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Items: 1 to 50 of 56

1.

Gram-scale synthesis of FICZ, a photoreactive endogenous ligand of the aryl hydrocarbon receptor.

Zhang C, Creech KL, Zuercher WJ, Willson TM.

Sci Rep. 2019 Jul 10;9(1):9982. doi: 10.1038/s41598-019-46374-7.

2.

CaMKK2 in myeloid cells is a key regulator of the immune-suppressive microenvironment in breast cancer.

Racioppi L, Nelson ER, Huang W, Mukherjee D, Lawrence SA, Lento W, Masci AM, Jiao Y, Park S, York B, Liu Y, Baek AE, Drewry DH, Zuercher WJ, Bertani FR, Businaro L, Geradts J, Hall A, Means AR, Chao N, Chang CY, McDonnell DP.

Nat Commun. 2019 Jun 4;10(1):2450. doi: 10.1038/s41467-019-10424-5.

3.

Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).

Asquith CRM, Treiber DK, Zuercher WJ.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1727-1731. doi: 10.1016/j.bmcl.2019.05.025. Epub 2019 May 16.

4.

A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction.

Drewry DH, Wells CI, Zuercher WJ, Willson TM.

SLAS Discov. 2019 Jun;24(5):505-514. doi: 10.1177/2472555219838210. Epub 2019 Apr 29.

PMID:
31034310
5.

Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.

Asquith CRM, Naegeli KM, East MP, Laitinen T, Havener TM, Wells CI, Johnson GL, Drewry DH, Zuercher WJ, Morris DC.

J Med Chem. 2019 May 9;62(9):4772-4778. doi: 10.1021/acs.jmedchem.9b00350. Epub 2019 Apr 19.

PMID:
30973735
6.

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).

Asquith CRM, Berger BT, Wan J, Bennett JM, Capuzzi SJ, Crona DJ, Drewry DH, East MP, Elkins JM, Fedorov O, Godoi PH, Hunter DM, Knapp S, Müller S, Torrice CD, Wells CI, Earp HS, Willson TM, Zuercher WJ.

J Med Chem. 2019 Mar 14;62(5):2830-2836. doi: 10.1021/acs.jmedchem.8b01213. Epub 2019 Feb 26.

7.

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.

Agajanian MJ, Walker MP, Axtman AD, Ruela-de-Sousa RR, Serafin DS, Rabinowitz AD, Graham DM, Ryan MB, Tamir T, Nakamichi Y, Gammons MV, Bennett JM, Couñago RM, Drewry DH, Elkins JM, Gileadi C, Gileadi O, Godoi PH, Kapadia N, Müller S, Santiago AS, Sorrell FJ, Wells CI, Fedorov O, Willson TM, Zuercher WJ, Major MB.

Cell Rep. 2019 Jan 2;26(1):79-93.e8. doi: 10.1016/j.celrep.2018.12.023.

8.

Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.

Foulkes DM, Byrne DP, Yeung W, Shrestha S, Bailey FP, Ferries S, Eyers CE, Keeshan K, Wells C, Drewry DH, Zuercher WJ, Kannan N, Eyers PA.

Sci Signal. 2018 Sep 25;11(549). pii: eaat7951. doi: 10.1126/scisignal.aat7951.

9.

GW779439X and Its Pyrazolopyridazine Derivatives Inhibit the Serine/Threonine Kinase Stk1 and Act As Antibiotic Adjuvants against β-Lactam-Resistant Staphylococcus aureus.

Schaenzer AJ, Wlodarchak N, Drewry DH, Zuercher WJ, Rose WE, Ferrer CA, Sauer JD, Striker R.

ACS Infect Dis. 2018 Oct 12;4(10):1508-1518. doi: 10.1021/acsinfecdis.8b00136. Epub 2018 Aug 15.

PMID:
30059625
10.

Identification of lead anti-human cytomegalovirus compounds targeting MAP4K4 via machine learning analysis of kinase inhibitor screening data.

Strang BL, Asquith CRM, Moshrif HF, Ho CM, Zuercher WJ, Al-Ali H.

PLoS One. 2018 Jul 26;13(7):e0201321. doi: 10.1371/journal.pone.0201321. eCollection 2018.

11.

New tools for carbohydrate sulfation analysis: heparan sulfate 2-O-sulfotransferase (HS2ST) is a target for small-molecule protein kinase inhibitors.

Byrne DP, Li Y, Ramakrishnan K, Barsukov IL, Yates EA, Eyers CE, Papy-Garcia D, Chantepie S, Pagadala V, Liu J, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.

Biochem J. 2018 Aug 14;475(15):2417-2433. doi: 10.1042/BCJ20180265.

12.

New tools for evaluating protein tyrosine sulfation: tyrosylprotein sulfotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors.

Byrne DP, Li Y, Ngamlert P, Ramakrishnan K, Eyers CE, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.

Biochem J. 2018 Aug 14;475(15):2435-2455. doi: 10.1042/BCJ20180266.

13.

1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.

Asquith CRM, Godoi PH, Couñago RM, Laitinen T, Scott JW, Langendorf CG, Oakhill JS, Drewry DH, Zuercher WJ, Koutentis PA, Willson TM, Kalogirou AS.

Molecules. 2018 May 19;23(5). pii: E1221. doi: 10.3390/molecules23051221.

14.

Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth.

Krulikas LJ, McDonald IM, Lee B, Okumu DO, East MP, Gilbert TSK, Herring LE, Golitz BT, Wells CI, Axtman AD, Zuercher WJ, Willson TM, Kireev D, Yeh JJ, Johnson GL, Baines AT, Graves LM.

SLAS Discov. 2018 Sep;23(8):850-861. doi: 10.1177/2472555218773045. Epub 2018 May 9.

PMID:
29742358
15.

Donated chemical probes for open science.

Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A.

Elife. 2018 Apr 20;7. pii: e34311. doi: 10.7554/eLife.34311.

16.

Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.

Asquith CRM, Laitinen T, Bennett JM, Godoi PH, East MP, Tizzard GJ, Graves LM, Johnson GL, Dornsife RE, Wells CI, Elkins JM, Willson TM, Zuercher WJ.

ChemMedChem. 2018 Jan 8;13(1):48-66. doi: 10.1002/cmdc.201700663. Epub 2017 Nov 27.

17.

A screen for kinase inhibitors identifies antimicrobial imidazopyridine aminofurazans as specific inhibitors of the Listeria monocytogenes PASTA kinase PrkA.

Schaenzer AJ, Wlodarchak N, Drewry DH, Zuercher WJ, Rose WE, Striker R, Sauer JD.

J Biol Chem. 2017 Oct 13;292(41):17037-17045. doi: 10.1074/jbc.M117.808600. Epub 2017 Aug 16.

18.

Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations.

Couñago RM, Allerston CK, Savitsky P, Azevedo H, Godoi PH, Wells CI, Mascarello A, de Souza Gama FH, Massirer KB, Zuercher WJ, Guimarães CRW, Gileadi O.

Sci Rep. 2017 Aug 8;7(1):7501. doi: 10.1038/s41598-017-07755-y.

19.

Novel application of the published kinase inhibitor set to identify therapeutic targets and pathways in triple negative breast cancer subtypes.

Matossian MD, Elliott S, Hoang VT, Burks HE, Phamduy TB, Chrisey DB, Zuercher WJ, Drewry DH, Wells C, Collins-Burow B, Burow ME.

PLoS One. 2017 Aug 3;12(8):e0177802. doi: 10.1371/journal.pone.0177802. eCollection 2017.

20.

Progress towards a public chemogenomic set for protein kinases and a call for contributions.

Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM.

PLoS One. 2017 Aug 2;12(8):e0181585. doi: 10.1371/journal.pone.0181585. eCollection 2017.

21.

A trust approach for sharing research reagents.

Edwards A, Morgan M, Al Chawaf A, Andrusiak K, Charney R, Cynader Z, ElDessouki A, Lee Y, Moeser A, Stern S, Zuercher WJ.

Sci Transl Med. 2017 May 31;9(392). pii: eaai9055. doi: 10.1126/scitranslmed.aai9055. Review.

PMID:
28566431
22.

High-throughput screening of a GlaxoSmithKline protein kinase inhibitor set identifies an inhibitor of human cytomegalovirus replication that prevents CREB and histone H3 post-translational modification.

Khan AS, Murray MJ, Ho CMK, Zuercher WJ, Reeves MB, Strang BL.

J Gen Virol. 2017 Apr;98(4):754-768. doi: 10.1099/jgv.0.000713. Epub 2017 Apr 20.

23.

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.

Simpson C, Jones NG, Hull-Ryde EA, Kireev D, Stashko M, Tang K, Janetka J, Wildman SA, Zuercher WJ, Schapira M, Hui R, Janzen W, Sibley LD.

ACS Infect Dis. 2016 Mar 11;2(3):194-206. Epub 2015 Dec 28.

24.

EGFR inhibitors identified as a potential treatment for chordoma in a focused compound screen.

Scheipl S, Barnard M, Cottone L, Jorgensen M, Drewry DH, Zuercher WJ, Turlais F, Ye H, Leite AP, Smith JA, Leithner A, Möller P, Brüderlein S, Guppy N, Amary F, Tirabosco R, Strauss SJ, Pillay N, Flanagan AM.

J Pathol. 2016 Jul;239(3):320-34. doi: 10.1002/path.4729. Epub 2016 May 31.

25.

The Intersection of Structural and Chemical Biology - An Essential Synergy.

Zuercher WJ, Elkins JM, Knapp S.

Cell Chem Biol. 2016 Jan 21;23(1):173-182. doi: 10.1016/j.chembiol.2015.12.005. Review.

26.

Using a Genetically Encoded Sensor to Identify Inhibitors of Toxoplasma gondii Ca2+ Signaling.

Sidik SM, Hortua Triana MA, Paul AS, El Bakkouri M, Hackett CG, Tran F, Westwood NJ, Hui R, Zuercher WJ, Duraisingh MT, Moreno SN, Lourido S.

J Biol Chem. 2016 Apr 29;291(18):9566-80. doi: 10.1074/jbc.M115.703546. Epub 2016 Mar 1.

27.

Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni.

Long T, Neitz RJ, Beasley R, Kalyanaraman C, Suzuki BM, Jacobson MP, Dissous C, McKerrow JH, Drewry DH, Zuercher WJ, Singh R, Caffrey CR.

PLoS Negl Trop Dis. 2016 Jan 11;10(1):e0004356. doi: 10.1371/journal.pntd.0004356. eCollection 2016 Jan.

28.

Discovery of Novel Small Molecules that Activate Satellite Cell Proliferation and Enhance Repair of Damaged Muscle.

Billin AN, Bantscheff M, Drewes G, Ghidelli-Disse S, Holt JA, Kramer HF, McDougal AJ, Smalley TL, Wells CI, Zuercher WJ, Henke BR.

ACS Chem Biol. 2016 Feb 19;11(2):518-29. doi: 10.1021/acschembio.5b00772. Epub 2016 Jan 7.

PMID:
26696218
29.

Comprehensive characterization of the Published Kinase Inhibitor Set.

Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ.

Nat Biotechnol. 2016 Jan;34(1):95-103. doi: 10.1038/nbt.3374. Epub 2015 Oct 26.

PMID:
26501955
30.

Corrigendum: The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Nov;11(11):887. doi: 10.1038/nchembio1115-887c. No abstract available.

PMID:
26485080
31.

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. No abstract available. Erratum in: Nat Chem Biol. 2015 Aug;11(8):541. Roth, Brian [Corrected to Roth, Bryan] and Frederiksen, Mathias [Added]. Nat Chem Biol. 2015 Nov;11(11):887.

32.

Transactivation Function-2 of Estrogen Receptor α Contains Transactivation Function-1-regulating Element.

Arao Y, Coons LA, Zuercher WJ, Korach KS.

J Biol Chem. 2015 Jul 10;290(28):17611-27. doi: 10.1074/jbc.M115.638650. Epub 2015 May 31.

33.

Serum and glucocorticoid-regulated kinase 1 regulates neutrophil clearance during inflammation resolution.

Burgon J, Robertson AL, Sadiku P, Wang X, Hooper-Greenhill E, Prince LR, Walker P, Hoggett EE, Ward JR, Farrow SN, Zuercher WJ, Jeffrey P, Savage CO, Ingham PW, Hurlstone AF, Whyte MK, Renshaw SA.

J Immunol. 2014 Feb 15;192(4):1796-805. doi: 10.4049/jimmunol.1300087. Epub 2014 Jan 15.

34.

Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS).

Drewry DH, Willson TM, Zuercher WJ.

Curr Top Med Chem. 2014;14(3):340-2. Review.

35.

Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.

Dranchak P, MacArthur R, Guha R, Zuercher WJ, Drewry DH, Auld DS, Inglese J.

PLoS One. 2013;8(3):e57888. doi: 10.1371/journal.pone.0057888. Epub 2013 Mar 7.

36.

A public-private partnership to unlock the untargeted kinome.

Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ.

Nat Chem Biol. 2013 Jan;9(1):3-6. doi: 10.1038/nchembio.1113. No abstract available.

PMID:
23238671
37.

The development of a high-content screening binding assay for the smoothened receptor.

Bee WT, Xie W, Truong M, Will M, Turunen B, Zuercher WJ, McMillan L, Li H, Hornberger KR, Davenport EA, Ames RS, Kallal LA.

J Biomol Screen. 2012 Aug;17(7):900-11. doi: 10.1177/1087057112447872. Epub 2012 May 29.

PMID:
22644265
38.

Estrogen-related receptor-α is a metabolic regulator of effector T-cell activation and differentiation.

Michalek RD, Gerriets VA, Nichols AG, Inoue M, Kazmin D, Chang CY, Dwyer MA, Nelson ER, Pollizzi KN, Ilkayeva O, Giguere V, Zuercher WJ, Powell JD, Shinohara ML, McDonnell DP, Rathmell JC.

Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18348-53. doi: 10.1073/pnas.1108856108. Epub 2011 Oct 31.

39.

The metabolic regulator ERRα, a downstream target of HER2/IGF-1R, as a therapeutic target in breast cancer.

Chang CY, Kazmin D, Jasper JS, Kunder R, Zuercher WJ, McDonnell DP.

Cancer Cell. 2011 Oct 18;20(4):500-10. doi: 10.1016/j.ccr.2011.08.023.

40.

Ligand-dependent regulation of the activity of the orphan nuclear receptor, small heterodimer partner (SHP), in the repression of bile acid biosynthetic CYP7A1 and CYP8B1 genes.

Miao J, Choi SE, Seok SM, Yang L, Zuercher WJ, Xu Y, Willson TM, Xu HE, Kemper JK.

Mol Endocrinol. 2011 Jul;25(7):1159-69. doi: 10.1210/me.2011-0033. Epub 2011 May 12.

41.

Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2).

Whitby RJ, Stec J, Blind RD, Dixon S, Leesnitzer LM, Orband-Miller LA, Williams SP, Willson TM, Xu R, Zuercher WJ, Cai F, Ingraham HA.

J Med Chem. 2011 Apr 14;54(7):2266-81. doi: 10.1021/jm1014296. Epub 2011 Mar 10.

42.

GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

Grant D, Yin L, Collins JL, Parks DJ, Orband-Miller LA, Wisely GB, Joshi S, Lazar MA, Willson TM, Zuercher WJ.

ACS Chem Biol. 2010 Oct 15;5(10):925-32. doi: 10.1021/cb100141y.

PMID:
20677822
43.

Discovery of tertiary sulfonamides as potent liver X receptor antagonists.

Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM.

J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p.

PMID:
20345102
44.

Current review of small molecule Ret kinase inhibitors.

Zuercher WJ, Turunen BJ, Lackey KE.

Mini Rev Med Chem. 2010 Feb;10(2):138-46. Review.

PMID:
20105131
45.

Evidence for allosteric interactions of antagonist binding to the smoothened receptor.

Rominger CM, Bee WL, Copeland RA, Davenport EA, Gilmartin A, Gontarek R, Hornberger KR, Kallal LA, Lai Z, Lawrie K, Lu Q, McMillan L, Truong M, Tummino PJ, Turunen B, Will M, Zuercher WJ, Rominger DH.

J Pharmacol Exp Ther. 2009 Jun;329(3):995-1005. doi: 10.1124/jpet.109.152090. Epub 2009 Mar 20. Erratum in: J Pharmacol Exp Ther. 2010 Feb;332(2):690.

PMID:
19304771
46.

Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.

Chao EY, Caravella JA, Watson MA, Campobasso N, Ghisletti S, Billin AN, Galardi C, Wang P, Laffitte BA, Iannone MA, Goodwin BJ, Nichols JA, Parks DJ, Stewart E, Wiethe RW, Williams SP, Smallwood A, Pearce KH, Glass CK, Willson TM, Zuercher WJ, Collins JL.

J Med Chem. 2008 Sep 25;51(18):5758-65. doi: 10.1021/jm800612u.

PMID:
18800767
47.

Selective partial agonism of liver X receptor alpha is related to differential corepressor recruitment.

Phelan CA, Weaver JM, Steger DJ, Joshi S, Maslany JT, Collins JL, Zuercher WJ, Willson TM, Walker M, Jaye M, Lazar MA.

Mol Endocrinol. 2008 Oct;22(10):2241-9. doi: 10.1210/me.2008-0041. Epub 2008 Jul 31.

48.

Recent advances in liver X receptor biology and chemistry.

Goodwin BJ, Zuercher WJ, Collins JL.

Curr Top Med Chem. 2008;8(9):781-91. Review.

PMID:
18537688
49.

On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.

Hyatt SM, Lockamy EL, Stein RA, McDonnell DP, Miller AB, Orband-Miller LA, Willson TM, Zuercher WJ.

J Med Chem. 2007 Dec 27;50(26):6722-4. Epub 2007 Dec 4.

50.

Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.

Xue Y, Chao E, Zuercher WJ, Willson TM, Collins JL, Redinbo MR.

Bioorg Med Chem. 2007 Mar 1;15(5):2156-66. Epub 2006 Dec 20.

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