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Items: 31

1.

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.

Wyllie S, Brand S, Thomas M, De Rycker M, Chung CW, Pena I, Bingham RP, Bueren-Calabuig JA, Cantizani J, Cebrian D, Craggs PD, Ferguson L, Goswami P, Hobrath J, Howe J, Jeacock L, Ko EJ, Korczynska J, MacLean L, Manthri S, Martinez MS, Mata-Cantero L, Moniz S, Nühs A, Osuna-Cabello M, Pinto E, Riley J, Robinson S, Rowland P, Simeons FRC, Shishikura Y, Spinks D, Stojanovski L, Thomas J, Thompson S, Viayna Gaza E, Wall RJ, Zuccotto F, Horn D, Ferguson MAJ, Fairlamb AH, Fiandor JM, Martin J, Gray DW, Miles TJ, Gilbert IH, Read KD, Marco M, Wyatt PG.

Proc Natl Acad Sci U S A. 2019 May 7;116(19):9318-9323. doi: 10.1073/pnas.1820175116. Epub 2019 Apr 8.

2.

Photoactivable Glycolipid Antigens Generate Stable Conjugates with CD1d for Invariant Natural Killer T Cell Activation.

Veerapen N, Kharkwal SS, Jervis P, Bhowruth V, Besra AK, North SJ, Haslam SM, Dell A, Hobrath J, Quaid PJ, Moynihan PJ, Cox LR, Kharkwal H, Zauderer M, Besra GS, Porcelli SA.

Bioconjug Chem. 2018 Sep 19;29(9):3161-3173. doi: 10.1021/acs.bioconjchem.8b00484. Epub 2018 Aug 23.

3.

Slow-Binding Inhibition of Mycobacterium tuberculosis Shikimate Kinase by Manzamine Alkaloids.

Simithy J, Fuanta NR, Alturki M, Hobrath JV, Wahba AE, Pina I, Rath J, Hamann MT, DeRuiter J, Goodwin DC, Calderón AI.

Biochemistry. 2018 Aug 14;57(32):4923-4933. doi: 10.1021/acs.biochem.8b00231. Epub 2018 Jul 31.

PMID:
30063132
4.

Oxazole and thiazole analogs of sulindac for cancer prevention.

Mathew B, Hobrath JV, Connelly MC, Guy RK, Reynolds RC.

Future Med Chem. 2018 Apr 1;10(7):743-753. doi: 10.4155/fmc-2017-0182. Epub 2018 Apr 19.

5.

Mechanism of irreversible inhibition of Mycobacterium tuberculosis shikimate kinase by ilimaquinone.

Simithy J, Fuanta NR, Hobrath JV, Kochanowska-Karamyan A, Hamann MT, Goodwin DC, Calderón AI.

Biochim Biophys Acta Proteins Proteom. 2018 May - Jun;1866(5-6):731-739. doi: 10.1016/j.bbapap.2018.04.007. Epub 2018 Apr 12.

PMID:
29654976
6.

Amine Containing Analogs of Sulindac for Cancer Prevention.

Mathew B, Hobrath JV, Connelly MC, Guy RK, Reynolds RC.

Open Med Chem J. 2018 Jan 31;12:1-12. doi: 10.2174/1874104501812010001. eCollection 2018.

7.

A multifaceted approach to identify non-specific enzyme inhibition: Application to Mycobacterium tuberculosis shikimate kinase.

Alturki MS, Fuanta NR, Jarrard MA, Hobrath JV, Goodwin DC, Rants'o TA, Calderón AI.

Bioorg Med Chem Lett. 2018 Feb 15;28(4):802-808. doi: 10.1016/j.bmcl.2017.12.002. Epub 2017 Dec 5.

PMID:
29366649
8.

Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens.

Mathew B, Hobrath JV, Lu W, Li Y, Reynolds RC.

Med Chem Res. 2017;26(11):3038-3045. doi: 10.1007/s00044-017-2001-z. Epub 2017 Aug 5.

9.

Diverse amide analogs of sulindac for cancer treatment and prevention.

Mathew B, Hobrath JV, Connelly MC, Kiplin Guy R, Reynolds RC.

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4614-4621. doi: 10.1016/j.bmcl.2017.09.022. Epub 2017 Sep 13.

10.

Characterization of a new pathway that activates lumisterol in vivo to biologically active hydroxylumisterols.

Slominski AT, Kim TK, Hobrath JV, Janjetovic Z, Oak ASW, Postlethwaite A, Lin Z, Li W, Takeda Y, Jetten AM, Tuckey RC.

Sci Rep. 2017 Sep 12;7(1):11434. doi: 10.1038/s41598-017-10202-7.

11.

Screening and Development of New Inhibitors of FtsZ from M. Tuberculosis.

Mathew B, Hobrath JV, Ross L, Connelly MC, Lofton H, Rajagopalan M, Guy RK, Reynolds RC.

PLoS One. 2016 Oct 21;11(10):e0164100. doi: 10.1371/journal.pone.0164100. eCollection 2016.

12.

Endogenously produced nonclassical vitamin D hydroxy-metabolites act as "biased" agonists on VDR and inverse agonists on RORα and RORγ.

Slominski AT, Kim TK, Hobrath JV, Oak ASW, Tang EKY, Tieu EW, Li W, Tuckey RC, Jetten AM.

J Steroid Biochem Mol Biol. 2017 Oct;173:42-56. doi: 10.1016/j.jsbmb.2016.09.024. Epub 2016 Sep 28. Review.

13.

Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.

Venukadasula PK, Owusu BY, Bansal N, Ross LJ, Hobrath JV, Bao D, Truss JW, Stackhouse M, Messick TE, Klampfer L, Galemmo RA Jr.

ACS Med Chem Lett. 2015 Dec 22;7(2):177-81. doi: 10.1021/acsmedchemlett.5b00357. eCollection 2016 Feb 11.

14.

Biochemical and structural characterization of mycobacterial aspartyl-tRNA synthetase AspS, a promising TB drug target.

Gurcha SS, Usha V, Cox JA, Fütterer K, Abrahams KA, Bhatt A, Alderwick LJ, Reynolds RC, Loman NJ, Nataraj V, Alemparte C, Barros D, Lloyd AJ, Ballell L, Hobrath JV, Besra GS.

PLoS One. 2014 Nov 19;9(11):e113568. doi: 10.1371/journal.pone.0113568. eCollection 2014.

15.

Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.

Ananthan S, Saini SK, Zhou G, Hobrath JV, Padmalayam I, Zhai L, Bostwick JR, Antonio T, Reith ME, McDowell S, Cho E, McAleer L, Taylor M, Luedtke RR.

J Med Chem. 2014 Aug 28;57(16):7042-60. doi: 10.1021/jm500801r. Epub 2014 Aug 15.

16.

Identification of shikimate kinase inhibitors among anti-Mycobacterium tuberculosis compounds by LC-MS.

Simithy J, Reeve N, Hobrath JV, Reynolds RC, Calderón AI.

Tuberculosis (Edinb). 2014 Mar;94(2):152-8. doi: 10.1016/j.tube.2013.12.004. Epub 2013 Dec 31.

PMID:
24429106
17.

Combining computational methods for hit to lead optimization in Mycobacterium tuberculosis drug discovery.

Ekins S, Freundlich JS, Hobrath JV, Lucile White E, Reynolds RC.

Pharm Res. 2014 Feb;31(2):414-35. doi: 10.1007/s11095-013-1172-7. Epub 2013 Oct 17.

18.
19.

Identification of novel Mt-Guab2 inhibitor series active against M. tuberculosis.

Usha V, Hobrath JV, Gurcha SS, Reynolds RC, Besra GS.

PLoS One. 2012;7(3):e33886. doi: 10.1371/journal.pone.0033886. Epub 2012 Mar 29.

20.

Identification of Rv0535 as methylthioadenosine phosphorylase from Mycobacterium tuberculosis.

Buckoreelall K, Sun Y, Hobrath JV, Wilson L, Parker WB.

Tuberculosis (Edinb). 2012 Mar;92(2):139-47. doi: 10.1016/j.tube.2011.11.010. Epub 2012 Jan 4.

21.

High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv.

Reynolds RC, Ananthan S, Faaleolea E, Hobrath JV, Kwong CD, Maddox C, Rasmussen L, Sosa MI, Thammasuvimol E, White EL, Zhang W, Secrist JA 3rd.

Tuberculosis (Edinb). 2012 Jan;92(1):72-83. doi: 10.1016/j.tube.2011.05.005. Epub 2011 Jun 25.

22.

A high-throughput screen with isogenic PTEN+/+ and PTEN-/- cells identifies CID1340132 as a novel compound that induces apoptosis in PTEN and PIK3CA mutant human cancer cells.

Li HF, Keeton A, Vitolo M, Maddox C, Rasmussen L, Hobrath J, White EL, Park BH, Piazza GA, Kim JS, Waldman T.

J Biomol Screen. 2011 Apr;16(4):383-93. doi: 10.1177/1087057110397357. Epub 2011 Feb 18.

23.

Discovery of novel benzoquinazolinones and thiazoloimidazoles, inhibitors of influenza H5N1 and H1N1 viruses, from a cell-based high-throughput screen.

Maddry JA, Chen X, Jonsson CB, Ananthan S, Hobrath J, Smee DF, Noah JW, Noah D, Xu X, Jia F, Maddox C, Sosa MI, White EL, Severson WE.

J Biomol Screen. 2011 Jan;16(1):73-81. doi: 10.1177/1087057110384613. Epub 2010 Nov 8.

PMID:
21059874
24.

Identification of novel small molecule activators of nuclear factor-κB with neuroprotective action via high-throughput screening.

Manuvakhova MS, Johnson GG, White MC, Ananthan S, Sosa M, Maddox C, McKellip S, Rasmussen L, Wennerberg K, Hobrath JV, White EL, Maddry JA, Grimaldi M.

J Neurosci Res. 2011 Jan;89(1):58-72. doi: 10.1002/jnr.22526.

25.

A high-throughput screen for chemical inhibitors of exocytic transport in yeast.

Zhang L, Nebane NM, Wennerberg K, Li Y, Neubauer V, Hobrath JV, McKellip S, Rasmussen L, Shindo N, Sosa M, Maddry JA, Ananthan S, Piazza GA, White EL, Harsay E.

Chembiochem. 2010 Jun 14;11(9):1291-301. doi: 10.1002/cbic.200900681.

26.

Antituberculosis activity of the molecular libraries screening center network library.

Maddry JA, Ananthan S, Goldman RC, Hobrath JV, Kwong CD, Maddox C, Rasmussen L, Reynolds RC, Secrist JA 3rd, Sosa MI, White EL, Zhang W.

Tuberculosis (Edinb). 2009 Sep;89(5):354-63. doi: 10.1016/j.tube.2009.07.006. Epub 2009 Sep 26.

27.

High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.

Ananthan S, Faaleolea ER, Goldman RC, Hobrath JV, Kwong CD, Laughon BE, Maddry JA, Mehta A, Rasmussen L, Reynolds RC, Secrist JA 3rd, Shindo N, Showe DN, Sosa MI, Suling WJ, White EL.

Tuberculosis (Edinb). 2009 Sep;89(5):334-53. doi: 10.1016/j.tube.2009.05.008. Epub 2009 Sep 15.

28.

Assay development and high-throughput antiviral drug screening against Bluetongue virus.

Li Q, Maddox C, Rasmussen L, Hobrath JV, White LE.

Antiviral Res. 2009 Sep;83(3):267-73. doi: 10.1016/j.antiviral.2009.06.004. Epub 2009 Jun 24.

29.

A novel sulindac derivative that does not inhibit cyclooxygenases but potently inhibits colon tumor cell growth and induces apoptosis with antitumor activity.

Piazza GA, Keeton AB, Tinsley HN, Gary BD, Whitt JD, Mathew B, Thaiparambil J, Coward L, Gorman G, Li Y, Sani B, Hobrath JV, Maxuitenko YY, Reynolds RC.

Cancer Prev Res (Phila). 2009 Jun;2(6):572-80. doi: 10.1158/1940-6207.CAPR-09-0001. Epub 2009 May 26.

30.

Recent advances in structure-based virtual screening of G-protein coupled receptors.

Ananthan S, Zhang W, Hobrath JV.

AAPS J. 2009 Mar;11(1):178-85. doi: 10.1208/s12248-009-9094-3. Epub 2009 Mar 17. Review.

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