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Items: 33

1.

Pyrrolidine nucleoside bisphosphonates as antituberculosis agents targeting hypoxanthine-guanine phosphoribosyltransferase.

Eng WS, Rejman D, Pohl R, West NP, Woods K, Naesens LMJ, Keough DT, Guddat LW.

Eur J Med Chem. 2018 Nov 5;159:10-22. doi: 10.1016/j.ejmech.2018.09.039. Epub 2018 Sep 19.

PMID:
30265958
2.

CD99 is a therapeutic target on disease stem cells in myeloid malignancies.

Chung SS, Eng WS, Hu W, Khalaj M, Garrett-Bakelman FE, Tavakkoli M, Levine RL, Carroll M, Klimek VM, Melnick AM, Park CY.

Sci Transl Med. 2017 Jan 25;9(374). pii: eaaj2025. doi: 10.1126/scitranslmed.aaj2025.

3.

Oligomeric state of hypoxanthine-guanine phosphoribosyltransferase from Mycobacterium tuberculosis.

Eng WS, Keough DT, Hockova D, Winzor DJ, Guddat LW.

Biochimie. 2017 Apr;135:6-14. doi: 10.1016/j.biochi.2016.12.020. Epub 2017 Jan 9.

PMID:
28082125
4.

First Crystal Structures of Mycobacterium tuberculosis 6-Oxopurine Phosphoribosyltransferase: Complexes with GMP and Pyrophosphate and with Acyclic Nucleoside Phosphonates Whose Prodrugs Have Antituberculosis Activity.

Eng WS, Hocková D, Špaček P, Janeba Z, West NP, Woods K, Naesens LM, Keough DT, Guddat LW.

J Med Chem. 2015 Jun 11;58(11):4822-38. doi: 10.1021/acs.jmedchem.5b00611. Epub 2015 May 13.

PMID:
25915781
5.

Synthesis, conformational studies, and biological properties of phosphonomethoxyethyl derivatives of nucleobases with a locked conformation via a pyrrolidine ring.

Pohl R, Poštová Slavětínská L, Eng WS, Keough DT, Guddat LW, Rejman D.

Org Biomol Chem. 2015 Apr 28;13(16):4693-705. doi: 10.1039/c5ob00097a.

PMID:
25798893
6.

Complex N-linked glycans serve as a determinant for exosome/microvesicle cargo recruitment.

Liang Y, Eng WS, Colquhoun DR, Dinglasan RR, Graham DR, Mahal LK.

J Biol Chem. 2014 Nov 21;289(47):32526-37. doi: 10.1074/jbc.M114.606269. Epub 2014 Sep 26.

7.

Mapping posttranscriptional regulation of the human glycome uncovers microRNA defining the glycocode.

Agrawal P, Kurcon T, Pilobello KT, Rakus JF, Koppolu S, Liu Z, Batista BS, Eng WS, Hsu KL, Liang Y, Mahal LK.

Proc Natl Acad Sci U S A. 2014 Mar 18;111(11):4338-43. doi: 10.1073/pnas.1321524111. Epub 2014 Mar 3.

8.

Inhibition of the Escherichia coli 6-oxopurine phosphoribosyltransferases by nucleoside phosphonates: potential for new antibacterial agents.

Keough DT, Hocková D, Rejman D, Spaček P, Vrbková S, Krečmerová M, Eng WS, Jans H, West NP, Naesens LM, de Jersey J, Guddat LW.

J Med Chem. 2013 Sep 12;56(17):6967-84. doi: 10.1021/jm400779n. Epub 2013 Aug 27.

PMID:
23927482
9.

Molecular imaging using fluorescent lectins permits rapid endoscopic identification of dysplasia in Barrett's esophagus.

Bird-Lieberman EL, Neves AA, Lao-Sirieix P, O'Donovan M, Novelli M, Lovat LB, Eng WS, Mahal LK, Brindle KM, Fitzgerald RC.

Nat Med. 2012 Jan 15;18(2):315-21. doi: 10.1038/nm.2616.

PMID:
22245781
10.

Identification of a conserved glycan signature for microvesicles.

Batista BS, Eng WS, Pilobello KT, Hendricks-Muñoz KD, Mahal LK.

J Proteome Res. 2011 Oct 7;10(10):4624-33. doi: 10.1021/pr200434y. Epub 2011 Sep 23.

11.

Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.

Atack JR, Hallett DJ, Tye S, Wafford KA, Ryan C, Sanabria-Bohórquez SM, Eng WS, Gibson RE, Burns HD, Dawson GR, Carling RW, Street LJ, Pike A, De Lepeleire I, Van Laere K, Bormans G, de Hoon JN, Van Hecken A, McKernan RM, Murphy MG, Hargreaves RJ.

J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15.

PMID:
20156926
12.

Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans.

Atack JR, Wong DF, Fryer TD, Ryan C, Sanabria S, Zhou Y, Dannals RF, Eng WS, Gibson RE, Burns HD, Vega JM, Vessy L, Scott-Stevens P, Beech JS, Baron JC, Sohal B, Schrag ML, Aigbirhio FI, McKernan RM, Hargreaves RJ.

J Pharmacol Exp Ther. 2010 Jan;332(1):17-25. doi: 10.1124/jpet.109.157909. Epub 2009 Sep 24.

PMID:
19779131
13.

In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist.

Atack JR, Maubach KA, Wafford KA, O'Connor D, Rodrigues AD, Evans DC, Tattersall FD, Chambers MS, MacLeod AM, Eng WS, Ryan C, Hostetler E, Sanabria SM, Gibson RE, Krause S, Burns HD, Hargreaves RJ, Agrawal NG, McKernan RM, Murphy MG, Gingrich K, Dawson GR, Musson DG, Petty KJ.

J Pharmacol Exp Ther. 2009 Nov;331(2):470-84. doi: 10.1124/jpet.109.157636. Epub 2009 Aug 24.

PMID:
19704033
14.

The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, alpha5IA, is similar in rats and primates.

Atack JR, Eng WS, Gibson RE, Ryan C, Francis B, Sohal B, Dawson GR, Hargreaves RJ, Burns HD.

Br J Pharmacol. 2009 Jul;157(5):796-803. doi: 10.1111/j.1476-5381.2009.00216.x. Epub 2009 Apr 30.

15.

Alternative zippering as an on-off switch for SNARE-mediated fusion.

Giraudo CG, Garcia-Diaz A, Eng WS, Chen Y, Hendrickson WA, Melia TJ, Rothman JE.

Science. 2009 Jan 23;323(5913):512-6. doi: 10.1126/science.1166500.

16.

Distinct domains of complexins bind SNARE complexes and clamp fusion in vitro.

Giraudo CG, Garcia-Diaz A, Eng WS, Yamamoto A, Melia TJ, Rothman JE.

J Biol Chem. 2008 Jul 25;283(30):21211-9. doi: 10.1074/jbc.M803478200. Epub 2008 May 22.

17.

The acyclic CB1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake.

Addy C, Wright H, Van Laere K, Gantz I, Erondu N, Musser BJ, Lu K, Yuan J, Sanabria-Bohórquez SM, Stoch A, Stevens C, Fong TM, De Lepeleire I, Cilissen C, Cote J, Rosko K, Gendrano IN 3rd, Nguyen AM, Gumbiner B, Rothenberg P, de Hoon J, Bormans G, Depré M, Eng WS, Ravussin E, Klein S, Blundell J, Herman GA, Burns HD, Hargreaves RJ, Wagner J, Gottesdiener K, Amatruda JM, Heymsfield SB.

Cell Metab. 2008 Jan;7(1):68-78. doi: 10.1016/j.cmet.2007.11.012.

18.

Energetics and dynamics of SNAREpin folding across lipid bilayers.

Li F, Pincet F, Perez E, Eng WS, Melia TJ, Rothman JE, Tareste D.

Nat Struct Mol Biol. 2007 Oct;14(10):890-6. Epub 2007 Sep 30.

PMID:
17906638
19.

[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor.

Burns HD, Van Laere K, Sanabria-Bohórquez S, Hamill TG, Bormans G, Eng WS, Gibson R, Ryan C, Connolly B, Patel S, Krause S, Vanko A, Van Hecken A, Dupont P, De Lepeleire I, Rothenberg P, Stoch SA, Cote J, Hagmann WK, Jewell JP, Lin LS, Liu P, Goulet MT, Gottesdiener K, Wagner JA, de Hoon J, Mortelmans L, Fong TM, Hargreaves RJ.

Proc Natl Acad Sci U S A. 2007 Jun 5;104(23):9800-5. Epub 2007 May 29.

20.

A clamping mechanism involved in SNARE-dependent exocytosis.

Giraudo CG, Eng WS, Melia TJ, Rothman JE.

Science. 2006 Aug 4;313(5787):676-80. Epub 2006 Jun 22.

21.

Visualization and quantification of neurokinin-1 (NK1) receptors in the human brain.

Hietala J, Nyman MJ, Eskola O, Laakso A, Grönroos T, Oikonen V, Bergman J, Haaparanta M, Forsback S, Marjamäki P, Lehikoinen P, Goldberg M, Burns D, Hamill T, Eng WS, Coimbra A, Hargreaves R, Solin O.

Mol Imaging Biol. 2005 Jul-Aug;7(4):262-72.

PMID:
16155744
22.

Localization and activity of the SNARE Ykt6 determined by its regulatory domain and palmitoylation.

Fukasawa M, Varlamov O, Eng WS, Söllner TH, Rothman JE.

Proc Natl Acad Sci U S A. 2004 Apr 6;101(14):4815-20. Epub 2004 Mar 24.

23.

Countercurrent distribution of two distinct SNARE complexes mediating transport within the Golgi stack.

Volchuk A, Ravazzola M, Perrelet A, Eng WS, Di Liberto M, Varlamov O, Fukasawa M, Engel T, Söllner TH, Rothman JE, Orci L.

Mol Biol Cell. 2004 Apr;15(4):1506-18. Epub 2004 Jan 23.

24.

i-SNAREs: inhibitory SNAREs that fine-tune the specificity of membrane fusion.

Varlamov O, Volchuk A, Rahimian V, Doege CA, Paumet F, Eng WS, Arango N, Parlati F, Ravazzola M, Orci L, Söllner TH, Rothman JE.

J Cell Biol. 2004 Jan 5;164(1):79-88. Epub 2003 Dec 29.

25.

A cell-based radioligand binding assay for farnesyl: protein transferase inhibitors.

Lobell RB, Davide JP, Kohl NE, Burns HD, Eng WS, Gibson RE.

J Biomol Screen. 2003 Aug;8(4):430-8.

PMID:
14567795
26.

Non-invasive radiotracer imaging as a tool for drug development.

Gibson RE, Burns HD, Hamill TG, Eng WS, Francis BE, Ryan C.

Curr Pharm Des. 2000 Jul;6(10):973-89. Review.

PMID:
10828297
27.

Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development.

Burns HD, Hamill TG, Eng WS, Francis B, Fioravanti C, Gibson RE.

Curr Opin Chem Biol. 1999 Aug;3(4):388-94. Review.

PMID:
10419855
28.

In vivo binding and autoradiographic imaging of (+)-3-[125I]Iodo-MK-801 to the NMDA receptor-channel complex in rat brain.

Gibson EG, Burns HD, Thorpe HH, Eng WS, Ransom R, Solomon H.

Int J Rad Appl Instrum B. 1992 Apr;19(3):319-26.

PMID:
1378426
29.

(+)-3-[123I]Iodo-MK-801: synthesis and characterization of binding to the N-methyl-D-aspartate receptor complex.

Ransom RW, Eng WS, Burns HD, Gibson RE, Solomon HF.

Life Sci. 1990;46(15):1103-10.

PMID:
2159097
30.

Synthesis and binding affinity of an iodinated juvenile hormone.

Prestwich GD, Eng WS, Robles S, Vogt RG, Wiśniewski JR, Wawrzeńczyk C.

J Biol Chem. 1988 Jan 25;263(3):1398-404.

31.

Comparison of crude and affinity purified cytosolic epoxide hydrolases from hepatic tissue of control and clofibrate-fed mice.

Hammock BD, Prestwich GD, Loury DN, Cheung PY, Eng WS, Park SK, Moody DE, Silva MH, Wixtrom RN.

Arch Biochem Biophys. 1986 Jan;244(1):292-309.

PMID:
3947062
32.

Structure-activity relationships among aromatic analogs of trail-following pheromone of subterranean termites.

Prestwich GD, Eng WS, Deaton E, Wichern D.

J Chem Ecol. 1984 Aug;10(8):1201-17. doi: 10.1007/BF00988549.

PMID:
24318906
33.

Synthesis and bioassay of isoprenoid 3-alkylthio-1,1,1-trifluoro-2-propanones: potent, selective inhibitors of juvenile hormone esterase.

Prestwich GD, Eng WS, Roe RM, Hammock BD.

Arch Biochem Biophys. 1984 Feb 1;228(2):639-45.

PMID:
6696451

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