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Research Output 1995 2019

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2019

Diverse compounds from pleuromutilin lead to a thioredoxin inhibitor and inducer of ferroptosis

Llabani, E., Hicklin, R. W., Lee, H. Y., Motika, S. E., Crawford, L. A., Weerapana, E. & Hergenrother, P., Jun 1 2019, In : Nature Chemistry. 11, 6, p. 521-532 12 p.

Research output: Contribution to journalArticle

Thioredoxins
Biological Products
Screening
Clustered Regularly Interspaced Short Palindromic Repeats
Molecules

Enantioselective Synthesis of Isocarbostyril Alkaloids and Analogs Using Catalytic Dearomative Functionalization of Benzene

Bingham, T. W., Hernandez, L. W., Olson, D. G., Svec, R. L., Hergenrother, P. & Sarlah, D., Jan 9 2019, In : Journal of the American Chemical Society. 141, 1, p. 657-670 14 p.

Research output: Contribution to journalArticle

Alkaloids
alkaloid
Benzene
Biological Products
benzene

Immunohistochemical characterization of procaspase-3 overexpression as a druggable target with PAC-1, a procaspase-3 activator, in canine and human brain cancers

Schlein, L. J., Fadl-Alla, B., Pondenis, H. C., Lezmi, S., Eberhart, C. G., LeBlanc, A. K., Dickinson, P. J., Hergenrother, P. & Fan, T. M., Jan 1 2019, In : Frontiers in Oncology. 9, FEB, 96.

Research output: Contribution to journalArticle

Open Access
Brain Neoplasms
Caspase 3
Canidae
Meningioma
Glioma

Structural analyses of NudT16–ADP-ribose complexes direct rational design of mutants with improved processing of poly(ADP-ribosyl)ated proteins

Thirawatananond, P., McPherson, R. L., Malhi, J., Nathan, S., Lambrecht, M. J., Brichacek, M., Hergenrother, P., Leung, A. K. L. & Gabelli, S. B., Dec 1 2019, In : Scientific Reports. 9, 1, 5940.

Research output: Contribution to journalArticle

Open Access
Adenosine Diphosphate Ribose
Ribose
Proteins
Poly Adenosine Diphosphate Ribose
ADP-ribosylarginine hydrolase
2018

(ADP-ribosyl)hydrolases: Structural Basis for Differential Substrate Recognition and Inhibition

Rack, J. G. M., Ariza, A., Drown, B. S., Henfrey, C., Bartlett, E., Shirai, T., Hergenrother, P. & Ahel, I., Dec 20 2018, In : Cell chemical biology. 25, 12, p. 1533-1546.e12

Research output: Contribution to journalArticle

Hydrolases
Adenosine Diphosphate
Ribose
Substrates
Enzymes

Monitoring Poly(ADP-ribosyl)glycohydrolase Activity with a Continuous Fluorescent Substrate

Drown, B. S., Shirai, T., Rack, J. G. M., Ahel, I. & Hergenrother, P., Dec 20 2018, In : Cell Chemical Biology. 25, 12, p. 1562-1570.e19

Research output: Contribution to journalArticle

Glycoside Hydrolases
Adenosine Diphosphate
Hydrolases
Post Translational Protein Processing
Monitoring

Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation

Peh, J., Boudreau, M. W., Smith, H. M. & Hergenrother, P., Aug 16 2018, In : Cell chemical biology. 25, 8, p. 996-1005.e4

Research output: Contribution to journalArticle

Mitogen-Activated Protein Kinase Kinases
Phosphotransferases
Degradation
Molecules
Caspase 3

Preparation of Structurally Diverse Compounds from the Natural Product Lycorine

Tasker, S. Z., Cowfer, A. E. & Hergenrother, P., Sep 21 2018, In : Organic Letters. 20, 18, p. 5894-5898 5 p.

Research output: Contribution to journalArticle

cross coupling
Biological Products
Substitution reactions
substitutes
preparation

Strong and sustained activation of the anticipatory unfolded protein response induces necrotic cell death

Livezey, M., Huang, R., Hergenrother, P. & Shapiro, D. J., Oct 2018, In : Cell Death and Differentiation. 25, 10, p. 1796-1807 12 p.

Research output: Contribution to journalArticle

Unfolded Protein Response
Cell Death
Adenosine Triphosphate
Autophagy
Arachidonic Acid

Targeting multidrug-resistant ovarian cancer through estrogen receptor a dependent ATP depletion caused by hyperactivation of the unfolded protein response

Zheng, X., Andruska, N., Lambrecht, M. J., He, S., Parissenti, A., Hergenrother, P., Nelson, E. & Shapiro, D. J., Jan 1 2018, In : Oncotarget. 9, 19, p. 14741-14753 13 p.

Research output: Contribution to journalArticle

Unfolded Protein Response
Estrogen Receptors
Ovarian Neoplasms
Paclitaxel
Adenosine Triphosphate

Tunable Stability of Imidazotetrazines Leads to a Potent Compound for Glioblastoma

Svec, R. L., Furiassi, L., Skibinski, C. G., Fan, T. M., Riggins, G. J. & Hergenrother, P., Nov 16 2018, In : ACS chemical biology. 13, 11, p. 3206-3216 11 p.

Research output: Contribution to journalArticle

temozolomide
Glioblastoma
Toxicity
Precision Medicine
Halogens
2017

Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer

Granchi, C., Fortunato, S., Meini, S., Rizzolio, F., Caligiuri, I., Tuccinardi, T., Lee, H. Y., Hergenrother, P. & Minutolo, F., Jul 19 2017, In : Journal of Agricultural and Food Chemistry. 65, 28, p. 5639-5649 11 p.

Research output: Contribution to journalArticle

saffron
lactate dehydrogenase
L-Lactate Dehydrogenase
chemical derivatives
Derivatives

Pharmacokinetics and derivation of an anticancer dosing regimen for the novel anti-cancer agent isobutyl-deoxynyboquinone (IB-DNQ), a NQO1 bioactivatable molecule, in the domestic felid species

Lundberg, A. P., Francis, J. M., Pajak, M., Parkinson, E. I., Wycislo, K. L., Rosol, T. J., Brown, M. E., London, C. A., Dirikolu, L., Hergenrother, P. & Fan, T. M., Apr 1 2017, In : Investigational New Drugs. 35, 2, p. 134-144 11 p.

Research output: Contribution to journalArticle

Pharmacokinetics
Felidae
Neoplasms
Squamous Cell Carcinoma
Antineoplastic Agents

Predictive compound accumulation rules yield a broad-spectrum antibiotic

Richter, M. F., Drown, B. S., Riley, A. P., Garcia, A., Shirai, T., Svec, R. L. & Hergenrother, P., May 18 2017, In : Nature. 545, 7654, p. 299-304 6 p.

Research output: Contribution to journalArticle

Gram-Negative Bacteria
Anti-Bacterial Agents
Biological Products
Pharmaceutical Preparations
Amines

Reactive Oxygen Species Synergize to Potently and Selectively Induce Cancer Cell Death

Lee, H. Y., Parkinson, E. I., Granchi, C., Paterni, I., Panigrahy, D., Seth, P., Minutolo, F. & Hergenrother, P., May 19 2017, In : ACS chemical biology. 12, 5, p. 1416-1424 9 p.

Research output: Contribution to journalArticle

Cell death
Superoxides
Hydrogen Peroxide
Reactive Oxygen Species
Cell Death

Single-cell analysis of early antiviral gene expression reveals a determinant of stochastic: IFNB1 expression

Doǧanay, S., Lee, M. Y., Baum, A., Peh, J., Hwang, S. Y., Yoo, J. Y., Hergenrother, P., García-Sastre, A., Myong, S. & Ha, T., Nov 1 2017, In : Integrative Biology (United Kingdom). 9, 11, p. 857-867 11 p.

Research output: Contribution to journalArticle

Single-Cell Analysis
Gene expression
Antiviral Agents
Genes
Interferons

Synergistic and targeted therapy with a procaspase-3 activator and temozolomide extends survival in glioma rodent models and is feasible for the treatment of canine malignant glioma patients

Joshi, A. D., Botham, R. C., Schlein, L. J., Roth, H. S., Mangraviti, A., Borodovsky, A., Tyler, B., Joslyn, S., Looper, J. S., Podell, M., Fan, T. M., Hergenrother, P. & Riggins, G. J., Jan 1 2017, In : Oncotarget. 8, 46, p. 80124-80138 15 p.

Research output: Contribution to journalArticle

temozolomide
Glioma
Caspase 3
Canidae
Rodentia
2016

Access to a Structurally Complex Compound Collection via Ring Distortion of the Alkaloid Sinomenine

Garcia, A., Drown, B. S. & Hergenrother, P., Oct 7 2016, In : Organic Letters. 18, 19, p. 4852-4855 4 p.

Research output: Contribution to journalArticle

complex compounds
alkaloids
Biological Products
Alkaloids
rings

A Potent Inhibitor of Protein Sequestration by Expanded Triplet (CUG) Repeats that Shows Phenotypic Improvements in a Drosophila Model of Myotonic Dystrophy

Luu, L. M., Nguyen, L., Peng, S., Lee, J. Y., Lee, H. Y., Wong, C. H., Hergenrother, P., Chan, H. Y. E. & Zimmerman, S. C., Jan 1 2016, In : ChemMedChem. 11, 13, p. 1428-1435 8 p.

Research output: Contribution to journalArticle

Trinucleotide Repeats
Myotonic Dystrophy
Drosophila
Lead compounds
Defects

Derivatives of procaspase-activating compound 1 (PAC-1) and their anticancer activities

Roth, H. S. & Hergenrother, P., Jan 1 2016, In : Current Medicinal Chemistry. 23, 3, p. 201-241 41 p.

Research output: Contribution to journalArticle

Cell Culture Techniques
Derivatives
Clinical Trials, Phase I
Structure-Activity Relationship
Cell culture

Porous photonic crystal external cavity laser biosensor

Huang, Q., Peh, J., Hergenrother, P. J. & Cunningham, B. T., Aug 15 2016, In : Applied Physics Letters. 109, 7, 071103.

Research output: Contribution to journalArticle

laser cavities
bioinstrumentation
photonics
crystals
wavelengths

Small-molecule procaspase-3 activation sensitizes cancer to treatment with diverse chemotherapeutics

Botham, R. C., Roth, H. S., Book, A. P., Roady, P. J., Fan, T. M. & Hergenrother, P., Aug 24 2016, In : ACS Central Science. 2, 8, p. 545-559 15 p.

Research output: Contribution to journalArticle

Cell death
Caspase 3
Doxorubicin
Toxicity
Tumors

The combination of vemurafenib and procaspase-3 activation is synergistic in mutant BRAF melanomas

Peh, J., Fan, T. M., Wycislo, K. L., Roth, H. S. & Hergenrother, P., Aug 1 2016, In : Molecular Cancer Therapeutics. 15, 8, p. 1859-1869 11 p.

Research output: Contribution to journalArticle

Caspase 3
Melanoma
Cell Death
Caspase 1
Mutation
2015

A Small Molecule that Induces Intrinsic Pathway Apoptosis with Unparalleled Speed

Palchaudhuri, R., Lambrecht, M. J., Botham, R. C., Partlow, K. C., van Ham, T. J., Putt, K. S., Nguyen, L. T., Kim, S. H., Peterson, R. T., Fan, T. M. & Hergenrother, P., Dec 1 2015, In : Cell Reports. 13, 9, p. 2027-2036 10 p.

Research output: Contribution to journalArticle

Apoptosis
Molecules
Voltage-Dependent Anion Channels
Mitochondrial Membrane Potential
Cell death

Deoxynybomycins inhibit mutant DNA gyrase and rescue mice infected with fluoroquinolone-resistant bacteria

Parkinson, E. I., Bair, J. S., Nakamura, B. A., Lee, H. Y., Kuttab, H. I., Southgate, E. H., Lezmi, S., Lau, G. & Hergenrother, P., Apr 22 2015, In : Nature communications. 6, 6947.

Research output: Contribution to journalArticle

DNA Gyrase
Fluoroquinolones
bacteria
mice
Bacteria

Deoxynyboquinones as NQO1-Activated Cancer Therapeutics

Parkinson, E. I. & Hergenrother, P., Oct 20 2015, In : Accounts of chemical research. 48, 10, p. 2715-2723 9 p.

Research output: Contribution to journalArticle

Substrates
Cells
Biological Products
Toxicity
Tumors

Removal of metabolic liabilities enables development of derivatives of procaspase-activating compound 1 (PAC-1) with improved pharmacokinetics

Roth, H. S., Botham, R. C., Schmid, S. C., Fan, T. M., Dirikolu, L. & Hergenrother, P., May 14 2015, In : Journal of Medicinal Chemistry. 58, 9, p. 4046-4065 20 p.

Research output: Contribution to journalArticle

Pharmacokinetics
Cell Culture Techniques
Neoplasms
Clinical Trials, Phase I
Liver Microsomes

Salicylketoximes that target glucose transporter 1 restrict energy supply to lung cancer cells

Granchi, C., Qian, Y., Lee, H. Y., Paterni, I., Pasero, C., Iegre, J., Carlson, K. E., Tuccinardi, T., Chen, X., Katzenellenbogen, J. A., Hergenrother, P. & Minutolo, F., Nov 1 2015, In : ChemMedChem. 10, 11, p. 1892-1900 9 p.

Research output: Contribution to journalArticle

Facilitative Glucose Transport Proteins
Lung Neoplasms
Cells
Glucose
Glycolysis

Synthesis and biological evaluation of non-glucose glycoconjugated N-hydroyxindole class LDH inhibitors as anticancer agents

Di Bussolo, V., Calvaresi, E. C., Granchi, C., Del Bino, L., Frau, I., Dasso Lang, M. C., Tuccinardi, T., Macchia, M., Martinelli, A., Hergenrother, P. & Minutolo, F., Jan 1 2015, In : RSC Advances. 5, 26, p. 19944-19954 11 p.

Research output: Contribution to journalArticle

Antineoplastic Agents
Cells
Mannose
Sugars
Glucosamine

Synthesis of Dimeric ADP-Ribose and Its Structure with Human Poly(ADP-ribose) Glycohydrolase

Lambrecht, M. J., Brichacek, M., Barkauskaite, E., Ariza, A., Ahel, I. & Hergenrother, P., Mar 18 2015, In : Journal of the American Chemical Society. 137, 10, p. 3558-3564 7 p.

Research output: Contribution to journalArticle

Adenosine Diphosphate Ribose
Administrative data processing
photosynthetically active radiation
Protein Binding
Dimers
2014

Detection of protein-small molecule binding using a self-referencing external cavity laser biosensor

Zhang, M., Peh, J., Hergenrother, P. J. & Cunningham, B. T., Apr 23 2014, In : Journal of the American Chemical Society. 136, 16, p. 5840-5843 4 p.

Research output: Contribution to journalArticle

Laser resonators
Biosensing Techniques
Biosensors
cavity
Lasers

Dual small-molecule targeting of procaspase-3 dramatically enhances zymogen activation and anticancer activity

Botham, R. C., Fan, T. M., Im, I., Borst, L. B., Dirikolu, L. & Hergenrother, P., Jan 29 2014, In : Journal of the American Chemical Society. 136, 4, p. 1312-1319 8 p.

Research output: Contribution to journalArticle

Enzyme Precursors
Caspase 3
targeting
cancer
Enzymes

Light activation of staphylococcus aureus toxin YoeBSa 1 reveals guanosine-specific endoribonuclease activity

Larson, A. S. & Hergenrother, P., Jan 14 2014, In : Biochemistry. 53, 1, p. 188-201 14 p.

Research output: Contribution to journalArticle

Endoribonucleases
Guanosine
Ribonucleases
Staphylococcus aureus
Ribosomes

Natural products as starting points for the synthesis of complex and diverse compounds

Morrison, K. C. & Hergenrother, P., Jan 1 2014, In : Natural Product Reports. 31, 1, p. 6-14 9 p.

Research output: Contribution to journalArticle

Biological Products
Screening
Proteins
Carbon
Modulation

Synthesis of bridged oxafenestranes from pleuromutilin

Hicklin, R. W., Lõpez Silva, T. L. & Hergenrother, P., Sep 8 2014, In : Angewandte Chemie - International Edition. 53, 37, p. 9880-9883 4 p.

Research output: Contribution to journalArticle

Carbon
Biological Products
X rays
Atoms
Molecules

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

Rafferty, R. J., Hicklin, R. W., Maloof, K. A. & Hergenrother, P., 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. & 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. & 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., 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. & 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., 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., 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., 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., 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. & 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. & 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. & 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. & 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

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., 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