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Items: 1 to 50 of 203

1.

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

Scott JS, Bowker SS, Brocklehurst KJ, Brown HS, Clarke DS, Easter A, Ertan A, Goldberg K, Hudson JA, Kavanagh S, Laber D, Leach AG, MacFaul PA, Martin EA, McKerrecher D, Schofield P, Svensson PH, Teague J.

J Med Chem. 2014 Nov 13;57(21):8984-98. doi: 10.1021/jm5011012. Epub 2014 Nov 3.

PMID:
25286150
2.

GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans.

Stone VM, Dhayal S, Brocklehurst KJ, Lenaghan C, Sörhede Winzell M, Hammar M, Xu X, Smith DM, Morgan NG.

Diabetologia. 2014 Jun;57(6):1182-91. doi: 10.1007/s00125-014-3213-0. Epub 2014 Mar 25.

3.

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human.

Scott JS, Brocklehurst KJ, Brown HS, Clarke DS, Coe H, Groombridge SD, Laber D, MacFaul PA, McKerrecher D, Schofield P.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3175-9. doi: 10.1016/j.bmcl.2013.04.006. Epub 2013 Apr 10.

PMID:
23628336
4.

Cysteine proteases: mode of action and role in epidermal differentiation.

Brocklehurst K, Philpott MP.

Cell Tissue Res. 2013 Feb;351(2):237-44. doi: 10.1007/s00441-013-1557-2. Epub 2013 Jan 24. Review.

PMID:
23344364
5.

Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.

Scott JS, Birch AM, Brocklehurst KJ, Broo A, Brown HS, Butlin RJ, Clarke DS, Davidsson O, Ertan A, Goldberg K, Groombridge SD, Hudson JA, Laber D, Leach AG, Macfaul PA, McKerrecher D, Pickup A, Schofield P, Svensson PH, Sörme P, Teague J.

J Med Chem. 2012 Jun 14;55(11):5361-79. doi: 10.1021/jm300310c. Epub 2012 May 17.

PMID:
22545772
6.

Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.

Brocklehurst KJ, Broo A, Butlin RJ, Brown HS, Clarke DS, Davidsson Ö, Goldberg K, Groombridge SD, Kelly EE, Leach A, McKerrecher D, O'Donnell C, Poucher S, Schofield P, Scott JS, Teague J, Westgate L, Wood MJ.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7310-6. doi: 10.1016/j.bmcl.2011.10.033. Epub 2011 Oct 18.

PMID:
22061639
7.

Identification of interactions involved in the generation of nucleophilic reactivity and of catalytic competence in the catalytic site Cys/His ion pair of papain.

Hussain S, Khan A, Gul S, Resmini M, Verma CS, Thomas EW, Brocklehurst K.

Biochemistry. 2011 Dec 13;50(49):10732-42. doi: 10.1021/bi201207z. Epub 2011 Nov 17.

PMID:
22044167
8.

The cytoprotective effects of oleoylethanolamide in insulin-secreting cells do not require activation of GPR119.

Stone VM, Dhayal S, Smith DM, Lenaghan C, Brocklehurst KJ, Morgan NG.

Br J Pharmacol. 2012 Apr;165(8):2758-70. doi: 10.1111/j.1476-5381.2011.01755.x.

9.

Upregulation of β-cell genes and improved function in rodent islets following chronic glucokinase activation.

Gill D, Brocklehurst KJ, Brown HW, Smith DM.

J Mol Endocrinol. 2011 Jul 18;47(1):59-67. doi: 10.1530/JME-10-0157. Print 2011 Aug.

PMID:
21571864
10.

Structural insights into substrate specificity and the anti beta-elimination mechanism of pectate lyase.

Seyedarabi A, To TT, Ali S, Hussain S, Fries M, Madsen R, Clausen MH, Teixteira S, Brocklehurst K, Pickersgill RW.

Biochemistry. 2010 Jan 26;49(3):539-46. doi: 10.1021/bi901503g.

PMID:
20000851
11.

Deformed lattice detection in real-world images using mean-shift belief propagation.

Park M, Brocklehurst K, Collins RT, Liu Y.

IEEE Trans Pattern Anal Mach Intell. 2009 Oct;31(10):1804-16. doi: 10.1109/TPAMI.2009.73.

PMID:
19696451
12.

Generation of nucleophilic character in the Cys25/His159 ion pair of papain involves Trp177 but not Asp158.

Gul S, Hussain S, Thomas MP, Resmini M, Verma CS, Thomas EW, Brocklehurst K.

Biochemistry. 2008 Feb 19;47(7):2025-35. doi: 10.1021/bi702126p. Epub 2008 Jan 29.

PMID:
18225918
13.

Molecular basis of the activity of the phytopathogen pectin methylesterase.

Fries M, Ihrig J, Brocklehurst K, Shevchik VE, Pickersgill RW.

EMBO J. 2007 Sep 5;26(17):3879-87. Epub 2007 Aug 23.

14.

Elucidation of substrate specificity in the cobalamin (vitamin B12) biosynthetic methyltransferases. Structure and function of the C20 methyltransferase (CbiL) from Methanothermobacter thermautotrophicus.

Frank S, Deery E, Brindley AA, Leech HK, Lawrence A, Heathcote P, Schubert HL, Brocklehurst K, Rigby SE, Warren MJ, Pickersgill RW.

J Biol Chem. 2007 Aug 17;282(33):23957-69. Epub 2007 Jun 13.

15.
17.

DNA affinity chromatography.

Brocklehurst K, Courey AJ, Gul S, Lin SH, Moritz RL.

CSH Protoc. 2006 Jun 1;2006(1). pii: pdb.prot4206. doi: 10.1101/pdb.prot4206. No abstract available.

PMID:
22485607
18.

Preparation of DNA affinity resin.

Brocklehurst K, Courey AJ, Gul S, Lin SH, Moritz RL.

CSH Protoc. 2006 Jun 1;2006(1). pii: pdb.prot4205. doi: 10.1101/pdb.prot4205. No abstract available.

PMID:
22485606
19.

Directed Orientation of Antibodies during Preparation of Antibody Affinity Resin.

Brocklehurst K, Courey AJ, Gul S, Lin SH, Moritz RL.

CSH Protoc. 2006 Jun 1;2006(1). pii: pdb.prot4204. doi: 10.1101/pdb.prot4204. No abstract available.

PMID:
22485605
20.

Protein ligand affinity chromatography.

Brocklehurst K, Courey AJ, Gul S, Lin SH, Moritz RL.

CSH Protoc. 2006 Jun 1;2006(1). pii: pdb.prot4203. doi: 10.1101/pdb.prot4203. No abstract available.

PMID:
22485604
21.

Lectin-agarose affinity chromatography.

Brocklehurst K, Courey AJ, Gul S, Lin SH, Moritz RL.

CSH Protoc. 2006 Jun 1;2006(1). pii: pdb.prot4202. doi: 10.1101/pdb.prot4202. No abstract available.

PMID:
22485603
22.

Characterization of retinaldehyde dehydrogenase 3.

Graham CE, Brocklehurst K, Pickersgill RW, Warren MJ.

Biochem J. 2006 Feb 15;394(Pt 1):67-75.

23.
24.

Stimulation of hepatocyte glucose metabolism by novel small molecule glucokinase activators.

Brocklehurst KJ, Payne VA, Davies RA, Carroll D, Vertigan HL, Wightman HJ, Aiston S, Waddell ID, Leighton B, Coghlan MP, Agius L.

Diabetes. 2004 Mar;53(3):535-41.

25.

Isomerization of the uncomplexed actinidin molecule: kinetic accessibility of additional steps in enzyme catalysis provided by solvent perturbation.

Reid JD, Hussain S, Bailey TS, Sonkaria S, Sreedharan SK, Thomas EW, Resmini M, Brocklehurst K.

Biochem J. 2004 Mar 1;378(Pt 2):699-703.

26.

Differences in regulatory properties between human and rat glucokinase regulatory protein.

Brocklehurst KJ, Davies RA, Agius L.

Biochem J. 2004 Mar 1;378(Pt 2):693-7.

27.

Improvement in hydrolytic antibody activity by change in haptenic structure from phosphate to phosphonate with retention of a common leaving-group determinant: evidence for the 'flexibility' hypothesis.

Gul S, Sonkaria S, Pinitglang S, Florez-Alvarez J, Hussain S, Thomas EW, Ostler EL, Gallacher G, Resmini M, Brocklehurst K.

Biochem J. 2003 Dec 15;376(Pt 3):813-21.

28.

Characterisation of CadR from Pseudomonas aeruginosa: a Cd(II)-responsive MerR homologue.

Brocklehurst KR, Megit SJ, Morby AP.

Biochem Biophys Res Commun. 2003 Aug 22;308(2):234-9.

PMID:
12901859
29.
30.

The functional analysis of directed amino-acid alterations in ZntR from Escherichia coli.

Khan S, Brocklehurst KR, Jones GW, Morby AP.

Biochem Biophys Res Commun. 2002 Dec 6;299(3):438-45.

PMID:
12445820
31.

A rat monoclonal antibody that catalyses the hydrolysis of a nitrophenyl-beta-lactam.

Ostler EL, Dean CJ, Barber N, Valeri M, James S, Resmini M, Boucher G, Romanov N, Brocklehurst K, Gallacher G.

Biochem Biophys Res Commun. 2002 Nov 29;299(2):273-6.

PMID:
12437982
32.

Polyclonal catalytic antibodies.

Ostler EL, Resmini M, Brocklehurst K, Gallacher G.

J Immunol Methods. 2002 Nov 1;269(1-2):111-24. Review.

PMID:
12379356
33.

Polyclonal antibody-catalysed hydrolysis of a beta-lactam.

Ostler EL, Resmini M, Boucher G, Romanov N, Brocklehurst K, Gallacher G.

Chem Commun (Camb). 2002 Feb 7;(3):226-7.

PMID:
12120377
34.

Variation in aspects of cysteine proteinase catalytic mechanism deduced by spectroscopic observation of dithioester intermediates, kinetic analysis and molecular dynamics simulations.

Reid JD, Hussain S, Sreedharan SK, Bailey TS, Pinitglang S, Thomas EW, Verma CS, Brocklehurst K.

Biochem J. 2001 Jul 15;357(Pt 2):343-52.

35.
36.

Biochemical and X-ray crystallographic studies on shikimate kinase: the important structural role of the P-loop lysine.

Krell T, Maclean J, Boam DJ, Cooper A, Resmini M, Brocklehurst K, Kelly SM, Price NC, Lapthorn AJ, Coggins JR.

Protein Sci. 2001 Jun;10(6):1137-49.

38.

Metal-ion tolerance in Escherichia coli: analysis of transcriptional profiles by gene-array technology.

Brocklehurst KR, Morby AP.

Microbiology. 2000 Sep;146 ( Pt 9):2277-82.

PMID:
10974115
39.
40.

A general kinetic approach to investigation of active-site availability in macromolecular catalysts.

Resmini M, Gul S, Carter S, Sonkaria S, Topham CM, Gallacher G, Brocklehurst K.

Biochem J. 2000 Feb 15;346 Pt 1:117-25.

41.

Synthesis of a transition state analogue for the hydrolysis of cocaine: assistance to phosphonylation of a 3beta-hydroxytropane by a neighbouring amide group.

Hagi-Pavli EP, Simms CS, Ostler EL, Brocklehurst K, Gallacher G.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1881-4.

PMID:
10406659
42.

ZntR is a Zn(II)-responsive MerR-like transcriptional regulator of zntA in Escherichia coli.

Brocklehurst KR, Hobman JL, Lawley B, Blank L, Marshall SJ, Brown NL, Morby AP.

Mol Microbiol. 1999 Feb;31(3):893-902.

43.

Increased expression of several components of the ATP dependant proteosome pathway in denervated rat muscle is reversed by beta 2-adrenergic agonists.

Waddell ID, Ruddock P, Brocklehurst KJ, Wilbraham JM, Worral V, Holloway BR.

Biochem Soc Trans. 1998 Nov;26(4):S311. No abstract available.

PMID:
10047825
44.

Enzymatically active papain preferentially induces an allergic response in mice.

Chambers L, Brown A, Pritchard DI, Sreedharan S, Brocklehurst K, Kalsheker NA.

Biochem Biophys Res Commun. 1998 Dec 30;253(3):837-40.

PMID:
9918815
45.
46.

Detection of a free enzyme isomerisation in actinidin catalysed hydrolysis.

Reid JD, Sreedharan S, Cole A, Maskell S, Bokth A, Thomas EW, Brocklehurst K.

Biochem Soc Trans. 1998 May;26(2):S173. No abstract available.

PMID:
9649848
47.

The kinetically influential ionizations of caricain D158N revealed by using 4,4'-dipyrimidyl disulfide as a reactivity probe.

Khan A, Connerton IF, Cummings NJ, Hussain S, Noble MA, Taylor MA, Thomas EW, Verma C, Brocklehurst K.

Biochem Soc Trans. 1998 May;26(2):S172. No abstract available.

PMID:
9649847
48.

Sensitivities of transition state geometries to P1-P2 binding in reactions of papain and actinidin.

Gul S, Pinitglang S, Thomas EW, Verma C, Brocklehurst K.

Biochem Soc Trans. 1998 May;26(2):S171. No abstract available.

PMID:
9649846
49.

Determination of the catalytic site content of a polyclonal catalytic antibody preparation.

Resmini M, Gul S, Sonkaria S, Gallacher G, Brocklehurst K.

Biochem Soc Trans. 1998 May;26(2):S170. No abstract available.

PMID:
9649845
50.

A classical enzyme active center motif lacks catalytic competence until modulated electrostatically.

Pinitglang S, Watts AB, Patel M, Reid JD, Noble MA, Gul S, Bokth A, Naeem A, Patel H, Thomas EW, Sreedharan SK, Verma C, Brocklehurst K.

Biochemistry. 1997 Aug 19;36(33):9968-82.

PMID:
9254592

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