19952019
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Research Output 1995 2019

2014

Synthesis of complex and diverse compounds through ring distortion of abietic acid

Rafferty, R. J., Hicklin, R. W., Maloof, K. A. & Hergenrother, P. J., Jan 3 2014, In : Angewandte Chemie - International Edition. 53, 1, p. 220-224 5 p.

Research output: Contribution to journalArticle

Biological Products
Molecules
Acids
Carbon
Lacquers

Targeting toxic RNAs that cause myotonic dystrophy type 1 (DM1) with a bisamidinium inhibitor

Wong, C. H., Nguyen, L., Peh, J., Luu, L. M., Sanchez, J. S., Richardson, S. L., Tuccinardi, T., Tsoi, H., Chan, W. Y., Chan, H. Y. E., Baranger, A. M., Hergenrother, P. J. & Zimmerman, S. C., Apr 30 2014, In : Journal of the American Chemical Society. 136, 17, p. 6355-6361 7 p.

Research output: Contribution to journalArticle

Myotonic Dystrophy
Poisons
RNA
ligand
targeting

Total synthesis, stereochemical assignment, and biological activity of all known (-)-trigonoliimines

Han, S., Morrison, K. C., Hergenrother, P. J. & Movassaghi, M., Jan 17 2014, In : Journal of Organic Chemistry. 79, 2, p. 473-486 14 p.

Research output: Contribution to journalArticle

Bioactivity
Alkaloids
Stereochemistry
Biological Products
Oxidation
2013

A ring-distortion strategy to construct stereochemically complex and structurally diverse compounds from natural products

Huigens, R. W., Morrison, K. C., Hicklin, R. W., Timothy, T. A., Richter, M. F. & Hergenrother, P. J., Mar 1 2013, In : Nature Chemistry. 5, 3, p. 195-202 8 p.

Research output: Contribution to journalArticle

Biological Products
Screening
Lead compounds
Chemical properties
Carbon

Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds

Granchi, C., Calvaresi, E. C., Tuccinardi, T., Paterni, I., Macchia, M., Martinelli, A., Hergenrother, P. J. & Minutolo, F., Oct 14 2013, In : Organic and Biomolecular Chemistry. 11, 38, p. 6588-6596 9 p.

Research output: Contribution to journalArticle

Scaffolds
inhibitors
carboxylates
cancer
Cells

Detection of endogenous MazF enzymatic activity in Staphylococcus aureus

Van Rensburg, J. J. & Hergenrother, P. J., Oct 8 2013, In : Analytical Biochemistry. 443, 1, p. 81-87 7 p.

Research output: Contribution to journalArticle

Antitoxins
Staphylococcus aureus
Assays
Endoribonucleases
Gene encoding

Dual targeting of the warburg effect with a glucose-conjugated lactate dehydrogenase inhibitor

Calvaresi, E. C., Granchi, C., Tuccinardi, T., Di Bussolo, V., Huigens, R. W., Lee, H. Y., Palchaudhuri, R., Macchia, M., Martinelli, A., Minutolo, F. & Hergenrother, P. J., Nov 25 2013, In : ChemBioChem. 14, 17, p. 2263-2267 5 p.

Research output: Contribution to journalArticle

L-Lactate Dehydrogenase
Glycolysis
Glucose
Enzyme Inhibitors
Nutrition

Efficient NQO1 substrates are potent and selective anticancer agents

Parkinson, E. I., Bair, J. S., Cismesia, M. & Hergenrother, P. J., Oct 18 2013, In : ACS chemical biology. 8, 10, p. 2173-2183 11 p.

Research output: Contribution to journalArticle

Quinones
Antineoplastic Agents
apaziquone
Substrates
Precision Medicine

External cavity laser biosensor

Ge, C., Lu, M., George, S., Flood, T. A., Wagner, C., Zheng, J., Pokhriyal, A., Eden, J. G., Hergenrother, P. J. & Cunningham, B. T., Apr 7 2013, In : Lab on a Chip. 13, 7, p. 1247-1256 10 p.

Research output: Contribution to journalArticle

Optics and Photonics
Laser resonators
Biosensing Techniques
Photonic crystals
Biosensors

Glucose conjugation for the specific targeting and treatment of cancer

Calvaresi, E. C. & Hergenrother, P. J., May 7 2013, In : Chemical Science. 4, 6, p. 2319-2333 15 p.

Research output: Contribution to journalArticle

Glycoconjugates
Glucose
Sugars
Facilitative Glucose Transport Proteins
Cytotoxins

Synthesis and anticancer activity of all known (-)-agelastatin alkaloids

Han, S., Siegel, D. S., Morrison, K. C., Hergenrother, P. J. & Movassaghi, M., Dec 6 2013, In : Journal of Organic Chemistry. 78, 23, p. 11970-11984 15 p.

Research output: Contribution to journalArticle

Alkaloids
Cells
Blood
Imidazoles
Confocal microscopy

Synthesis and anticancer activity of epipolythiodiketopiperazine alkaloids

Boyer, N., Morrison, K. C., Kim, J., Hergenrother, P. J. & Movassaghi, M., Mar 4 2013, In : Chemical Science. 4, 4, p. 1646-1657 12 p.

Research output: Contribution to journalArticle

Alkaloids
Biological Products
Cells
Derivatives
Cell death

Synthesis of (±)-actinophyllic acid and analogs: Applications of cascade reactions and diverted total synthesis

Granger, B. A., Jewett, I. T., Butler, J. D., Hua, B., Knezevic, C. E., Parkinson, E. I., Hergenrother, P. J. & Martin, S. F., Sep 4 2013, In : Journal of the American Chemical Society. 135, 35, p. 12984-12986 3 p.

Research output: Contribution to journalArticle

Acids
acid
Chemical operations
Indole Alkaloids
Alkaloids
2012

An NQO1 substrate with potent antitumor activity that selectively kills by PARP1-induced programmed necrosis

Huang, X., Dong, Y., Bey, E. A., Kilgore, J. A., Bair, J. S., Li, L. S., Patel, M., Parkinson, E. I., Wang, Y., Williams, N. S., Gao, J., Hergenrother, P. J. & Boothman, D. A., Jun 15 2012, In : Cancer Research. 72, 12, p. 3038-3047 10 p.

Research output: Contribution to journalArticle

Necrosis
Neoplasms
NAD
Oxidation-Reduction
Reactive Oxygen Species

Artificial activation of toxin-antitoxin systems as an antibacterial strategy

Williams, J. J. & Hergenrother, P., Jun 1 2012, In : Trends in Microbiology. 20, 6, p. 291-298 8 p.

Research output: Contribution to journalReview article

Antitoxins
Bacterial Chromosomes
Bacterial Genomes
Genes
Plasmids

Differential effects of procaspase-3 activating compounds in the induction of cancer cell death

West, D. C., Qin, Y., Peterson, Q. P., Thomas, D. L., Palchaudhuri, R., Morrison, K. C., Lucas, P. W., Palmer, A. E., Fan, T. M. & Hergenrother, P. J., May 7 2012, In : Molecular Pharmaceutics. 9, 5, p. 1425-1434 10 p.

Research output: Contribution to journalArticle

Caspase 3
Cell Death
Neoplasms
Apoptosis
2-carboxyarabinitol 1-phosphate

Identification of a Novel Protein Synthesis Inhibitor Active against Gram-Positive Bacteria

Eibergen, N. R., Im, I., Patel, N. Y. & Hergenrother, P. J., Mar 1 2012, In : ChemBioChem. 13, 4, p. 574-583 10 p.

Research output: Contribution to journalArticle

Protein Synthesis Inhibitors
Gram-Positive Bacteria
Bacteria
Staphylococcus aureus
Methicillin

Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1)

Hsu, D. C., Roth, H. S., West, D. C., Botham, R. C., Novotny, C. J., Schmid, S. C. & Hergenrother, P. J., Jan 9 2012, In : ACS Combinatorial Science. 14, 1, p. 44-50 7 p.

Research output: Contribution to journalArticle

Caspase 3
Cells
Cell culture
Apoptosis
Hydrazones

Selective small molecule inhibition of poly(ADP-ribose) glycohydrolase (PARG)

Finch, K. E., Knezevic, C. E., Nottbohm, A. C., Partlow, K. C. & Hergenrother, P. J., Mar 16 2012, In : ACS chemical biology. 7, 3, p. 563-570 8 p.

Research output: Contribution to journalArticle

Poly(ADP-ribose) Polymerases
ADP-ribosylarginine hydrolase
Molecules
DNA Damage
Poly Adenosine Diphosphate Ribose

Structure and mechanism of a canonical poly(ADP-ribose) glycohydrolase

Dunstan, M. S., Barkauskaite, E., Lafite, P., Knezevic, C. E., Brassington, A., Ahel, M., Hergenrother, P. J., Leys, D. & Ahel, I., Jul 6 2012, In : Nature communications. 3, 878.

Research output: Contribution to journalArticle

ribose
adenosine diphosphate
Glycoside Hydrolases
inhibitors
Tetrahymena thermophila

Whole cell microtubule analysis by flow cytometry

Morrison, K. C. & Hergenrother, P. J., Jan 1 2012, In : Analytical Biochemistry. 420, 1, p. 26-32 7 p.

Research output: Contribution to journalArticle

Flow cytometry
Tubulin
Microtubules
Flow Cytometry
Polymerization
2011

Cribrostatin 6 induces death in cancer cells through a reactive oxygen species (ROS)-mediated mechanism

Hoyt, M. T., Palchaudhuri, R. & Hergenrother, P., Aug 1 2011, In : Investigational New Drugs. 29, 4, p. 562-573 12 p.

Research output: Contribution to journalArticle

Reactive Oxygen Species
Neoplasms
Cell Cycle Checkpoints
Biological Products
Antineoplastic Agents

Discovery of N-hydroxyindole-based inhibitors of human lactate dehydrogenase isoform A (LDH-A) as starvation agents against cancer cells

Granchi, C., Roy, S., Giacomelli, C., MacChia, M., Tuccinardi, T., Martinelli, A., Lanza, M., Betti, L., Giannaccini, G., Lucacchini, A., Funel, N., León, L. G., Giovannetti, E., Peters, G. J., Palchaudhuri, R., Calvaresi, E. C., Hergenrother, P. J. & Minutolo, F., Mar 24 2011, In : Journal of Medicinal Chemistry. 54, 6, p. 1599-1612 14 p.

Research output: Contribution to journalArticle

Starvation
L-Lactate Dehydrogenase
Protein Isoforms
Glycolysis
Neoplasms
Photonic crystals
Biosensors
Modulators
Screening
Throughput

Pharmacokinetics and derivation of an anticancer dosing regimen for PAC-1, a preferential small molecule activator of procaspase-3, in healthy dogs

Lucas, P. W., Schmit, J. M., Peterson, Q. P., West, D. C., Hsu, D. C., Novotny, C. J., Dirikolu, L., Churchwell, M. I., Doerge, D. R., Garrett, L. D., Hergenrother, P. & Fan, T. M., Oct 1 2011, In : Investigational New Drugs. 29, 5, p. 901-911 11 p.

Research output: Contribution to journalArticle

Caspase 3
Pharmacokinetics
Dogs
Lymphoma
2-carboxyarabinitol 1-phosphate

Runaway ROS as a selective anticancer strategy

Parkinson, E. I. & Hergenrother, P. J., Nov 4 2011, In : ChemMedChem. 6, 11, p. 1957-1959 3 p.

Research output: Contribution to journalComment/debate

Phytogenic Antineoplastic Agents
Dioxolanes
Glutathione S-Transferase pi
Homeless Youth
Oxidative stress

Toxin-antitoxin (TA) systems are prevalent and transcribed in clinical isolates of Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus

Williams, J. J., Halvorsen, E. M., Dwyer, E. M., Difazio, R. M. & Hergenrother, P. J., Sep 1 2011, In : FEMS microbiology letters. 322, 1, p. 41-50 10 p.

Research output: Contribution to journalArticle

Antitoxins
Methicillin-Resistant Staphylococcus aureus
Pseudomonas aeruginosa
Bacteria
Reverse Transcriptase Polymerase Chain Reaction

Transcript profiling and RNA interference as tools to identify small molecule mechanisms and therapeutic potential

Palchaudhuri, R. & Hergenrother, P. J., Jan 21 2011, In : ACS chemical biology. 6, 1, p. 21-32 12 p.

Research output: Contribution to journalReview article

RNA Interference
RNA
Molecules
Pattern matching
Drug Discovery

Triphenylmethyl derivatives enhances the anticancer effect of immunotoxins

Risberg, K., Guldvik, I. J., Palchaudhuri, R., Xi, Y., Ju, J., Fodstad, Ø., Hergenrother, P. J. & Andersson, Y., Jun 1 2011, In : Journal of Immunotherapy. 34, 5, p. 438-447 10 p.

Research output: Contribution to journalArticle

Immunotoxins
Organophosphonates
Stearoyl-CoA Desaturase
Neoplasms
Nude Rats

Txe, an endoribonuclease of the enterococcal Axe-Txe toxin-antitoxin system, cleaves mRNA and inhibits protein synthesis

Halvorsen, E. M., Williams, J. J., Bhimani, A. J., Billings, E. A. & Hergenrother, P. J., Feb 1 2011, In : Microbiology. 157, 2, p. 387-397 11 p.

Research output: Contribution to journalArticle

Endoribonucleases
Antitoxins
Messenger RNA
Poisons
Operon
2010

A noncompetitive small molecule inhibitor of estrogen-regulated gene expression and breast cancer cell growth that enhances proteasome-dependent degradation of estrogen receptor α

Kretzer, N. M., Cherian, M. T., Mao, C., Aninye, I. O., Reynolds, P. D., Schiff, R., Hergenrother, P., Nordeen, S. K., Wilson, E. M. & Shapiro, D. J., Dec 31 2010, In : Journal of Biological Chemistry. 285, 53, p. 41863-41873 11 p.

Research output: Contribution to journalArticle

Cell growth
Proteasome Endopeptidase Complex
Gene expression
Estrogen Receptors
Estrogens

Chemistry and biology of deoxynyboquinone, a potent inducer of cancer cell death

Bair, J. S., Palchaudhuri, R. & Hergenrother, P. J., Apr 21 2010, In : Journal of the American Chemical Society. 132, 15, p. 5469-5478 10 p.

Research output: Contribution to journalArticle

Cell death
Helper-Inducer T-Lymphocytes
cancer
Cell Death
Cells

Discovery and canine preclinical assessment of a nontoxic procaspase-3-activating compound

Peterson, Q. P., Hsu, D. C., Novotny, C. J., West, D. C., Kim, D., Schmit, J. M., Dirikolu, L., Hergenrother, P. J. & Fan, T. M., Sep 15 2010, In : Cancer Research. 70, 18, p. 7232-7241 10 p.

Research output: Contribution to journalArticle

Caspase 3
Canidae
Dogs
Caspases
Neoplasms

Identification of novel synthetic toll-like receptor 2 agonists by high throughput screening

Guan, Y., Omueti-Ayoade, K., Mutha, S. K., Hergenrother, P. J. & Tapping, R. I., Jul 30 2010, In : Journal of Biological Chemistry. 285, 31, p. 23755-23762 8 p.

Research output: Contribution to journalArticle

Toll-Like Receptor 2
Toll-Like Receptors
Screening
Throughput
Small Molecule Libraries

N -((1-benzyl-1 H -1,2,3-triazol-4-yl)methyl)arylamide as a new scaffold that provides rapid access to antimicrotubule agents: Synthesis and evaluation of antiproliferative activity against select cancer cell lines

Stefely, J. A., Palchaudhuri, R., Miller, P. A., Peterson, R. J., Moraski, G. C., Hergenrother, P. J. & Miller, M. J., Apr 22 2010, In : Journal of Medicinal Chemistry. 53, 8, p. 3389-3395 7 p.

Research output: Contribution to journalArticle

Tubulin
HeLa Cells
Polymerization
Computer Simulation
Cell Line

Phenylcinnamides as novel antimitotic agents

Leslie, B. J., Holaday, C. R., Nguyen, T. & Hergenrother, P. J., May 27 2010, In : Journal of Medicinal Chemistry. 53, 10, p. 3964-3972 9 p.

Research output: Contribution to journalArticle

Antimitotic Agents
P-Glycoprotein
Neoplasms
Cell Death
M Phase Cell Cycle Checkpoints

Preparation of the caspase-3/7 substrate Ac-DEVD-pNA by solution-phase peptide synthesis

Peterson, Q. P., Goode, D. R., West, D. C., Botham, R. C. & Hergenrother, P., Feb 1 2010, In : Nature Protocols. 5, 2, p. 294-302 9 p.

Research output: Contribution to journalArticle

Caspase 7
Caspases
Caspase 3
Peptides
Substrates
2009

A method for identifying small molecule aggregators using photonic crystal biosensor microplates

Chan, L. L., Lidstone, E. A., Finch, K. E., Heeres, J. T., Hergenrother, P. J. & Cunningham, B. T., Jan 1 2009, Proceedings of the 31st Annual International Conference of the IEEE Engineering in Medicine and Biology Society: Engineering the Future of Biomedicine, EMBC 2009. IEEE Computer Society, p. 788-791 4 p. 5333796. (Proceedings of the 31st Annual International Conference of the IEEE Engineering in Medicine and Biology Society: Engineering the Future of Biomedicine, EMBC 2009).

Research output: Chapter in Book/Report/Conference proceedingConference contribution

Optics and Photonics
Biosensing Techniques
Photonic crystals
Biosensors
Assays

A Method for Identifying Small-Molecule Aggregators Using Photonic Crystal Biosensor Microplates

Chan, L. L., Lidstone, E. A., Finch, K. E., Heeres, J. T., Hergenrother, P. J. & Cunningham, B. T., Dec 2009, In : Journal of Laboratory Automation. 14, 6, p. 348-359 12 p.

Research output: Contribution to journalArticle

Optics and Photonics
Biosensing Techniques
Photonic crystals
Biosensors
Assays
Optics and Photonics
Biosensing Techniques
Photonic crystals
Biosensors
Assays

Identifying modulators of protein-protein interactions using photonic crystal biosensors

Heeres, J. T., Kim, S. H., Leslie, B. J., Lidstone, E. A., Cunningham, B. T. & Hergenrother, P. J., Dec 30 2009, In : Journal of the American Chemical Society. 131, 51, p. 18202-18203 2 p.

Research output: Contribution to journalArticle

Optics and Photonics
Biosensing Techniques
Photonic crystals
Biosensors
Modulators

Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells

Rosenthal, A. S., Chen, X., Liu, J. O., West, D. C., Hergenrother, P. J., Shapiro, T. A. & Posner, G. H., Feb 26 2009, In : Journal of Medicinal Chemistry. 52, 4, p. 1198-1203 6 p.

Research output: Contribution to journalArticle

Sulfones
Malaria
Mefloquine
Neoplasms
Cell Line

PAC-1 Activates Procaspase-3 in Vitro through Relief of Zinc-Mediated Inhibition

Peterson, Q. P., Goode, D. R., West, D. C., Ramsey, K. N., Lee, J. J. Y. & Hergenrother, P. J., Apr 24 2009, In : Journal of Molecular Biology. 388, 1, p. 144-158 15 p.

Research output: Contribution to journalArticle

Caspase 3
Zinc
Apoptosis
2-carboxyarabinitol 1-phosphate
In Vitro Techniques

Procaspase-3 activation as an anti-cancer strategy: Structure-activity relationship of procaspase-activating compound 1 (PAC-1) and its cellular co-localization with caspase-3

Peterson, Q. P., Hsu, D. C., Goode, D. R., Novotny, C. J., Totten, R. K. & Hergenrother, P. J., Sep 24 2009, In : Journal of Medicinal Chemistry. 52, 18, p. 5721-5731 11 p.

Research output: Contribution to journalArticle

Structure-Activity Relationship
Caspase 3
Neoplasms
Zinc
Cell Culture Techniques

Small molecule ligands for bulged RNA secondary structures

Meyer, S. T. & Hergenrother, P. J., Sep 17 2009, In : Organic Letters. 11, 18, p. 4052-4055 4 p.

Research output: Contribution to journalArticle

wedges
affinity
selectivity
RNA
Intercalating Agents

Total synthesis and cytoprotective properties of dykellic acid

Thompson, C. M., Quinn, C. A. & Hergenrother, P. J., Jan 8 2009, In : Journal of Medicinal Chemistry. 52, 1, p. 117-125 9 p.

Research output: Contribution to journalArticle

Reactive Oxygen Species
Cell Death
Rotenone
Caspase Inhibitors
Etoposide
2008

A general method for discovering inhibitors of protein-DNA interactions using photonic crystal biosensors

Chan, L. L., Pineda, M., Heeres, J. T., Hergenrother, P. J. & Cunningham, B. T., Jul 18 2008, In : ACS chemical biology. 3, 7, p. 437-448 12 p.

Research output: Contribution to journalArticle

Optics and Photonics
Biosensing Techniques
Photonic crystals
Biosensors
DNA-Binding Proteins

A new small molecule inhibitor of estrogen receptor α binding to estrogen response elements blocks estrogen-dependent growth of cancer cells

Mao, C., Patterson, N. M., Cherian, M. T., Aninye, I. O., Zhang, C., Montoya, J. B., Cheng, J., Putt, K. S., Hergenrother, P. J., Wilson, E. M., Nardulli, A. M., Nordeen, S. K. & Shapiro, D. J., May 9 2008, In : Journal of Biological Chemistry. 283, 19, p. 12819-12830 12 p.

Research output: Contribution to journalArticle

Response Elements
Estrogen Receptors
Estrogens
Cells
Molecules