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Items: 46

1.

Evaluation of the In Vitro Activity of Eravacycline against a Broad Spectrum of Recent Clinical Anaerobic Isolates.

Snydman DR, McDermott LA, Jacobus NV, Kerstein K, Grossman TH, Sutcliffe JA.

Antimicrob Agents Chemother. 2018 Apr 26;62(5). pii: e02206-17. doi: 10.1128/AAC.02206-17. Print 2018 May.

2.

The Fluorocycline TP-271 Is Efficacious in Models of Aerosolized Bacillus anthracis Infection in BALB/c Mice and Cynomolgus Macaques.

Grossman TH, Anderson MS, Drabek L, Gooldy M, Heine HS, Henning LN, Lin W, Newman JV, Nevarez R, Siefkas-Patterson K, Radcliff AK, Sutcliffe JA.

Antimicrob Agents Chemother. 2017 Sep 22;61(10). pii: e01103-17. doi: 10.1128/AAC.01103-17. Print 2017 Oct.

3.

Heterocyclyl tetracyclines. 2. 7-Methoxy-8-pyrrolidinyltetracyclines: discovery of TP-2758, a potent, orally efficacious antimicrobial against Gram-negative pathogens.

Sun C, Deng Y, Hunt DK, Fyfe C, Chen CL, Clark RB, Grossman TH, Sutcliffe JA, Xiao XY.

J Antibiot (Tokyo). 2018 Feb;71(2):287-297. doi: 10.1038/ja.2017.86. Epub 2017 Jul 26.

PMID:
28743974
4.

The Fluorocycline TP-271 Is Efficacious in Models of Aerosolized Francisella tularensis SCHU S4 Infection in BALB/c Mice and Cynomolgus Macaques.

Grossman TH, Anderson MS, Christ D, Gooldy M, Henning LN, Heine HS, Kindt MV, Lin W, Siefkas-Patterson K, Radcliff AK, Tam VH, Sutcliffe JA.

Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00448-17. doi: 10.1128/AAC.00448-17. Print 2017 Aug.

5.

Fluorocycline TP-271 Is Potent against Complicated Community-Acquired Bacterial Pneumonia Pathogens.

Grossman TH, Fyfe C, O'Brien W, Hackel M, Minyard MB, Waites KB, Dubois J, Murphy TM, Slee AM, Weiss WJ, Sutcliffe JA.

mSphere. 2017 Feb 22;2(1). pii: e00004-17. doi: 10.1128/mSphere.00004-17. eCollection 2017 Jan-Feb.

6.

Heterocyclyl Tetracyclines. 1. 7-Trifluoromethyl-8-Pyrrolidinyltetracyclines: Potent, Broad Spectrum Antibacterial Agents with Enhanced Activity against Pseudomonas aeruginosa.

Deng Y, Sun C, Hunt DK, Fyfe C, Chen CL, Grossman TH, Sutcliffe JA, Xiao XY.

J Med Chem. 2017 Mar 23;60(6):2498-2512. doi: 10.1021/acs.jmedchem.6b01903. Epub 2017 Mar 15.

PMID:
28248499
7.

Eravacycline Is Active against Bacterial Isolates Expressing the Polymyxin Resistance Gene mcr-1.

Fyfe C, LeBlanc G, Close B, Nordmann P, Dumas J, Grossman TH.

Antimicrob Agents Chemother. 2016 Oct 21;60(11):6989-6990. doi: 10.1128/AAC.01646-16. Print 2016 Nov. No abstract available.

8.

Resistance to Macrolide Antibiotics in Public Health Pathogens.

Fyfe C, Grossman TH, Kerstein K, Sutcliffe J.

Cold Spring Harb Perspect Med. 2016 Oct 3;6(10). pii: a025395. doi: 10.1101/cshperspect.a025395. Review.

9.

Tetracycline Antibiotics and Resistance.

Grossman TH.

Cold Spring Harb Perspect Med. 2016 Apr 1;6(4):a025387. doi: 10.1101/cshperspect.a025387. Review.

10.

Erratum for Grossman et al., target- and resistance-based mechanistic studies with TP-434, a novel fluorocycline antibiotic.

Grossman TH, Starosta AL, Fyfe C, O'Brien W, Rothstein DM, Mikolajka A, Wilson DN, Sutcliffe JA.

Antimicrob Agents Chemother. 2015 Sep;59(9):5870. doi: 10.1128/AAC.01551-15. No abstract available.

11.

Design, Synthesis, and Biological Evaluation of Hexacyclic Tetracyclines as Potent, Broad Spectrum Antibacterial Agents.

Sun C, Hunt DK, Chen CL, Deng Y, He M, Clark RB, Fyfe C, Grossman TH, Sutcliffe JA, Xiao XY.

J Med Chem. 2015 Jun 11;58(11):4703-12. doi: 10.1021/acs.jmedchem.5b00262. Epub 2015 May 20.

PMID:
25927406
12.

Eravacycline (TP-434) is efficacious in animal models of infection.

Grossman TH, Murphy TM, Slee AM, Lofland D, Sutcliffe JA.

Antimicrob Agents Chemother. 2015 May;59(5):2567-71. doi: 10.1128/AAC.04354-14. Epub 2015 Feb 17.

13.

Eravacycline (TP-434) is active in vitro against biofilms formed by uropathogenic Escherichia coli.

Grossman TH, O'Brien W, Kerstein KO, Sutcliffe JA.

Antimicrob Agents Chemother. 2015 Apr;59(4):2446-9. doi: 10.1128/AAC.04967-14. Epub 2015 Jan 26.

14.

In vitro susceptibility testing of eravacycline is unaffected by medium age and nonstandard assay parameters.

Grossman TH, Pillar CM, Sahm DF, Sutcliffe JA.

Antimicrob Agents Chemother. 2015 Apr;59(4):2426-7. doi: 10.1128/AAC.04727-14. Epub 2015 Jan 20.

15.

The efflux pump inhibitor timcodar improves the potency of antimycobacterial agents.

Grossman TH, Shoen CM, Jones SM, Jones PL, Cynamon MH, Locher CP.

Antimicrob Agents Chemother. 2015 Mar;59(3):1534-41. doi: 10.1128/AAC.04271-14. Epub 2014 Dec 22.

16.

Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.

Grillot AL, Le Tiran A, Shannon D, Krueger E, Liao Y, O'Dowd H, Tang Q, Ronkin S, Wang T, Waal N, Li P, Lauffer D, Sizensky E, Tanoury J, Perola E, Grossman TH, Doyle T, Hanzelka B, Jones S, Dixit V, Ewing N, Liao S, Boucher B, Jacobs M, Bennani Y, Charifson PS.

J Med Chem. 2014 Nov 13;57(21):8792-816. doi: 10.1021/jm500563g. Epub 2014 Oct 28.

PMID:
25317480
17.

Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.

Perola E, Stamos D, Grillot AL, Ronkin S, Wang T, LeTiran A, Tang Q, Deininger DD, Liao Y, Tian SK, Drumm JE, Nicolau DP, Tessier PR, Mani N, Grossman TH, Charifson PS.

Bioorg Med Chem Lett. 2014 May 1;24(9):2177-81. doi: 10.1016/j.bmcl.2014.03.022. Epub 2014 Mar 19.

PMID:
24685546
18.

Synthesis and biological evaluation of 8-aminomethyltetracycline derivatives as novel antibacterial agents.

Clark RB, He M, Deng Y, Sun C, Chen CL, Hunt DK, O'Brien WJ, Fyfe C, Grossman TH, Sutcliffe JA, Achorn C, Hogan PC, Katz CE, Niu J, Zhang WY, Zhu Z, Ronn M, Xiao XY.

J Med Chem. 2013 Oct 24;56(20):8112-38. doi: 10.1021/jm401211t. Epub 2013 Oct 3.

PMID:
24047201
19.

Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens.

Sutcliffe JA, O'Brien W, Fyfe C, Grossman TH.

Antimicrob Agents Chemother. 2013 Nov;57(11):5548-58. doi: 10.1128/AAC.01288-13. Epub 2013 Aug 26.

20.

Susceptibility of tetracyclines to Tet(a) resistance is independent of interdomain loop sequence.

Fyfe C, Sutcliffe JA, Grossman TH.

Antimicrob Agents Chemother. 2013 May;57(5):2430-1. doi: 10.1128/AAC.00393-13. Epub 2013 Mar 11. No abstract available.

21.

Development and characterization of a Pseudomonas aeruginosa in vitro coupled transcription-translation assay system for evaluation of translation inhibitors.

Fyfe C, Sutcliffe JA, Grossman TH.

J Microbiol Methods. 2012 Sep;90(3):256-61. doi: 10.1016/j.mimet.2012.05.018. Epub 2012 Jun 5.

22.

In vitro activity of TP-271 against Mycobacterium abscessus, Mycobacterium fortuitum, and Nocardia species.

Cynamon M, Jureller J, Desai B, Ramachandran K, Sklaney M, Grossman TH.

Antimicrob Agents Chemother. 2012 Jul;56(7):3986-8. doi: 10.1128/AAC.00743-12. Epub 2012 May 14.

23.

Target- and resistance-based mechanistic studies with TP-434, a novel fluorocycline antibiotic.

Grossman TH, Starosta AL, Fyfe C, O'Brien W, Rothstein DM, Mikolajka A, Wilson DN, Sutcliffe JA.

Antimicrob Agents Chemother. 2012 May;56(5):2559-64. doi: 10.1128/AAC.06187-11. Epub 2012 Feb 21. Erratum in: Antimicrob Agents Chemother. 2015 Sep;59(9):5870.

24.

Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.

Clark RB, Hunt DK, He M, Achorn C, Chen CL, Deng Y, Fyfe C, Grossman TH, Hogan PC, O'Brien WJ, Plamondon L, Rönn M, Sutcliffe JA, Zhu Z, Xiao XY.

J Med Chem. 2012 Jan 26;55(2):606-22. doi: 10.1021/jm201467r. Epub 2012 Jan 6.

PMID:
22148555
25.

Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent.

Xiao XY, Hunt DK, Zhou J, Clark RB, Dunwoody N, Fyfe C, Grossman TH, O'Brien WJ, Plamondon L, Rönn M, Sun C, Zhang WY, Sutcliffe JA.

J Med Chem. 2012 Jan 26;55(2):597-605. doi: 10.1021/jm201465w. Epub 2012 Jan 4.

PMID:
22148514
26.

Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase.

Ronkin SM, Badia M, Bellon S, Grillot AL, Gross CH, Grossman TH, Mani N, Parsons JD, Stamos D, Trudeau M, Wei Y, Charifson PS.

Bioorg Med Chem Lett. 2010 May 1;20(9):2828-31. doi: 10.1016/j.bmcl.2010.03.052. Epub 2010 Mar 15.

PMID:
20356737
28.

Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.

Charifson PS, Grillot AL, Grossman TH, Parsons JD, Badia M, Bellon S, Deininger DD, Drumm JE, Gross CH, LeTiran A, Liao Y, Mani N, Nicolau DP, Perola E, Ronkin S, Shannon D, Swenson LL, Tang Q, Tessier PR, Tian SK, Trudeau M, Wang T, Wei Y, Zhang H, Stamos D.

J Med Chem. 2008 Sep 11;51(17):5243-63. doi: 10.1021/jm800318d. Epub 2008 Aug 9.

PMID:
18690678
29.

Dual targeting of GyrB and ParE by a novel aminobenzimidazole class of antibacterial compounds.

Grossman TH, Bartels DJ, Mullin S, Gross CH, Parsons JD, Liao Y, Grillot AL, Stamos D, Olson ER, Charifson PS, Mani N.

Antimicrob Agents Chemother. 2007 Feb;51(2):657-66. Epub 2006 Nov 20.

30.

In vitro characterization of the antibacterial spectrum of novel bacterial type II topoisomerase inhibitors of the aminobenzimidazole class.

Mani N, Gross CH, Parsons JD, Hanzelka B, Müh U, Mullin S, Liao Y, Grillot AL, Stamos D, Charifson PS, Grossman TH.

Antimicrob Agents Chemother. 2006 Apr;50(4):1228-37.

31.
32.

Active-site residues of Escherichia coli DNA gyrase required in coupling ATP hydrolysis to DNA supercoiling and amino acid substitutions leading to novobiocin resistance.

Gross CH, Parsons JD, Grossman TH, Charifson PS, Bellon S, Jernee J, Dwyer M, Chambers SP, Markland W, Botfield M, Raybuck SA.

Antimicrob Agents Chemother. 2003 Mar;47(3):1037-46.

33.

Multiple inhibitor analysis of the brequinar and leflunomide binding sites on human dihydroorotate dehydrogenase.

McLean JE, Neidhardt EA, Grossman TH, Hedstrom L.

Biochemistry. 2001 Feb 20;40(7):2194-200.

PMID:
11329288
34.

Expression and isolation of antimicrobial small molecules from soil DNA libraries.

MacNeil IA, Tiong CL, Minor C, August PR, Grossman TH, Loiacono KA, Lynch BA, Phillips T, Narula S, Sundaramoorthi R, Tyler A, Aldredge T, Long H, Gilman M, Holt D, Osburne MS.

J Mol Microbiol Biotechnol. 2001 Apr;3(2):301-8.

PMID:
11321587
35.

Sequence analysis and functional characterization of the violacein biosynthetic pathway from Chromobacterium violaceum.

August PR, Grossman TH, Minor C, Draper MP, MacNeil IA, Pemberton JM, Call KM, Holt D, Osburne MS.

J Mol Microbiol Biotechnol. 2000 Oct;2(4):513-9.

PMID:
11075927
36.

Expression and characterization of E. coli-produced soluble, functional human dihydroorotate dehydrogenase: a potential target for immunosuppression.

Neidhardt EA, Punreddy SR, McLean JE, Hedstrom L, Grossman TH.

J Mol Microbiol Biotechnol. 1999 Aug;1(1):183-8.

PMID:
10941801
37.

Cloning the soil metagenome: a strategy for accessing the genetic and functional diversity of uncultured microorganisms.

Rondon MR, August PR, Bettermann AD, Brady SF, Grossman TH, Liles MR, Loiacono KA, Lynch BA, MacNeil IA, Minor C, Tiong CL, Gilman M, Osburne MS, Clardy J, Handelsman J, Goodman RM.

Appl Environ Microbiol. 2000 Jun;66(6):2541-7.

38.

Structures of human dihydroorotate dehydrogenase in complex with antiproliferative agents.

Liu S, Neidhardt EA, Grossman TH, Ocain T, Clardy J.

Structure. 2000 Jan 15;8(1):25-33.

39.

Production of secreted, soluble human two-domain CD4 protein in Escherichia coli.

Osburne MS, Neidhardt EA, Godoy JE, van Schravendijk MR, Grossman TH.

J Immunol Methods. 1999 Apr 22;224(1-2):19-24.

PMID:
10357202
40.

Spontaneous cAMP-dependent derepression of gene expression in stationary phase plays a role in recombinant expression instability.

Grossman TH, Kawasaki ES, Punreddy SR, Osburne MS.

Gene. 1998 Mar 16;209(1-2):95-103.

PMID:
9524234
41.

High-level production of a secreted, heterodimeric alpha beta murine T-cell receptor in Escherichia coli.

Golden A, Khandekar SS, Osburne MS, Kawasaki E, Reinherz EL, Grossman TH.

J Immunol Methods. 1997 Aug 7;206(1-2):163-9.

PMID:
9328579
42.
43.

Sequence and genetic organization of a Bacillus subtilis operon encoding 2,3-dihydroxybenzoate biosynthetic enzymes.

Rowland BM, Grossman TH, Osburne MS, Taber HW.

Gene. 1996 Oct 31;178(1-2):119-23.

PMID:
8921902
45.

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