Featured Compound

8H/343 induces death in cancer cells, arrest cells in the G2/M phase of the cell cycle, and inhibits transcription of certain CYP enzymes. Link to
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Featured Compound

Apramycin induces elimination of certain plasmids from drug-resistant bacteria, thus sensitizing the bacteria to conventional antibiotics.
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Featured Compound

Dykellic acid protects cells from death as induced by various cytotoxins, and does so in a manner not associated with reactive oxygen species scavenging or caspase inhibition.
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Featured Compound

S-PAC-1 enhances the activity of procaspase-3 in vitro and induces apoptosis of cancer cells in culture. S-PAC-1 showed encouraging results in a Phase I clinical trial in pet dogs with lymphoma.
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Featured Compound

Ferric salts inhibit the formation of P. aeruginosa biofilms and sensitizes these bacteria to standard antibiotics. Paper #1 »
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Featured Compound

PAC-1 induces death in cancer cells in a manner proportional to procaspase-3 levels and is currently in a Phase I clinical trial in dogs with cancer. PAC-1 has been licensed to Vanquish Oncology for development as a chemotherapeutic for humans.
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Clinical Trial »

Featured Compound

TPMP-II-2 induces death in cancer cells, and arrests cells in the G1 phase of the cell cycle through an unknown mechanism. Certain members of this class of compounds have been licensed to LinkCore Pharmaceuticals for development as a human chemotherapeutic.  Paper »

Featured Compound

Deoxynyboquinone (DNQ) induces cancer cell death with a potency rivaling doxorubicin. DNQ is the most potent quinone that operates purely through a toxic reactive oxygen species (ROS)-based mechanism, and we are using DNQ to investigate ROS-induced toxicity as a selective anticancer strategy.  Paper #1 » Paper #2 » Paper #3 »

Featured Compound

TPMP-III-2 induces death in cancer cells by disrupting/preventing the formation of microtubules.
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Featured Compound

Deoxystreptamine dimers bind tightly and selectively to specifically-sized RNA hairpin loops.
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Featured Compound

RBPI-3 is a rhodanine-based inhibitor of the enzyme poly(ADP-ribose) glycohydrolase (PARG). This compound potently inhibits PARG in vitro and in cell lysates, with complete specificity over the other PAR glycohydrolase enzyme, called ARH3.
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Featured Compound

A new class of wedge-shaped compounds have been reported. These compounds are soluble and stable in aqueous solution, and bind to certain classes of RNA secondary structures.
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Featured Compound

ABTZ-1 is a potent antibacterial agent with activity against a wide-variety of Gram-positive pathogens, including drug-resistant strains. ABTZ-1 induces bacterial cell death through inhibition of bacterial translation.
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Featured Compound

G2 is one of >50 complex and diverse compounds synthesized from gibberellic acid.
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Featured Compound

A1 is one of >50 complex and diverse compounds synthesized from adrenosterone.
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Featured Compound

Q1 is one of >50 complex and diverse compounds synthesized from quinine.
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Featured Compound

[4.5.5.5]oxafenestranes are synthesized from the natural product pleuromutilin. X-ray crystallography was used to show that these strained oxafenestranes possess highly-planarized quaternary carbon atoms with bonds that significantly deviate from the canonical tetrahedral geometry.
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Featured Compound

DNM-2 specifically inhibits the mutant DNA gyrase that arises when bacteria become resistant to fluoroquinolones, and potently induces bacterial cell death. DNM-2 has outstanding pharmacokinetic properties when given orally, and cures mice infected with MRSA.
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Featured Hergenrother Group Member

Mike Lambrecht received his B.S. in chemistry from the University of Wisconsin and joined the Hergenrother lab in the fall of 2010. In the Hergenrother lab Mike synthesized the natural product dimeric ADP-ribose, fully characterized its ability to be processed as a substrate by poly(ADP-ribose) glycohydrolase enzymes, and constructed novel probes to evaluate its binding to various proteins. At the University of Illinois Mike is a member of the NIH Chemical Biology Interface Training Program, and he will present some of his work at the 2015 Gordon Research Conference on Carbohydrates.

Featured Hergenrother Group Member

Quinn Peterson graduated from UIUC in July 2011 with a PhD in Biochemistry. Quinn was a member of the Chemistry-Biology Interface Training Grant. Quinn was part of the team that identified the mechanism by which the novel anti-cancer agent PAC-1 activates procaspase-3 and that defined the SAR and sub-cellular localization for PAC-1. Quinn also developed a gram-scale solution-phase synthesis of the Ac-DEVD-pNA caspase-3/-7 substrate and developed the compound S-PAC-1 for a Phase I clinical trial in pet dogs with lymphoma, and probed the In 2009 Quinn was awarded a predoctoral fellowship from the Medicinal Chemistry Division of the American Chemical Society and presented his work at Experimental Biology 2009 among numerous other conferences. Quinn is now a posdoctoral fellow in the laboratory of Professor Douglas Melton at Harvard University.

Featured Hergenrother Group Member

Claire Knezevic graduated in 2008 with a B.A. in Chemistry from Scripps College. While in the Hergenrother laboratory, Claire has been part of the design, synthesis, and evaluation of novel inhibitors of poly(ADP-ribose) glycohydrolase (PARG), including the X-ray structure of one of these inhibitors bound to PARG. Claire presented some of her work at PARP 2010 in Zurich, Switzerland, and at the 2012 Bioorganic Gordon Research Conference. She is an NSF predoctoral fellow.

Featured Hergenrother Group Member

Howard Roth graduated in 2009 with a B.S. in chemistry from Northwestern University, where he conducted undergraduate research with Prof. Karl Scheidt. In the Hergenrother laboratory Howard has been working on the development of potent anticancer agents, and recently published a manuscript on the design, synthesis, and evaluation of a 837-membered library of PAC-1 derivatives, and a manuscript on pharmacokinetically-optimized derivatives of PAC-1. Howard was awarded a predoctoral fellowship from the Medicinal Chemistry Division of the American Chemical Society.

Featured Hergenrother Group Member

Rachel Botham graduated with a B.S. in Chemistry and Biological Sciences from the University of Pittsburgh, and joined the chemical biology graduate program at UIUC as a member of the Chemical Biology Interface Training Program and as a Springborn Fellow. While in the Hergenrother lab Rachel has demonstrated the tremendous synergistic potential of the anticancer compound PAC-1. In addition, she has developed a convenient synthesis of a chromogenic caspase substrate, and was part of the team that identified potent new anticancer agents from a library of PAC-1 derivatives. She has recently presented her work at the Cell Biology of Metals Gordon Research Conference. Rachel is an NSF predoctoral fellow.

Featured Hergenrother Group Member

Joe Bair graduated from UIUC in December of 2011 with a PhD in Chemistry. While in the Hergenrother lab Joe synthesized the novel anticancer compound DNQ, an extremely potent azaanthraquinone, and Joe also determined the mechanism by which DNQ induces death in cancer cells. While at UIUC Joe was the recipient of the Pytosh Graduate Fellowship, the Pines travel award, and the Fuson Travel Award, an award that allowed Joe to present his work at the 2010 Gordon Research Conference on Natural Products. Joe is now a postdoctoral fellow in the laboratory of John Hartwig at UC Berkeley.

Featured Hergenrother Group Member

Julia Williams graduated with a B.S. in Microbiology from the University of Idaho and joined the Hergenrother lab in 2007 as a graduate student in the Department of Microbiology. Julia is investigating the tractability of toxin-antitoxin systems as novel antibacterial targets, and has published a manuscript on the mechanism of the txe toxin, on the prevalence of toxin-antitoxin genes in MRSA and P. aeruginosa, and a review of the potential of exploiting plasmid-encoded factors in antimicrobial therapy, and another on artificial activation of toxin-antitoxin systems as an antibacterial strategy. Julia is a member of the NIH Cellular and Molecular Biology Training Grant, and presented some of her research at PacifiChem 2010.

Featured Hergenrother Group Member

Karen Morrison received her B.S. in chemistry from Harvey Mudd College in 2008 and joined the Department of Chemistry at UIUC later that year as a Springborn Fellow and a National Science Foundation predoctoral fellow. Karen was part of the team that synthesized >160 complex and diverse compounds from natural products. In addition, Karen has published manuscripts on a novel and facile method for the evaluation of compounds that affect the tubulin/microtubulin dynamic, and on transcriptional profiling of PAC-1 and derivatives. Karen presented some of her work at the 2012 ACS meeting in San Diego, at the 2012 Bioorganic Gordon Research Conference, and at the Graduate Research Symposium at UC Boulder in July 2012.

Featured Hergenrother Group Member

Betsy Parkinson graduated with B.S. in Chemistry from Rhodes College and joined the Hergenrother lab in 2010 as a graduate student in chemical biology and as an NSF predoctoral fellow. Betsy is investigating the therapeutic potential of the novel anticancer compound DNQ, and was part of the team that discovered this compound’s mode-of-action and in vivo activity, and has utilized molecular modeling to design and synthesize novel and potent derivatives. Betsy also developed a novel derivative of deoxynybomycin as a potent and selective antibacterial agent. Betsy presented her work at the EORTC-NCI-AACR Symposium on 'Molecular Targets and Cancer Therapeutics' in Dublin, Ireland (November 2012), the High-Throughput Chemistry and Chemical Biology Gordon Research Conference (June 2013), and the Medicinal Chemistry Gordon Research Conference (August 2013) where she won a best poster award. Betsy was awarded a pre-doctoral fellowship from the from the Medicinal Chemistry Division of the American Chemical Society for 2013-2014.

Featured Hergenrother Group Member

Robert Hicklin received his B.S. in chemistry from the University of Central Missouri and joined the Hergenrother lab in the fall of 2010 as a graduate student in organic chemistry. Rob was part of the team that synthesized >160 complex and diverse compounds from natural products from gibberellic acid, adrenosterone, and quinine. In addition, he was recently a co-author on a manuscript reporting the synthesis of 84 complex and diverse compounds from the natural product abietic acid, and a manuscript reporting the discovery that fenastranes could be constructed from pleuromutilin. Rob was the recipient of the Pines Graduate Fellowship for 2014-2015.

Featured Hergenrother Group Member

Michelle Richter received her B.S. in biochemistry from Union College and joined the Hergenrother lab in the Fall of 2011 as a graduate student in organic chemistry and a member of the NIH Chemical Biology Interface Training Program. Michelle was part of the team that recently reported the synthesis of >160 complex and diverse compounds that were synthesized from natural products. Michelle is an NSF predoctoral fellow.

Featured Hergenrother Group Member

Ryan Rafferty graduated with a PhD in Chemistry from the laboratory of Professor Robert Williams at Colorado State and joined the Hergenrother laboratory in 2011. In the Hergenrother laboratory Dr. Rafferty has developed a facile method for the creation of complex and diverse compounds from the natural product abietic acid. Ryan presented some of his work at the Natural Product Gordon Research Conference in 2013.

Welcome, our laboratory uses small organic molecules to identify and define novel targets for the treatment of a variety of intractable biomedical problems. We use the tools of synthetic organic chemistry, biochemistry, combinatorial chemistry, high-throughput screening, and cell biology to explore disease states that have for a variety of reasons resisted the standard paradigm of drug discovery and development. In the course of this work we often obtain clinical samples from patients in an effort to both define the levels of a target in the patient population and to test the efficacy of our compounds in these clinical isolates. We are actively using small molecules to define novel biological targets for the treatment of cancer, neurodegeneration, and drug-resistant bacteria.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

NEW: Evi Llabani receives the inaugural C*STAR fellowship!

NEW: The Phase 1 clinical trial of PAC-1 in human cancer patients is beginning!  See listing on clinicaltrials.gov and listen to the interview

Vanquish Oncology, Inc., announces multimillion dollar investment to move PAC-1
to human clinical trials for cancer patients. See news article.

Animation video of recent Nature Chemistry paper

Vanquish Oncology, Inc., launched to develop procaspase-activating
compounds from Hergenrother lab for treatment of cancer.

See article on graduate student Quinn Peterson's research

As of June 15, 2009 a clinical trial of s-PAC-1 in pet dogs with lymphoma will begin at the UIUC School of Veterinary Medicine. For more information or to enroll your dog in this trial please see: http://vetmed.illinois.edu/vth/MedServices/ClinicalTrial/PDF/Oncology/SulfonamidePAC-1.pdf

 

Department of Chemistry, University of Illinois at Urbana-Champaign
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