List of works - Donna Huryn

2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway

scientific article

2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition

scientific article

4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands

scientific article (publication date: March 2005)

A Focused Library of Tetrahydropyrimidinone Amides via a Tandem Biginelli-Ugi Multi-Component Process

article published in 2006

A case study from the chemistry core of the Pittsburgh Molecular Library Screening Center: the Polo-like kinase polo-box domain (Plk1-PBD).

scientific article

A small-molecule oxocarbazate inhibitor of human cathepsin L blocks severe acute respiratory syndrome and ebola pseudotype virus infection into human embryonic kidney 293T cells.

scientific article

Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway

scientific article published on 22 December 2015

Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease

scientific article

Bulged DNA substrates for identifying poxvirus resolvase inhibitors

scientific article

Carboxylic acid (bio)isosteres in drug design

scientific article published on 29 January 2013

Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators

scientific article

Contributions of academic laboratories to the discovery and development of chemical biology tools

scientific article

Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists

scientific article

Delayed treatment with PTBA analogs reduces postinjury renal fibrosis after kidney injury

scientific article published on 9 December 2015

Design, synthesis and biological evaluation of a library of thiocarbazates and their activity as cysteine protease inhibitors

scientific article published on May 2010

Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype

scientific article published on May 2008

Development and Implementation of a High-Throughput High-Content Screening Assay to Identify Inhibitors of Androgen Receptor Nuclear Localization in Castration-Resistant Prostate Cancer Cells

scientific article

Discovery of a novel series of Notch-sparing gamma-secretase inhibitors

scientific article

Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease

scientific article

Do Zebrafish Obey Lipinski Rules?

scientific article published on 24 April 2019

Drug discovery in an academic setting: playing to the strengths

scientific article published on 17 January 2013

Editorial [Hot topic: Medicinal Chemistry in the Pilot Phase of the Molecular Libraries Screening Center Network (Guest Editor: Donna M. Huryn)]

scientific article published on 01 January 2009

Experimental Design on Single-Time-Point High-Throughput Microsomal Stability Assay

scientific article published on 01 June 2004

Ferroptosis as a Novel Therapeutic Target for Friedreich's Ataxia

scientific article published on 11 January 2019

HCS campaign to identify selective inhibitors of IL-6-induced STAT3 pathway activation in head and neck cancer cell lines

scientific article

HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus

scientific article

Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays

scientific article

Identification and characterization of small molecule antagonists of pRb inactivation by viral oncoproteins

scientific article published in April 2012

Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor

scientific article published on November 2007

Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening

scientific article published on August 2009

Identification of novel inhibitors of dietary lipid absorption using zebrafish

scientific article

Integrity profiling of high throughput screening hits using LC-MS and related techniques

scientific article

Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L

scientific article

Mechanism of action of selective inhibitors of IL-6 induced STAT3 pathway in head and neck cancer cell lines

scientific article

Medicinal Chemistry: Where Are All the Women?

scientific article published on 25 August 2017

Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies

scientific article published on 28 September 2012

Microtubule-stabilising drugs for therapy of Alzheimer's disease and other neurodegenerative disorders with axonal transport impairments

scientific article

Molecular docking of cathepsin L inhibitors in the binding site of papain

scientific article published on 4 July 2008

Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors

scientific article published in April 2005

Optimization of a higher throughput microsomal stability screening assay for profiling drug discovery candidates

scientific article published in August 2003

Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors

scientific article

Our scope expansion to include biologics

scientific article published on 12 March 2015

PTPRT epigenetic silencing defines lung cancer with STAT3 activation and can direct STAT3 targeted therapies

scientific article published on 13 October 2019

Paclitaxel C-10 carbamates: potential candidates for the treatment of neurodegenerative tauopathies

scientific article published on 25 April 2007

Pharmaceutical profiling method for lipophilicity and integrity using liquid chromatography–mass spectrometry

scientific article published on 01 July 2003

Pyrimidinone-peptoid hybrid molecules with distinct effects on molecular chaperone function and cell proliferation

scientific article published on 14 December 2007

Screening of 5-HT1A receptor antagonists using molecularly imprinted polymers

scientific article

Select pyrimidinones inhibit the propagation of the malarial parasite, Plasmodium falciparum

scientific article published on 20 January 2009

Structure Property Relationships of Carboxylic Acid Isosteres

scientific article published on 11 March 2016

Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.

scientific article

Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives

scientific article published on 5 June 2008

Synthesis and biological activity of a focused library of mitogen-activated protein kinase phosphatase inhibitors

scientific article

Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan

scientific article published in May 2005

Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity

scientific article published in July 2006

Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors

scientific article

Synthesis of the 6′-Fluoro Derivatives of Carbocyclic 2′,3′-Dideoxy-3′-oxa-adenosine

Synthesis, characterization and evaluation of pro-drugs of VLA-4 antagonists

scientific article published in April 2004

The identification and optimization of orally efficacious, small molecule VLA-4 antagonists

scientific article

The identification, characterization and optimization of small molecule probes of cysteine proteases: experiences of the Penn Center for Molecular Discovery with cathepsin B and cathepsin L.

scientific article

Toxicity, pharmacokinetics and metabolism of a novel inhibitor of IL-6-induced STAT3 activation

scientific article published on 24 October 2016

p97: An Emerging Target for Cancer, Neurodegenerative Diseases, and Viral Infections

scientific article published on 09 October 2019

List of works by Donna Huryn

2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway

2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition

4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands

A Focused Library of Tetrahydropyrimidinone Amides via a Tandem Biginelli-Ugi Multi-Component Process

A case study from the chemistry core of the Pittsburgh Molecular Library Screening Center: the Polo-like kinase polo-box domain (Plk1-PBD).

A small-molecule oxocarbazate inhibitor of human cathepsin L blocks severe acute respiratory syndrome and ebola pseudotype virus infection into human embryonic kidney 293T cells.

Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway

Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease

Bulged DNA substrates for identifying poxvirus resolvase inhibitors

Carboxylic acid (bio)isosteres in drug design

Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators

Contributions of academic laboratories to the discovery and development of chemical biology tools

Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists

Delayed treatment with PTBA analogs reduces postinjury renal fibrosis after kidney injury

Design, synthesis and biological evaluation of a library of thiocarbazates and their activity as cysteine protease inhibitors

Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype

Development and Implementation of a High-Throughput High-Content Screening Assay to Identify Inhibitors of Androgen Receptor Nuclear Localization in Castration-Resistant Prostate Cancer Cells

Discovery of a novel series of Notch-sparing gamma-secretase inhibitors

Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease

Do Zebrafish Obey Lipinski Rules?

Drug discovery in an academic setting: playing to the strengths

Editorial [Hot topic: Medicinal Chemistry in the Pilot Phase of the Molecular Libraries Screening Center Network (Guest Editor: Donna M. Huryn)]

Experimental Design on Single-Time-Point High-Throughput Microsomal Stability Assay

Ferroptosis as a Novel Therapeutic Target for Friedreich's Ataxia

HCS campaign to identify selective inhibitors of IL-6-induced STAT3 pathway activation in head and neck cancer cell lines

HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus

Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays

Identification and characterization of small molecule antagonists of pRb inactivation by viral oncoproteins

Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor

Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening

Identification of novel inhibitors of dietary lipid absorption using zebrafish

Integrity profiling of high throughput screening hits using LC-MS and related techniques

Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L

Mechanism of action of selective inhibitors of IL-6 induced STAT3 pathway in head and neck cancer cell lines

Medicinal Chemistry: Where Are All the Women?

Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies

Microtubule-stabilising drugs for therapy of Alzheimer's disease and other neurodegenerative disorders with axonal transport impairments

Molecular docking of cathepsin L inhibitors in the binding site of papain

Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors

Optimization of a higher throughput microsomal stability screening assay for profiling drug discovery candidates

Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors

Our scope expansion to include biologics

PTPRT epigenetic silencing defines lung cancer with STAT3 activation and can direct STAT3 targeted therapies

Paclitaxel C-10 carbamates: potential candidates for the treatment of neurodegenerative tauopathies

Pharmaceutical profiling method for lipophilicity and integrity using liquid chromatography–mass spectrometry

Pyrimidinone-peptoid hybrid molecules with distinct effects on molecular chaperone function and cell proliferation

Screening of 5-HT1A receptor antagonists using molecularly imprinted polymers

Select pyrimidinones inhibit the propagation of the malarial parasite, Plasmodium falciparum

Structure Property Relationships of Carboxylic Acid Isosteres

Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.

Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives

Synthesis and biological activity of a focused library of mitogen-activated protein kinase phosphatase inhibitors

Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan

Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors

Synthesis of the 6′-Fluoro Derivatives of Carbocyclic 2′,3′-Dideoxy-3′-oxa-adenosine

Synthesis, characterization and evaluation of pro-drugs of VLA-4 antagonists

The identification and optimization of orally efficacious, small molecule VLA-4 antagonists

The identification, characterization and optimization of small molecule probes of cysteine proteases: experiences of the Penn Center for Molecular Discovery with cathepsin B and cathepsin L.

Toxicity, pharmacokinetics and metabolism of a novel inhibitor of IL-6-induced STAT3 activation

p97: An Emerging Target for Cancer, Neurodegenerative Diseases, and Viral Infections