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Items: 1 to 50 of 66

1.

Efficacy and Improved Resistance Potential of a Cofactor-Independent InhA Inhibitor of Mycobacterium tuberculosis in the C3HeB/FeJ Mouse Model.

Robertson GT, Ektnitphong VA, Scherman MS, McNeil MB, Dennison D, Korkegian A, Smith AJ, Halladay J, Carter DS, Xia Y, Zhou Y, Choi W, Berry PW, Mao W, Hernandez V, Alley MRK, Parish T, Lenaerts AJ.

Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02071-18. doi: 10.1128/AAC.02071-18. Print 2019 Apr.

2.

Comparative pharmacokinetics of spectinamide 1599 after subcutaneous and intrapulmonary aerosol administration in mice.

Rathi C, Lukka PB, Wagh S, Lee RE, Lenaerts AJ, Braunstein M, Hickey A, Gonzalez-Juarrero M, Meibohm B.

Tuberculosis (Edinb). 2019 Jan;114:119-122. doi: 10.1016/j.tube.2018.12.006. Epub 2018 Dec 31.

PMID:
30711150
3.

Discovery of a cofactor-independent inhibitor of Mycobacterium tuberculosis InhA.

Xia Y, Zhou Y, Carter DS, McNeil MB, Choi W, Halladay J, Berry PW, Mao W, Hernandez V, O'Malley T, Korkegian A, Sunde B, Flint L, Woolhiser LK, Scherman MS, Gruppo V, Hastings C, Robertson GT, Ioerger TR, Sacchettini J, Tonge PJ, Lenaerts AJ, Parish T, Alley M.

Life Sci Alliance. 2018 Jun 1;1(3):e201800025. doi: 10.26508/lsa.201800025. eCollection 2018 Jun.

4.

Host Directed Therapy for Chronic Tuberculosis via Intrapulmonary Delivery of Aerosolized Peptide Inhibitors Targeting the IL-10-STAT3 Pathway.

Upadhyay R, Sanchez-Hidalgo A, Wilusz CJ, Lenaerts AJ, Arab J, Yeh J, Stefanisko K, Tarasova NI, Gonzalez-Juarrero M.

Sci Rep. 2018 Nov 9;8(1):16610. doi: 10.1038/s41598-018-35023-0.

5.

Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13.

Aggarwal A, Parai MK, Shetty N, Wallis D, Woolhiser L, Hastings C, Dutta NK, Galaviz S, Dhakal RC, Shrestha R, Wakabayashi S, Walpole C, Matthews D, Floyd D, Scullion P, Riley J, Epemolu O, Norval S, Snavely T, Robertson GT, Rubin EJ, Ioerger TR, Sirgel FA, van der Merwe R, van Helden PD, Keller P, Böttger EC, Karakousis PC, Lenaerts AJ, Sacchettini JC.

Cell. 2017 Jul 13;170(2):249-259.e25. doi: 10.1016/j.cell.2017.06.025. Epub 2017 Jun 29.

6.

Structure-Activity Relationships of Spectinamide Antituberculosis Agents: A Dissection of Ribosomal Inhibition and Native Efflux Avoidance Contributions.

Liu J, Bruhn DF, Lee RB, Zheng Z, Janusic T, Scherbakov D, Scherman MS, Boshoff HI, Das S, Rakesh, Waidyarachchi SL, Brewer TA, Gracia B, Yang L, Bollinger J, Robertson GT, Meibohm B, Lenaerts AJ, Ainsa J, Böttger EC, Lee RE.

ACS Infect Dis. 2017 Jan 13;3(1):72-88. doi: 10.1021/acsinfecdis.6b00158. Epub 2016 Nov 11.

7.

Spectinamides are effective partner agents for the treatment of tuberculosis in multiple mouse infection models.

Robertson GT, Scherman MS, Bruhn DF, Liu J, Hastings C, McNeil MR, Butler MM, Bowlin TL, Lee RB, Lee RE, Lenaerts AJ.

J Antimicrob Chemother. 2017 Mar 1;72(3):770-777. doi: 10.1093/jac/dkw467.

8.

Antibiotic Bactericidal Activity Is Countered by Maintaining pH Homeostasis in Mycobacterium smegmatis.

Bartek IL, Reichlen MJ, Honaker RW, Leistikow RL, Clambey ET, Scobey MS, Hinds AB, Born SE, Covey CR, Schurr MJ, Lenaerts AJ, Voskuil MI.

mSphere. 2016 Aug 24;1(4). pii: e00176-16. doi: 10.1128/mSphere.00176-16. eCollection 2016 Jul-Aug.

9.

Discovery of Novel Oral Protein Synthesis Inhibitors of Mycobacterium tuberculosis That Target Leucyl-tRNA Synthetase.

Palencia A, Li X, Bu W, Choi W, Ding CZ, Easom EE, Feng L, Hernandez V, Houston P, Liu L, Meewan M, Mohan M, Rock FL, Sexton H, Zhang S, Zhou Y, Wan B, Wang Y, Franzblau SG, Woolhiser L, Gruppo V, Lenaerts AJ, O'Malley T, Parish T, Cooper CB, Waters MG, Ma Z, Ioerger TR, Sacchettini JC, Rullas J, Angulo-Barturen I, Pérez-Herrán E, Mendoza A, Barros D, Cusack S, Plattner JJ, Alley MR.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):6271-80. doi: 10.1128/AAC.01339-16. Print 2016 Oct.

10.

Bedaquiline and Pyrazinamide Treatment Responses Are Affected by Pulmonary Lesion Heterogeneity in Mycobacterium tuberculosis Infected C3HeB/FeJ Mice.

Irwin SM, Prideaux B, Lyon ER, Zimmerman MD, Brooks EJ, Schrupp CA, Chen C, Reichlen MJ, Asay BC, Voskuil MI, Nuermberger EL, Andries K, Lyons MA, Dartois V, Lenaerts AJ.

ACS Infect Dis. 2016 Apr 8;2(4):251-267. Epub 2016 Feb 24.

11.

Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.

Rakesh, Bruhn DF, Scherman MS, Singh AP, Yang L, Liu J, Lenaerts AJ, Lee RE.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):388-391. doi: 10.1016/j.bmcl.2015.12.002. Epub 2015 Dec 7.

12.

In vitro and in vivo Evaluation of Synergism between Anti-Tubercular Spectinamides and Non-Classical Tuberculosis Antibiotics.

Bruhn DF, Scherman MS, Liu J, Scherbakov D, Meibohm B, Böttger EC, Lenaerts AJ, Lee RE.

Sci Rep. 2015 Sep 14;5:13985. doi: 10.1038/srep13985.

13.

Susceptibility of Mycobacterium abscessus to antimycobacterial drugs in preclinical models.

Obregón-Henao A, Arnett KA, Henao-Tamayo M, Massoudi L, Creissen E, Andries K, Lenaerts AJ, Ordway DJ.

Antimicrob Agents Chemother. 2015 Nov;59(11):6904-12. doi: 10.1128/AAC.00459-15. Epub 2015 Aug 24.

14.

Heterogeneous disease progression and treatment response in a C3HeB/FeJ mouse model of tuberculosis.

Lanoix JP, Lenaerts AJ, Nuermberger EL.

Dis Model Mech. 2015 Jun;8(6):603-10. doi: 10.1242/dmm.019513. Epub 2015 Mar 30.

15.

Presence of multiple lesion types with vastly different microenvironments in C3HeB/FeJ mice following aerosol infection with Mycobacterium tuberculosis.

Irwin SM, Driver E, Lyon E, Schrupp C, Ryan G, Gonzalez-Juarrero M, Basaraba RJ, Nuermberger EL, Lenaerts AJ.

Dis Model Mech. 2015 Jun;8(6):591-602. doi: 10.1242/dmm.019570. Epub 2015 Mar 30.

16.

Computational pharmacokinetics/pharmacodynamics of rifampin in a mouse tuberculosis infection model.

Lyons MA, Lenaerts AJ.

J Pharmacokinet Pharmacodyn. 2015 Aug;42(4):375-89. doi: 10.1007/s10928-015-9419-z. Epub 2015 May 31.

17.

Nonclinical models for antituberculosis drug development: a landscape analysis.

Gumbo T, Lenaerts AJ, Hanna D, Romero K, Nuermberger E.

J Infect Dis. 2015 Jun 15;211 Suppl 3:S83-95. doi: 10.1093/infdis/jiv183. Review.

PMID:
26009617
18.

Evaluation of moxifloxacin-containing regimens in pathologically distinct murine tuberculosis models.

Li SY, Irwin SM, Converse PJ, Mdluli KE, Lenaerts AJ, Nuermberger EL.

Antimicrob Agents Chemother. 2015 Jul;59(7):4026-30. doi: 10.1128/AAC.00105-15. Epub 2015 Apr 27.

19.

Improving acid-fast fluorescent staining for the detection of mycobacteria using a new nucleic acid staining approach.

Ryan GJ, Shapiro HM, Lenaerts AJ.

Tuberculosis (Edinb). 2014 Sep;94(5):511-8. doi: 10.1016/j.tube.2014.07.004. Epub 2014 Jul 28.

PMID:
25130623
20.

Isolation and purification of Mycobacterium tuberculosis from H37Rv infected guinea pig lungs.

Shi L, Ryan GJ, Bhamidi S, Troudt J, Amin A, Izzo A, Lenaerts AJ, McNeil MR, Belisle JT, Crick DC, Chatterjee D.

Tuberculosis (Edinb). 2014 Sep;94(5):525-30. doi: 10.1016/j.tube.2014.05.003. Epub 2014 Jun 30.

PMID:
25037320
21.

Mycobacterium tuberculosis Lsr2 is a global transcriptional regulator required for adaptation to changing oxygen levels and virulence.

Bartek IL, Woolhiser LK, Baughn AD, Basaraba RJ, Jacobs WR Jr, Lenaerts AJ, Voskuil MI.

MBio. 2014 Jun 3;5(3):e01106-14. doi: 10.1128/mBio.01106-14.

22.

Limited activity of clofazimine as a single drug in a mouse model of tuberculosis exhibiting caseous necrotic granulomas.

Irwin SM, Gruppo V, Brooks E, Gilliland J, Scherman M, Reichlen MJ, Leistikow R, Kramnik I, Nuermberger EL, Voskuil MI, Lenaerts AJ.

Antimicrob Agents Chemother. 2014 Jul;58(7):4026-34. doi: 10.1128/AAC.02565-14. Epub 2014 May 5.

23.

Pentacyclic nitrofurans with in vivo efficacy and activity against nonreplicating Mycobacterium tuberculosis.

Rakesh, Bruhn DF, Scherman MS, Woolhiser LK, Madhura DB, Maddox MM, Singh AP, Lee RB, Hurdle JG, McNeil MR, Lenaerts AJ, Meibohm B, Lee RE.

PLoS One. 2014 Feb 5;9(2):e87909. doi: 10.1371/journal.pone.0087909. eCollection 2014.

24.

Spectinamides: a new class of semisynthetic antituberculosis agents that overcome native drug efflux.

Lee RE, Hurdle JG, Liu J, Bruhn DF, Matt T, Scherman MS, Vaddady PK, Zheng Z, Qi J, Akbergenov R, Das S, Madhura DB, Rathi C, Trivedi A, Villellas C, Lee RB, Rakesh, Waidyarachchi SL, Sun D, McNeil MR, Ainsa JA, Boshoff HI, Gonzalez-Juarrero M, Meibohm B, Böttger EC, Lenaerts AJ.

Nat Med. 2014 Feb;20(2):152-158. doi: 10.1038/nm.3458. Epub 2014 Jan 26.

25.

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis.

Pethe K, Bifani P, Jang J, Kang S, Park S, Ahn S, Jiricek J, Jung J, Jeon HK, Cechetto J, Christophe T, Lee H, Kempf M, Jackson M, Lenaerts AJ, Pham H, Jones V, Seo MJ, Kim YM, Seo M, Seo JJ, Park D, Ko Y, Choi I, Kim R, Kim SY, Lim S, Yim SA, Nam J, Kang H, Kwon H, Oh CT, Cho Y, Jang Y, Kim J, Chua A, Tan BH, Nanjundappa MB, Rao SP, Barnes WS, Wintjens R, Walker JR, Alonso S, Lee S, Kim J, Oh S, Oh T, Nehrbass U, Han SJ, No Z, Lee J, Brodin P, Cho SN, Nam K, Kim J.

Nat Med. 2013 Sep;19(9):1157-60. doi: 10.1038/nm.3262. Epub 2013 Aug 4.

PMID:
23913123
26.

Bayesian models leveraging bioactivity and cytotoxicity information for drug discovery.

Ekins S, Reynolds RC, Kim H, Koo MS, Ekonomidis M, Talaue M, Paget SD, Woolhiser LK, Lenaerts AJ, Bunin BA, Connell N, Freundlich JS.

Chem Biol. 2013 Mar 21;20(3):370-8. doi: 10.1016/j.chembiol.2013.01.011.

27.

A physiologically based pharmacokinetic model of rifampin in mice.

Lyons MA, Reisfeld B, Yang RS, Lenaerts AJ.

Antimicrob Agents Chemother. 2013 Apr;57(4):1763-71. doi: 10.1128/AAC.01567-12. Epub 2013 Jan 28.

28.

Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.

Rakesh, Bruhn D, Madhura DB, Maddox M, Lee RB, Trivedi A, Yang L, Scherman MS, Gilliland JC, Gruppo V, McNeil MR, Lenaerts AJ, Meibohm B, Lee RE.

Bioorg Med Chem. 2012 Oct 15;20(20):6063-72. doi: 10.1016/j.bmc.2012.08.023. Epub 2012 Aug 28.

29.

Comprehensive analysis of methods used for the evaluation of compounds against Mycobacterium tuberculosis.

Franzblau SG, DeGroote MA, Cho SH, Andries K, Nuermberger E, Orme IM, Mdluli K, Angulo-Barturen I, Dick T, Dartois V, Lenaerts AJ.

Tuberculosis (Edinb). 2012 Nov;92(6):453-88. doi: 10.1016/j.tube.2012.07.003. Epub 2012 Aug 30. Review.

30.

Effects of P-MAPA Immunomodulator on Toll-Like Receptors and p53: Potential Therapeutic Strategies for Infectious Diseases and Cancer.

Fávaro WJ, Nunes OS, Seiva FR, Nunes IS, Woolhiser LK, Durán N, Lenaerts AJ.

Infect Agent Cancer. 2012 Jun 18;7(1):14. doi: 10.1186/1750-9378-7-14.

31.

Mouse model for efficacy testing of antituberculosis agents via intrapulmonary delivery.

Gonzalez-Juarrero M, Woolhiser LK, Brooks E, DeGroote MA, Lenaerts AJ.

Antimicrob Agents Chemother. 2012 Jul;56(7):3957-9. doi: 10.1128/AAC.00464-12. Epub 2012 Apr 30.

32.

Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in vitro and for better physical chemical properties for bioavailability.

Scherman MS, North EJ, Jones V, Hess TN, Grzegorzewicz AE, Kasagami T, Kim IH, Merzlikin O, Lenaerts AJ, Lee RE, Jackson M, Morisseau C, McNeil MR.

Bioorg Med Chem. 2012 May 15;20(10):3255-62. doi: 10.1016/j.bmc.2012.03.058. Epub 2012 Mar 31.

33.

Evaluation of a mouse model of necrotic granuloma formation using C3HeB/FeJ mice for testing of drugs against Mycobacterium tuberculosis.

Driver ER, Ryan GJ, Hoff DR, Irwin SM, Basaraba RJ, Kramnik I, Lenaerts AJ.

Antimicrob Agents Chemother. 2012 Jun;56(6):3181-95. doi: 10.1128/AAC.00217-12. Epub 2012 Apr 2.

34.

Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis.

Debnath J, Siricilla S, Wan B, Crick DC, Lenaerts AJ, Franzblau SG, Kurosu M.

J Med Chem. 2012 Apr 26;55(8):3739-55. doi: 10.1021/jm201608g. Epub 2012 Apr 6.

35.

Inhibition of mycolic acid transport across the Mycobacterium tuberculosis plasma membrane.

Grzegorzewicz AE, Pham H, Gundi VA, Scherman MS, North EJ, Hess T, Jones V, Gruppo V, Born SE, Korduláková J, Chavadi SS, Morisseau C, Lenaerts AJ, Lee RE, McNeil MR, Jackson M.

Nat Chem Biol. 2012 Feb 19;8(4):334-41. doi: 10.1038/nchembio.794.

36.

Importance of confirming data on the in vivo efficacy of novel antibacterial drug regimens against various strains of Mycobacterium tuberculosis.

De Groote MA, Gruppo V, Woolhiser LK, Orme IM, Gilliland JC, Lenaerts AJ.

Antimicrob Agents Chemother. 2012 Feb;56(2):731-8. doi: 10.1128/AAC.05701-11. Epub 2011 Dec 5.

37.

A novel metabolite of antituberculosis therapy demonstrates host activation of isoniazid and formation of the isoniazid-NAD+ adduct.

Mahapatra S, Woolhiser LK, Lenaerts AJ, Johnson JL, Eisenach KD, Joloba ML, Boom WH, Belisle JT.

Antimicrob Agents Chemother. 2012 Jan;56(1):28-35. doi: 10.1128/AAC.05486-11. Epub 2011 Oct 28.

38.

Novel pyridopyrazine and pyrimidothiazine derivatives as FtsZ inhibitors.

Mathew B, Srivastava S, Ross LJ, Suling WJ, White EL, Woolhiser LK, Lenaerts AJ, Reynolds RC.

Bioorg Med Chem. 2011 Dec 1;19(23):7120-8. doi: 10.1016/j.bmc.2011.09.062. Epub 2011 Oct 5.

39.

Glycolytic and non-glycolytic functions of Mycobacterium tuberculosis fructose-1,6-bisphosphate aldolase, an essential enzyme produced by replicating and non-replicating bacilli.

de la Paz Santangelo M, Gest PM, Guerin ME, Coinçon M, Pham H, Ryan G, Puckett SE, Spencer JS, Gonzalez-Juarrero M, Daher R, Lenaerts AJ, Schnappinger D, Therisod M, Ehrt S, Sygusch J, Jackson M.

J Biol Chem. 2011 Nov 18;286(46):40219-31. doi: 10.1074/jbc.M111.259440. Epub 2011 Sep 23.

40.

Lipoarabinomannan localization and abundance during growth of Mycobacterium smegmatis.

Dhiman RK, Dinadayala P, Ryan GJ, Lenaerts AJ, Schenkel AR, Crick DC.

J Bacteriol. 2011 Oct;193(20):5802-9. doi: 10.1128/JB.05299-11. Epub 2011 Aug 12.

41.

Location of intra- and extracellular M. tuberculosis populations in lungs of mice and guinea pigs during disease progression and after drug treatment.

Hoff DR, Ryan GJ, Driver ER, Ssemakulu CC, De Groote MA, Basaraba RJ, Lenaerts AJ.

PLoS One. 2011 Mar 21;6(3):e17550. doi: 10.1371/journal.pone.0017550.

42.

Torticollis in mice intravenously infected with Mycobacterium tuberculosis.

Magden ER, Weiner CM, Gilliland JC, DeGroote MA, Lenaerts AJ, Kendall LV.

J Am Assoc Lab Anim Sci. 2011 Mar;50(2):244-7.

43.

Comparative studies evaluating mouse models used for efficacy testing of experimental drugs against Mycobacterium tuberculosis.

De Groote MA, Gilliland JC, Wells CL, Brooks EJ, Woolhiser LK, Gruppo V, Peloquin CA, Orme IM, Lenaerts AJ.

Antimicrob Agents Chemother. 2011 Mar;55(3):1237-47. doi: 10.1128/AAC.00595-10. Epub 2010 Dec 6.

44.

Activities of TMC207, rifampin, and pyrazinamide against Mycobacterium tuberculosis infection in guinea pigs.

Shang S, Shanley CA, Caraway ML, Orme EA, Henao-Tamayo M, Hascall-Dove L, Ackart D, Lenaerts AJ, Basaraba RJ, Orme IM, Ordway DJ.

Antimicrob Agents Chemother. 2011 Jan;55(1):124-31. doi: 10.1128/AAC.00978-10. Epub 2010 Oct 11.

45.

Multiple M. tuberculosis phenotypes in mouse and guinea pig lung tissue revealed by a dual-staining approach.

Ryan GJ, Hoff DR, Driver ER, Voskuil MI, Gonzalez-Juarrero M, Basaraba RJ, Crick DC, Spencer JS, Lenaerts AJ.

PLoS One. 2010 Jun 14;5(6):e11108. doi: 10.1371/journal.pone.0011108.

46.

Evaluation of standard chemotherapy in the guinea pig model of tuberculosis.

Ordway DJ, Shanley CA, Caraway ML, Orme EA, Bucy DS, Hascall-Dove L, Henao-Tamayo M, Harton MR, Shang S, Ackart D, Kraft SL, Lenaerts AJ, Basaraba RJ, Orme IM.

Antimicrob Agents Chemother. 2010 May;54(5):1820-33. doi: 10.1128/AAC.01521-09. Epub 2010 Feb 16.

47.

Discovery, synthesis, and biological evaluation of piperidinol analogs with anti-tuberculosis activity.

Sun D, Scherman MS, Jones V, Hurdle JG, Woolhiser LK, Knudson SE, Lenaerts AJ, Slayden RA, McNeil MR, Lee RE.

Bioorg Med Chem. 2009 May 15;17(10):3588-94. doi: 10.1016/j.bmc.2009.04.005. Epub 2009 Apr 9.

48.

Testing of experimental compounds in a relapse model of tuberculosis using granulocyte-macrophage colony-stimulating factor gene-disrupted mice.

Woolhiser LK, Hoff DR, Marietta KS, Orme IM, Lenaerts AJ.

Antimicrob Agents Chemother. 2009 Jan;53(1):306-8. doi: 10.1128/AAC.01346-07. Epub 2008 Oct 13.

49.

Metronidazole lacks antibacterial activity in guinea pigs infected with Mycobacterium tuberculosis.

Hoff DR, Caraway ML, Brooks EJ, Driver ER, Ryan GJ, Peloquin CA, Orme IM, Basaraba RJ, Lenaerts AJ.

Antimicrob Agents Chemother. 2008 Nov;52(11):4137-40. doi: 10.1128/AAC.00196-08. Epub 2008 Aug 11.

50.

A microbiological assessment of novel nitrofuranylamides as anti-tuberculosis agents.

Hurdle JG, Lee RB, Budha NR, Carson EI, Qi J, Scherman MS, Cho SH, McNeil MR, Lenaerts AJ, Franzblau SG, Meibohm B, Lee RE.

J Antimicrob Chemother. 2008 Nov;62(5):1037-45. doi: 10.1093/jac/dkn307. Epub 2008 Aug 7.

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