Publications by authors named "Sylvie Garneau-Tsodikova"

100Publications

Myeloid arginase-1 controls excessive inflammation and modulates T cell responses in Pseudomonas aeruginosa pneumonia.

Immunobiology 2020 Nov 24;226(1):152034. Epub 2020 Nov 24.

University of Kentucky, Department of Pharmacy Practice and Science, 789 S. Limestone Street, Lexington, KY 40536, USA. Electronic address:

View Article and Find Full Text PDF
November 2020

Broad-Spectrum Antifungal Agents: Fluorinated Aryl- and Heteroaryl-Substituted Hydrazones.

ChemMedChem 2021 Jan 16;16(1):124-133. Epub 2020 Oct 16.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, 40536-0596, USA.

View Article and Find Full Text PDF
January 2021

Second Generation of Zafirlukast Derivatives with Improved Activity against the Oral Pathogen .

ACS Med Chem Lett 2020 Oct 18;11(10):1905-1912. Epub 2020 Mar 18.

Department of Pharmaceutical Sciences, University of Kentucky, Lee T. Todd, Jr. Building, 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
October 2020

Unimodular Methylation by Adenylation-Thiolation Domains Containing an Embedded Methyltransferase.

J Mol Biol 2020 Oct 11;432(21):5802-5808. Epub 2020 Sep 11.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
October 2020

Structure-Guided Optimization of Inhibitors of Acetyltransferase Eis from .

ACS Chem Biol 2020 06 18;15(6):1581-1594. Epub 2020 May 18.

Department of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
June 2020

A comprehensive overview of the medicinal chemistry of antifungal drugs: perspectives and promise.

Chem Soc Rev 2020 Apr 6;49(8):2426-2480. Epub 2020 Mar 6.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
April 2020

Modified Aminoglycosides Bind Nucleic Acids in High-Molecular-Weight Complexes.

Antibiotics (Basel) 2020 Feb 21;9(2). Epub 2020 Feb 21.

Department of Microbiology and Center for RNA Biology, The Ohio State University, Columbus, OH 43210-1292, USA.

View Article and Find Full Text PDF
February 2020

Characterization of a Unique Interrupted Adenylation Domain That Can Catalyze Three Reactions.

ACS Chem Biol 2020 01 30;15(1):282-289. Epub 2019 Dec 30.

Department of Pharmaceutical Sciences, College of Pharmacy , University of Kentucky , Lexington , Kentucky 40536-0596 , United States.

View Article and Find Full Text PDF
January 2020

Combining Chalcones with Donepezil to Inhibit Both Cholinesterases and Aβ Fibril Assembly.

Molecules 2019 Dec 24;25(1). Epub 2019 Dec 24.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
December 2019

Distorted Gold(I)-Phosphine Complexes as Antifungal Agents.

J Med Chem 2020 03 16;63(5):2455-2469. Epub 2019 Dec 16.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
March 2020

Resisting resistance: gearing up for war.

Medchemcomm 2019 Sep 7;10(9):1512-1516. Epub 2019 Aug 7.

University of Kentucky , 789 South Limestone Street , Lexington , KY 40536-0596 , USA . Email:

View Article and Find Full Text PDF
September 2019

Probing the Robustness of Inhibitors of Tuberculosis Aminoglycoside Resistance Enzyme Eis by Mutagenesis.

ACS Infect Dis 2019 10 21;5(10):1772-1778. Epub 2019 Aug 21.

Department of Pharmaceutical Sciences, College of Pharmacy , University of Kentucky , 789 South Limestone Street , Lexington , Kentucky 40536-0596 , United States.

View Article and Find Full Text PDF
October 2019

Novel zafirlukast derivatives exhibit selective antibacterial activity against .

Medchemcomm 2019 Jun 10;10(6):926-933. Epub 2019 Jun 10.

Department of Pharmaceutical Sciences , University of Kentucky , Lee T. Todd, Jr. Building, 789 South Limestone Street , Lexington , KY 40536-0596 , USA . Email: ; Tel: +859 218 1686.

View Article and Find Full Text PDF
June 2019

Publisher Correction: Unusual substrate and halide versatility of phenolic halogenase PltM.

Nat Commun 2019 Apr 30;10(1):2053. Epub 2019 Apr 30.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, 40536-0596, USA.

View Article and Find Full Text PDF
April 2019

Unusual substrate and halide versatility of phenolic halogenase PltM.

Nat Commun 2019 03 19;10(1):1255. Epub 2019 Mar 19.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, 40536-0596, USA.

View Article and Find Full Text PDF
March 2019

Investigating the promiscuity of the chloramphenicol nitroreductase from Haemophilus influenzae towards the reduction of 4-nitrobenzene derivatives.

Bioorg Med Chem Lett 2019 05 21;29(9):1127-1132. Epub 2019 Feb 21.

University of Kentucky, College of Pharmacy, Department of Pharmaceutical Sciences, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
May 2019

Probing the limits of interrupted adenylation domains by engineering a trifunctional enzyme capable of adenylation, N-, and S-methylation.

Org Biomol Chem 2019 01;17(5):1169-1175

University of Kentucky, Department of Pharmaceutical Sciences, College of Pharmacy, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
January 2019

N,N'-diaryl-bishydrazones in a biphenyl platform: Broad spectrum antifungal agents.

Eur J Med Chem 2019 Feb 18;164:273-281. Epub 2018 Dec 18.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
February 2019

Multifunctional Donepezil Analogues as Cholinesterase and BACE1 Inhibitors.

Molecules 2018 Dec 8;23(12). Epub 2018 Dec 8.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
December 2018

Synthesis, antimicrobial activity, attenuation of aminoglycoside resistance in MRSA, and ribosomal A-site binding of pyrene-neomycin conjugates.

Eur J Med Chem 2019 Feb 14;163:381-393. Epub 2018 Nov 14.

NUBAD, LLC, Greenville, SC, 29605, United States; Department of Chemistry, Clemson University, Clemson, SC, 29634, United States. Electronic address:

View Article and Find Full Text PDF
February 2019

Synergistic combinations of azoles and antihistamines against Candida species in vitro.

Med Mycol 2019 Oct;57(7):874-884

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, Kentucky, USA.

View Article and Find Full Text PDF
October 2019

Making figures: are you taking the best approach to maximize visibility?

Medchemcomm 2018 Sep 8;9(9):1399-1403. Epub 2018 Aug 8.

University of Kentucky , College of Pharmacy , Department of Pharmaceutical Sciences , 789 South Limestone Street , Lexington , KY 40536-0596 , USA . Email: ; Email:

View Article and Find Full Text PDF
September 2018

Interfering With DNA Decondensation as a Strategy Against Mycobacteria.

Front Microbiol 2018 5;9:2034. Epub 2018 Sep 5.

Electron Microscopy Center Amsterdam, Academic Medical Center, Amsterdam UMC, University of Amsterdam, Amsterdam, Netherlands.

View Article and Find Full Text PDF
September 2018

Nucleoside triphosphate cosubstrates control the substrate profile and efficiency of aminoglycoside 3'--phosphotransferase type IIa.

Medchemcomm 2018 Aug 16;9(8):1332-1339. Epub 2018 Jul 16.

Department of Pharmaceutical Sciences , College of Pharmacy , University of Kentucky , Lexington , KY 40536-0596 , USA . Email: ; Email: ; ; Tel: +859 218 1686.

View Article and Find Full Text PDF
August 2018

Using MbtH-Like Proteins to Alter the Substrate Profile of a Nonribosomal Peptide Adenylation Enzyme.

Chembiochem 2018 10 4;19(20):2186-2194. Epub 2018 Oct 4.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lee T. Todd, Jr. Building, 789 South Limestone St., Lexington, KY, 40536-0596, USA.

View Article and Find Full Text PDF
October 2018

What are the drugs of the future?

Medchemcomm 2018 May 23;9(5):757-758. Epub 2018 Apr 23.

University of Kentucky , 789 South Limestone Street , Lexington , KY 40536-0596 , USA . Email: ; Email:

View Article and Find Full Text PDF
May 2018

What is medicinal chemistry? - Demystifying a rapidly evolving discipline!

Medchemcomm 2017 Sep 16;8(9):1739-1741. Epub 2017 Aug 16.

University of Kentucky , 789 South Limestone Street , Lexington , KY , 40536-0596 USA . Email:

View Article and Find Full Text PDF
September 2017

Derivatives of Ribosome-Inhibiting Antibiotic Chloramphenicol Inhibit the Biosynthesis of Bacterial Cell Wall.

ACS Infect Dis 2018 07 1;4(7):1121-1129. Epub 2018 May 1.

Raymond and Beverly Sackler Faculty of Exact Sciences, School of Chemistry , Tel Aviv University , Tel Aviv , 6997801 , Israel.

View Article and Find Full Text PDF
July 2018

Differential Effects of Linkers on the Activity of Amphiphilic Tobramycin Antifungals.

Molecules 2018 Apr 13;23(4). Epub 2018 Apr 13.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
April 2018

Potent 1,2,4-Triazino[5,6 b]indole-3-thioether Inhibitors of the Kanamycin Resistance Enzyme Eis from Mycobacterium tuberculosis.

ACS Infect Dis 2018 06 30;4(6):1030-1040. Epub 2018 Mar 30.

Department of Pharmaceutical Sciences , University of Kentucky , Lee T. Todd, Jr. Building, 789 South Limestone Street , Lexington , Kentucky 40536-0596 , United States.

View Article and Find Full Text PDF
June 2018

Structural basis for backbone N-methylation by an interrupted adenylation domain.

Nat Chem Biol 2018 05 19;14(5):428-430. Epub 2018 Mar 19.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, USA.

View Article and Find Full Text PDF
May 2018

Engineering Bifunctional Enzymes Capable of Adenylating and Selectively Methylating the Side Chain or Core of Amino Acids.

ACS Synth Biol 2018 02 2;7(2):399-404. Epub 2018 Feb 2.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
February 2018

Acetylation by Eis and Deacetylation by Rv1151c of Mycobacterium tuberculosis HupB: Biochemical and Structural Insight.

Biochemistry 2018 02 18;57(5):781-790. Epub 2018 Jan 18.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
February 2018

Comprehensive review of chemical strategies for the preparation of new aminoglycosides and their biological activities.

Chem Soc Rev 2018 Feb;47(4):1189-1249

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
February 2018

Novel fluconazole derivatives with promising antifungal activity.

Bioorg Med Chem 2018 02 17;26(3):573-580. Epub 2017 Dec 17.

University of Kentucky, Department of Pharmaceutical Sciences, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
February 2018

Evaluation of Aminoglycoside and Carbapenem Resistance in a Collection of Drug-Resistant Pseudomonas aeruginosa Clinical Isolates.

Microb Drug Resist 2018 Sep 20;24(7):1020-1030. Epub 2017 Dec 20.

College of Pharmacy, Department of Pharmaceutical Sciences, University of Kentucky , Lexington, Kentucky.

View Article and Find Full Text PDF
September 2018

Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents.

J Med Chem 2018 01 19;61(1):158-173. Epub 2017 Dec 19.

Department of Pharmaceutical Sciences, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
January 2018

New Application of Neomycin B-Bisbenzimidazole Hybrids as Antifungal Agents.

ACS Infect Dis 2018 02 11;4(2):196-207. Epub 2017 Dec 11.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , Lee T. Todd, Jr. Building, 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
February 2018

Deciphering Nature's Intricate Way of N,S-Dimethylating l-Cysteine: Sequential Action of Two Bifunctional Adenylation Domains.

Biochemistry 2017 11 7;56(46):6087-6097. Epub 2017 Nov 7.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
November 2017

Repurposing antipsychotic drugs into antifungal agents: Synergistic combinations of azoles and bromperidol derivatives in the treatment of various fungal infections.

Eur J Med Chem 2017 Oct 19;139:12-21. Epub 2017 Jul 19.

Department of Pharmaceutical Sciences, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
October 2017

Activation and Loading of the Starter Unit during Thiocoraline Biosynthesis.

Biochemistry 2017 08 17;56(34):4457-4467. Epub 2017 Aug 17.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
August 2017

Novel alkylated azoles as potent antifungals.

Eur J Med Chem 2017 Jun 31;133:309-318. Epub 2017 Mar 31.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
June 2017

Combating Enhanced Intracellular Survival (Eis)-Mediated Kanamycin Resistance of Mycobacterium tuberculosis by Novel Pyrrolo[1,5-a]pyrazine-Based Eis Inhibitors.

ACS Infect Dis 2017 04 17;3(4):302-309. Epub 2017 Feb 17.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
April 2017

Discovery and Optimization of Two Eis Inhibitor Families as Kanamycin Adjuvants against Drug-Resistant .

ACS Med Chem Lett 2016 Dec 15;7(12):1219-1221. Epub 2016 Sep 15.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , Lexington, Kentucky 40536, United States.

View Article and Find Full Text PDF
December 2016

Sulfonamide-Based Inhibitors of Aminoglycoside Acetyltransferase Eis Abolish Resistance to Kanamycin in Mycobacterium tuberculosis.

J Med Chem 2016 12 22;59(23):10619-10628. Epub 2016 Nov 22.

University of Kentucky , Department of Pharmaceutical Sciences, College of Pharmacy, 789 South Limestone St., Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
December 2016

In Vitro Assays to Identify Antibiotics Targeting DNA Metabolism.

Methods Mol Biol 2017 ;1520:175-200

Department of Pharmaceutical Sciences, University of Kentucky, 789 S. Limestone Street, Lexington, KY, 40536, USA.

View Article and Find Full Text PDF
January 2018

Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.

Bioorg Med Chem 2017 01 10;25(1):58-66. Epub 2016 Oct 10.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
January 2017

A complex game of hide and seek: the search for new antifungals.

Medchemcomm 2016 Jul 17;7(7):1285-1306. Epub 2016 May 17.

University of Kentucky, Department of Pharmaceutical Sciences, 789 South Limestone Street, Lexington, KY, USA. ; Tel: 859-218-1686.

View Article and Find Full Text PDF
July 2016

Discovery of Allosteric and Selective Inhibitors of Inorganic Pyrophosphatase from Mycobacterium tuberculosis.

ACS Chem Biol 2016 11 26;11(11):3084-3092. Epub 2016 Sep 26.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
November 2016

Expanding Aminoglycoside Resistance Enzyme Regiospecificity by Mutation and Truncation.

Biochemistry 2016 Oct 26;55(40):5726-5737. Epub 2016 Sep 26.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
October 2016

High throughput LSPR and SERS analysis of aminoglycoside antibiotics.

Analyst 2016 Aug;141(17):5120-6

Département de chimie and Centre for self-assembled chemical structures (CSACS), Université de Montréal, CP 6128 Succ. Centre-Ville, Montreal, QC, CanadaH3C 3J7.

View Article and Find Full Text PDF
August 2016

Flipping the Switch "On" for Aminoglycoside-Resistance Enzymes: The Mechanism Is Finally Revealed!

Structure 2016 07;24(7):1011-3

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
July 2016

Identification of Ebsulfur Analogues with Broad-Spectrum Antifungal Activity.

ChemMedChem 2016 07 23;11(14):1507-16. Epub 2016 Jun 23.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA.

View Article and Find Full Text PDF
July 2016

Ask the experts: how to curb antibiotic resistance and plug the antibiotics gap?

Future Med Chem 2016 06 21;8(10):1027-32. Epub 2016 Jun 21.

Chief Executive Antibiotic Research, York, UK.

View Article and Find Full Text PDF
June 2016

Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.

Bioorg Med Chem 2016 08 4;24(16):3680-6. Epub 2016 Jun 4.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
August 2016

Expanding Substrate Promiscuity by Engineering a Novel Adenylating-Methylating NRPS Bifunctional Enzyme.

Chembiochem 2016 07 3;17(14):1328-32. Epub 2016 Jun 3.

Department of Pharmaceutical Sciences, University of Kentucky, BioPharm Complex (Room 423), 789 South Limestone Street, Lexington, KY, 40536-0596, USA.

View Article and Find Full Text PDF
July 2016

Concise Synthesis of Spergualin-Inspired Molecules With Broad-Spectrum Antibiotic Activity.

Medchemcomm 2015 May 30;6(5):912-918. Epub 2015 Mar 30.

Program in Chemical Biology, University of Michigan, Ann Arbor, MI 48109; Department of Pharmaceutical Chemistry, University of California at San Francisco San Francisco, CA 94158.

View Article and Find Full Text PDF
May 2015

Development of ebsulfur analogues as potent antibacterials against methicillin-resistant Staphylococcus aureus.

Bioorg Med Chem 2016 12 31;24(24):6298-6306. Epub 2016 Mar 31.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
December 2016

A biocatalytic approach to capuramycin analogues by exploiting a substrate permissive N-transacylase CapW.

Org Biomol Chem 2016 Apr 6;14(16):3956-62. Epub 2016 Apr 6.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA.

View Article and Find Full Text PDF
April 2016

A review of patents (2011-2015) towards combating resistance to and toxicity of aminoglycosides.

Medchemcomm 2016;7(1):50-68. Epub 2015 Nov 19.

University of Kentucky, Department of Pharmaceutical Sciences, 789 South Limestone Street, Lexington, KY, USA. ; Tel: 859-218-1686.

View Article and Find Full Text PDF
November 2015

Potent Inhibitors of Acetyltransferase Eis Overcome Kanamycin Resistance in Mycobacterium tuberculosis.

ACS Chem Biol 2016 06 7;11(6):1639-46. Epub 2016 Apr 7.

Department of Pharmaceutical Sciences, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
June 2016

Mechanisms of Resistance to Aminoglycoside Antibiotics: Overview and Perspectives.

Medchemcomm 2016 Jan 21;7(1):11-27. Epub 2015 Sep 21.

Beloit College, Department of Chemistry, 700 College Street, Beloit, WI, USA. ; Tel: 608-363-2273.

View Article and Find Full Text PDF
January 2016

Arginine-linked neomycin B dimers: synthesis, rRNA binding, and resistance enzyme activity.

Medchemcomm 2016 Jan 3;7(1):164-169. Epub 2015 Oct 3.

Clemson University, Department of Chemistry, Clemson, SC, 29634, USA; NUBAD, LLC, Greenville, SC, 29605, USA.

View Article and Find Full Text PDF
January 2016

Differential Effects of Structural Modifications on the Competition of Chalcones for the PIB Amyloid Imaging Ligand-Binding Site in Alzheimer's Disease Brain and Synthetic Aβ Fibrils.

ACS Chem Neurosci 2016 Feb 30;7(2):171-6. Epub 2015 Dec 30.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
February 2016

Synthesis and Biological Activity of Mono- and Di-N-acylated Aminoglycosides.

ACS Med Chem Lett 2015 Nov 30;6(11):1134-9. Epub 2015 Sep 30.

Department of Pharmaceutical Sciences, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
November 2015

A combination approach to treating fungal infections.

Sci Rep 2015 Nov 23;5:17070. Epub 2015 Nov 23.

Department of Pharmaceutical Sciences, University of Kentucky, Lexington, KY, 40536-0596, USA.

View Article and Find Full Text PDF
November 2015

Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.

J Med Chem 2015 Dec 1;58(23):9124-32. Epub 2015 Dec 1.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky , 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
December 2015

Crystal structure of halogenase PltA from the pyoluteorin biosynthetic pathway.

J Struct Biol 2015 Dec 28;192(3):349-357. Epub 2015 Sep 28.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536-0596, USA. Electronic address:

View Article and Find Full Text PDF
December 2015

Effects of structural modifications on the metal binding, anti-amyloid activity, and cholinesterase inhibitory activity of chalcones.

Org Biomol Chem 2015 Sep 6;13(36):9418-26. Epub 2015 Aug 6.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
September 2015

Chemically related 4,5-linked aminoglycoside antibiotics drive subunit rotation in opposite directions.

Nat Commun 2015 Jul 30;6:7896. Epub 2015 Jul 30.

1] Department of Physiology and Biophysics, Weill Cornell Medical College, New York, New York 10065, USA [2] Tri-Institutional Training Program in Chemical Biology, Weill Cornell Medical College, Rockefeller University, Memorial Sloan-Kettering Cancer Center, New York, New York 10065, USA.

View Article and Find Full Text PDF
July 2015

Crystal structure of O-methyltransferase CalO6 from the calicheamicin biosynthetic pathway: a case of challenging structure determination at low resolution.

BMC Struct Biol 2015 Jul 15;15:13. Epub 2015 Jul 15.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, 40536-0596, Lexington, KY, USA.

View Article and Find Full Text PDF
July 2015

Comparative Study of Eis-like Enzymes from Pathogenic and Nonpathogenic Bacteria.

ACS Infect Dis 2015 Jun 4;1(6):272-83. Epub 2015 May 4.

College of Pharmacy, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
June 2015

Amphiphilic Tobramycin Analogues as Antibacterial and Antifungal Agents.

Antimicrob Agents Chemother 2015 Aug 1;59(8):4861-9. Epub 2015 Jun 1.

Department of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky, USA

View Article and Find Full Text PDF
August 2015

Tobramycin Variants with Enhanced Ribosome-Targeting Activity.

Chembiochem 2015 Jul 17;16(11):1565-70. Epub 2015 Jun 17.

Department of Microbiology, Center for RNA Biology, Ohio State University, 484 W. 12th Avenue, Columbus, OH 43210-1292 (USA).

View Article and Find Full Text PDF
July 2015

Enzymatic Evidence for a Revised Congocidine Biosynthetic Pathway.

Chembiochem 2015 Jun 8;16(9):1307-13. Epub 2015 May 8.

Department of Pharmaceutical Sciences, University of Kentucky, BioPharm Complex (Room 423), 789 South Limestone Street, Lexington, KY 40536-0596 (USA).

View Article and Find Full Text PDF
June 2015

Inhibition of aminoglycoside acetyltransferase resistance enzymes by metal salts.

Antimicrob Agents Chemother 2015 Jul 4;59(7):4148-56. Epub 2015 May 4.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky, USA

View Article and Find Full Text PDF
July 2015

Influence of linker length and composition on enzymatic activity and ribosomal binding of neomycin dimers.

Antimicrob Agents Chemother 2015 Jul 20;59(7):3899-905. Epub 2015 Apr 20.

Department of Pharmaceutical Sciences, University of Kentucky, BioPharm Complex, Lexington, Kentucky, USA

View Article and Find Full Text PDF
July 2015

Rapid synthesis, RNA binding, and antibacterial screening of a peptidic-aminosugar (PA) library.

ACS Chem Biol 2015 May 23;10(5):1278-89. Epub 2015 Feb 23.

†Laboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, South Carolina 29634, United States.

View Article and Find Full Text PDF
May 2015

Interrupted adenylation domains: unique bifunctional enzymes involved in nonribosomal peptide biosynthesis.

Nat Prod Rep 2015 May;32(5):641-53

Beloit College, Department of Chemistry, 700 College Street, Beloit, WI 53511, USA.

View Article and Find Full Text PDF
May 2015

Adenylation and S-methylation of cysteine by the bifunctional enzyme TioN in thiocoraline biosynthesis.

J Am Chem Soc 2014 Dec 26;136(49):17350-4. Epub 2014 Nov 26.

Department of Pharmaceutical Sciences, University of Kentucky , Lexington, Kentucky 40536-0596, United States.

View Article and Find Full Text PDF
December 2014

Antimycobacterial activity of DNA intercalator inhibitors of Mycobacterium tuberculosis primase DnaG.

J Antibiot (Tokyo) 2015 Mar 24;68(3):153-7. Epub 2014 Sep 24.

Department of Pharmaceutical Sciences, University of Kentucky, Lexington, KY, USA.

View Article and Find Full Text PDF
March 2015

New trends in aminoglycosides use.

Medchemcomm 2014 Aug;5(8):1075-1091

University of Kentucky, Department of Pharmaceutical Sciences, College of Pharmacy, BioPharm Complex, Room 423, 789 South Limestone Street, Lexington, KY, 40536-0596, U.S.A.

View Article and Find Full Text PDF
August 2014

Inhibition of glioma progression by a newly discovered CD38 inhibitor.

Int J Cancer 2015 Mar 7;136(6):1422-33. Epub 2014 Aug 7.

Department of Neurobiology, George S. Wise Faculty of Life Sciences, Tel Aviv University, Ramat Aviv, Israel.

View Article and Find Full Text PDF
March 2015

A random sequential mechanism of aminoglycoside acetylation by Mycobacterium tuberculosis Eis protein.

PLoS One 2014 3;9(4):e92370. Epub 2014 Apr 3.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, BioPharm Complex, Lexington, Kentucky, United States of America.

View Article and Find Full Text PDF
January 2015

Chemical and structural insights into the regioversatility of the aminoglycoside acetyltransferase Eis.

Chembiochem 2013 Nov 17;14(16):2127-35. Epub 2013 Sep 17.

Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109 (USA); Life Sciences Institute, University of Michigan, Ann Arbor, MI 48109 (USA).

View Article and Find Full Text PDF
November 2013

KtzJ-dependent serine activation and O-methylation by KtzH for kutznerides biosynthesis.

J Antibiot (Tokyo) 2014 Jan 9;67(1):59-64. Epub 2013 Oct 9.

Department of Pharmaceutical Sciences, University of Kentucky, Lexington, KY, USA.

View Article and Find Full Text PDF
January 2014

Discovery of inhibitors of Bacillus anthracis primase DnaG.

Biochemistry 2013 Oct 19;52(39):6905-10. Epub 2013 Sep 19.

Department of Medicinal Chemistry, College of Pharmacy, University of Michigan , Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
October 2013

Resistance in tuberculosis: what do we know and where can we go?

Front Microbiol 2013 23;4:208. Epub 2013 Jul 23.

Department of Pharmaceutical Sciences, University of Kentucky Lexington, KY, USA.

View Article and Find Full Text PDF
July 2013

Strategies to overcome the action of aminoglycoside-modifying enzymes for treating resistant bacterial infections.

Future Med Chem 2013 Jul;5(11):1285-309

University of Kentucky, College of Pharmacy, Bio Pharm Complex, Room 423, Lexington, KY 40536-0596, USA.

View Article and Find Full Text PDF
July 2013

Redesign of substrate specificity and identification of the aminoglycoside binding residues of Eis from Mycobacterium tuberculosis.

Biochemistry 2013 Jul 16;52(30):5125-32. Epub 2013 Jul 16.

Life Sciences Institute, 210 Washtenaw Avenue, University of Michigan, Ann Arbor, Michigan 48109-2216, United States.

View Article and Find Full Text PDF
July 2013

Amyloid-β probes: Review of structure-activity and brain-kinetics relationships.

Beilstein J Org Chem 2013 28;9:1012-44. Epub 2013 May 28.

Department of Pharmaceutical Sciences, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, United States ; Life Sciences Institute and Department of Medicinal Chemistry, University of Michigan, 210 Washtenaw Ave, Ann Arbor, MI, 48109-2216, United States.

View Article and Find Full Text PDF
June 2013

Investigation of the role of linker moieties in bifunctional tacrine hybrids.

Bioorg Med Chem 2013 Jun 14;21(12):3614-23. Epub 2013 Mar 14.

Department of Medicinal Chemistry in the College of Pharmacy, University of Michigan, Ann Arbor, MI 48109-2216, USA.

View Article and Find Full Text PDF
June 2013

Domain dissection and characterization of the aminoglycoside resistance enzyme ANT(3″)-Ii/AAC(6')-IId from Serratia marcescens.

Biochimie 2013 Jun 26;95(6):1319-25. Epub 2013 Feb 26.

Life Sciences Institute, 210 Washtenaw Ave, University of Michigan, Ann Arbor, MI 48109-2216, USA.

View Article and Find Full Text PDF
June 2013

Unexpected N-acetylation of capreomycin by mycobacterial Eis enzymes.

J Antimicrob Chemother 2013 Apr 11;68(4):800-5. Epub 2012 Dec 11.

Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA.

View Article and Find Full Text PDF
April 2013

Biochemical and structural analysis of aminoglycoside acetyltransferase Eis from Anabaena variabilis.

Mol Biosyst 2012 Oct;8(12):3305-13

University of Michigan, Life Sciences Institute, 210 Washtenaw Ave, Ann Arbor, MI 48109, USA.

View Article and Find Full Text PDF
October 2012