doré AS, Tehan BG.

Curr Top Med Chem. 2017;17(1):71-78. Review.

PMID:
27448651
5.

GPCR-Bench: A Benchmarking Set and Practitioners' Guide for G Protein-Coupled Receptor Docking.

Weiss DR, Bortolato A, Tehan B, Mason JS.

J Chem Inf Model. 2016 Apr 25;56(4):642-51. doi: 10.1021/acs.jcim.5b00660. Epub 2016 Mar 24.

PMID:
26958710
6.

[Benchmarking is an Effective Instrument to Improve Clinical Services--Contra].

Lepping P, Tehan B.

Psychiatr Prax. 2016 Mar;43(2):72-3. doi: 10.1055/s-0041-109340. Epub 2016 Mar 8. German. No abstract available.

PMID:
26953804
7.

Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.

Harpsøe K, Isberg V, Tehan BG, Weiss D, Arsova A, Marshall FH, Bräuner-Osborne H, Gloriam DE.

Sci Rep. 2015 Sep 11;5:13869. doi: 10.1038/srep13869.

8.

Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).

Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M.

J Med Chem. 2015 Aug 27;58(16):6653-64. doi: 10.1021/acs.jmedchem.5b00892. Epub 2015 Aug 12.

PMID:
26225459
9.

Pharmacology and physiology of gastrointestinal enteroendocrine cells.

Mace OJ, Tehan B, Marshall F.

Pharmacol Res Perspect. 2015 Aug;3(4):e00155. doi: 10.1002/prp2.155. Epub 2015 Jul 7. Review.

10.

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain.

Doré AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH.

Nature. 2014 Jul 31;511(7511):557-62. doi: 10.1038/nature13396. Epub 2014 Jul 6.

PMID:
25042998
11.

Structure of Class B GPCRs: new horizons for drug discovery.

Bortolato A, Doré AS, Hollenstein K, Tehan BG, Mason JS, Marshall FH.

Br J Pharmacol. 2014 Jul;171(13):3132-45. doi: 10.1111/bph.12689. Review.

12.

Unifying family A GPCR theories of activation.

Tehan BG, Bortolato A, Blaney FE, Weir MP, Mason JS.

Pharmacol Ther. 2014 Jul;143(1):51-60. doi: 10.1016/j.pharmthera.2014.02.004. Epub 2014 Feb 19. Review.

PMID:
24561131
13.

Water network perturbation in ligand binding: adenosine A(2A) antagonists as a case study.

Bortolato A, Tehan BG, Bodnarchuk MS, Essex JW, Mason JS.

J Chem Inf Model. 2013 Jul 22;53(7):1700-13. doi: 10.1021/ci4001458. Epub 2013 Jun 14.

PMID:
23725291
14.

Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.

Christopher JA, Brown J, Doré AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M.

J Med Chem. 2013 May 9;56(9):3446-55. doi: 10.1021/jm400140q. Epub 2013 Apr 9.

15.

Pharmacology and structure of isolated conformations of the adenosine A₂A receptor define ligand efficacy.

Bennett KA, Tehan B, Lebon G, Tate CG, Weir M, Marshall FH, Langmead CJ.

Mol Pharmacol. 2013 May;83(5):949-58. doi: 10.1124/mol.112.084509. Epub 2013 Feb 19.

16.

Evaluating the enthalpic contribution to ligand binding using QM calculations: effect of methodology on geometries and interaction energies.

Gleeson D, Tehan B, Gleeson MP, Limtrakul J.

Org Biomol Chem. 2012 Sep 21;10(35):7053-61. doi: 10.1039/c2ob25657f. Epub 2012 Aug 2.

PMID:
22858758
17.

Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design.

Congreve M, Andrews SP, Doré AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH.

J Med Chem. 2012 Mar 8;55(5):1898-903. doi: 10.1021/jm201376w. Epub 2012 Jan 27.

18.

Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine.

Doré AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH.

Structure. 2011 Sep 7;19(9):1283-93. doi: 10.1016/j.str.2011.06.014.

19.

Biophysical mapping of the adenosine A2A receptor.

Zhukov A, Andrews SP, Errey JC, Robertson N, Tehan B, Mason JS, Marshall FH, Weir M, Congreve M.

J Med Chem. 2011 Jul 14;54(13):4312-23. doi: 10.1021/jm2003798. Epub 2011 Jun 10.

20.

The identification of novel orally active mGluR5 antagonist GSK2210875.

Pilla M, Andreoli M, Tessari M, Delle-Fratte S, Roth A, Butler S, Brown F, Shah P, Bettini E, Cavallini P, Benedetti R, Minick D, Smith P, Tehan B, D'Alessandro P, Lorthioir O, Ball C, Garzya V, Goodacre C, Watson S.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7521-4. doi: 10.1016/j.bmcl.2010.09.120. Epub 2010 Nov 2.

PMID:
21051228
21.

Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.

Budzik B, Garzya V, Shi D, Walker G, Woolley-Roberts M, Pardoe J, Lucas A, Tehan B, Rivero RA, Langmead CJ, Watson J, Wu Z, Forbes IT, Jin J.

ACS Med Chem Lett. 2010 Jun 8;1(6):244-8. doi: 10.1021/ml100105x. eCollection 2010 Sep 9.

22.

Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor.

Avlani VA, Langmead CJ, Guida E, Wood MD, Tehan BG, Herdon HJ, Watson JM, Sexton PM, Christopoulos A.

Mol Pharmacol. 2010 Jul;78(1):94-104. doi: 10.1124/mol.110.064345. Epub 2010 Apr 22.

PMID:
20413650
23.

Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors.

Lebon G, Langmead CJ, Tehan BG, Hulme EC.

Mol Pharmacol. 2009 Feb;75(2):331-41. doi: 10.1124/mol.108.050963. Epub 2008 Nov 11.

24.

Roof and floor of the muscarinic binding pocket: variations in the binding modes of orthosteric ligands.

Goodwin JA, Hulme EC, Langmead CJ, Tehan BG.

Mol Pharmacol. 2007 Dec;72(6):1484-96. Epub 2007 Sep 11.

PMID:
17848601
25.

Comparisons of the HBV and HIV polymerase, and antiviral resistance mutations.

Bartholomeusz A, Tehan BG, Chalmers DK.

Antivir Ther. 2004 Apr;9(2):149-60. Review.

PMID:
15134177
26.

Microvascular free tissue transfer in the management of squamous cell carcinoma of the tongue during pregnancy.

Lloyd CJ, Paley MD, Penfold CN, Varadarajan V, Tehan B, Gollins SW.

Br J Oral Maxillofac Surg. 2003 Apr;41(2):109-11.

PMID:
12694703
27.

A consensus neural network-based technique for discriminating soluble and poorly soluble compounds.

Manallack DT, Tehan BG, Gancia E, Hudson BD, Ford MG, Livingstone DJ, Whitley DC, Pitt WR.

J Chem Inf Comput Sci. 2003 Mar-Apr;43(2):674-9.

PMID:
12653537
28.

Molecular mapping in the CNS.

Wong MG, Tehan BG, Lloyd EJ.

Curr Pharm Des. 2002;8(17):1547-70. Review.

PMID:
12052200
29.
30.

Ecstasy toxicity.

Hardern R, Tehan B.

J Accid Emerg Med. 1995 Mar;12(1):74. No abstract available.

31.

The SMART needle. A new Doppler ultrasound-guided vascular access needle.

Vucevic M, Tehan B, Gamlin F, Berridge JC, Boylan M.

Anaesthesia. 1994 Oct;49(10):889-91.

32.

Another cause of failure of patient-controlled analgesia.

Caldicott LD, Tehan B, Jayaratnasingam S.

Anaesthesia. 1994 May;49(5):456. No abstract available.

33.

Hyperthermia associated with 3,4-methylenedioxyethamphetamine ('Eve').

Tehan B, Hardern R, Bodenham A.

Anaesthesia. 1993 Jun;48(6):507-10. Review.

34.

Ecstasy and dantrolene.

Tehan B.

BMJ. 1993 Jan 9;306(6870):146. No abstract available.

35.

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