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Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.
Howard S, Amin N, Benowitz AB, Chiarparin E, Cui H, Deng X, Heightman TD, Holmes DJ, Hopkins A, Huang J, Jin Q, Kreatsoulas C, Martin AC, Massey F, McCloskey L, Mortenson PN, Pathuri P, Tisi D, Williams PA. Howard S, et al. Among authors: huang j. ACS Med Chem Lett. 2013 Oct 18;4(12):1208-12. doi: 10.1021/ml4003277. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900632 Free PMC article.
Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.
Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Huang J, Jones GE, Sukmar SK, Spitzfaden C, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND. Miles TJ, et al. Among authors: huang j. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5437-41. doi: 10.1016/j.bmcl.2013.07.013. Epub 2013 Jul 17. Bioorg Med Chem Lett. 2013. PMID: 23968823
Frequency of Spontaneous Resistance to Peptide Deformylase Inhibitor GSK1322322 in Haemophilus influenzae, Staphylococcus aureus, Streptococcus pyogenes, and Streptococcus pneumoniae.
Min S, Ingraham K, Huang J, McCloskey L, Rilling S, Windau A, Pizzollo J, Butler D, Aubart K, Miller LA, Zalacain M, Holmes DJ, O'Dwyer K. Min S, et al. Among authors: huang j. Antimicrob Agents Chemother. 2015 Aug;59(8):4644-52. doi: 10.1128/AAC.00484-15. Epub 2015 May 26. Antimicrob Agents Chemother. 2015. PMID: 26014938 Free PMC article.
Discovery and Characterization of a Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate Synthase.
Concha N, Huang J, Bai X, Benowitz A, Brady P, Grady LC, Kryn LH, Holmes D, Ingraham K, Jin Q, Pothier Kaushansky L, McCloskey L, Messer JA, O'Keefe H, Patel A, Satz AL, Sinnamon RH, Schneck J, Skinner SR, Summerfield J, Taylor A, Taylor JD, Evindar G, Stavenger RA. Concha N, et al. Among authors: huang j. J Med Chem. 2016 Aug 11;59(15):7299-304. doi: 10.1021/acs.jmedchem.6b00746. Epub 2016 Jul 20. J Med Chem. 2016. PMID: 27379833
Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase.
Chan PF, Germe T, Bax BD, Huang J, Thalji RK, Bacqué E, Checchia A, Chen D, Cui H, Ding X, Ingraham K, McCloskey L, Raha K, Srikannathasan V, Maxwell A, Stavenger RA. Chan PF, et al. Among authors: huang j. Proc Natl Acad Sci U S A. 2017 May 30;114(22):E4492-E4500. doi: 10.1073/pnas.1700721114. Epub 2017 May 15. Proc Natl Acad Sci U S A. 2017. PMID: 28507124 Free PMC article.
Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening.
Machutta CA, Kollmann CS, Lind KE, Bai X, Chan PF, Huang J, Ballell L, Belyanskaya S, Besra GS, Barros-Aguirre D, Bates RH, Centrella PA, Chang SS, Chai J, Choudhry AE, Coffin A, Davie CP, Deng H, Deng J, Ding Y, Dodson JW, Fosbenner DT, Gao EN, Graham TL, Graybill TL, Ingraham K, Johnson WP, King BW, Kwiatkowski CR, Lelièvre J, Li Y, Liu X, Lu Q, Lehr R, Mendoza-Losana A, Martin J, McCloskey L, McCormick P, O'Keefe HP, O'Keeffe T, Pao C, Phelps CB, Qi H, Rafferty K, Scavello GS, Steiginga MS, Sundersingh FS, Sweitzer SM, Szewczuk LM, Taylor A, Toh MF, Wang J, Wang M, Wilkins DJ, Xia B, Yao G, Zhang J, Zhou J, Donahue CP, Messer JA, Holmes D, Arico-Muendel CC, Pope AJ, Gross JW, Evindar G. Machutta CA, et al. Among authors: huang j. Nat Commun. 2017 Jul 17;8:16081. doi: 10.1038/ncomms16081. Nat Commun. 2017. PMID: 28714473 Free PMC article.
Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones.
Jeannot F, Taillier T, Despeyroux P, Renard S, Rey A, Mourez M, Poeverlein C, Khichane I, Perrin MA, Versluys S, Stavenger RA, Huang J, Germe T, Maxwell A, Cao S, Huseby DL, Hughes D, Bacqué E. Jeannot F, et al. Among authors: huang j. J Med Chem. 2018 Apr 26;61(8):3565-3581. doi: 10.1021/acs.jmedchem.7b01892. Epub 2018 Apr 10. J Med Chem. 2018. PMID: 29596745
Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.
Miles TJ, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Rittenhouse S, Xiang H, Pearson N. Miles TJ, et al. Among authors: huang j. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7483-8. doi: 10.1016/j.bmcl.2011.09.114. Epub 2011 Oct 10. Bioorg Med Chem Lett. 2011. PMID: 22030032
Structural basis of DNA gyrase inhibition by antibacterial QPT-1, anticancer drug etoposide and moxifloxacin.
Chan PF, Srikannathasan V, Huang J, Cui H, Fosberry AP, Gu M, Hann MM, Hibbs M, Homes P, Ingraham K, Pizzollo J, Shen C, Shillings AJ, Spitzfaden CE, Tanner R, Theobald AJ, Stavenger RA, Bax BD, Gwynn MN. Chan PF, et al. Among authors: huang j. Nat Commun. 2015 Dec 7;6:10048. doi: 10.1038/ncomms10048. Nat Commun. 2015. PMID: 26640131 Free PMC article.
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