about
2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligandsContributions of academic laboratories to the discovery and development of chemical biology toolsIdentification of novel inhibitors of dietary lipid absorption using zebrafishOptimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitorsDevelopment and Implementation of a High-Throughput High-Content Screening Assay to Identify Inhibitors of Androgen Receptor Nuclear Localization in Castration-Resistant Prostate Cancer Cells.HCS campaign to identify selective inhibitors of IL-6-induced STAT3 pathway activation in head and neck cancer cell lines2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.Synthesis and biological activity of a focused library of mitogen-activated protein kinase phosphatase inhibitors.Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus.Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin LA case study from the chemistry core of the Pittsburgh Molecular Library Screening Center: the Polo-like kinase polo-box domain (Plk1-PBD).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.Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators.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.Bulged DNA substrates for identifying poxvirus resolvase inhibitorsIdentification and characterization of small molecule antagonists of pRb inactivation by viral oncoproteins.The identification and optimization of orally efficacious, small molecule VLA-4 antagonists.Integrity profiling of high throughput screening hits using LC-MS and related techniques.Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.Pyrimidinone-peptoid hybrid molecules with distinct effects on molecular chaperone function and cell proliferation.Structure Property Relationships of Carboxylic Acid Isosteres.Carboxylic acid (bio)isosteres in drug design.Delayed treatment with PTBA analogs reduces postinjury renal fibrosis after kidney injury.Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening.Select pyrimidinones inhibit the propagation of the malarial parasite, Plasmodium falciparumMicrotubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies.Drug discovery in an academic setting: playing to the strengths.Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.Screening of 5-HT1A receptor antagonists using molecularly imprinted polymers.Identification and synthesis of a unique thiocarbazate cathepsin L inhibitorBegacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.Our scope expansion to include biologics.Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.Molecular docking of cathepsin L inhibitors in the binding site of papain.Paclitaxel C-10 carbamates: potential candidates for the treatment of neurodegenerative tauopathies.Design, synthesis and biological evaluation of a library of thiocarbazates and their activity as cysteine protease inhibitors.Toxicity, pharmacokinetics and metabolism of a novel inhibitor of IL-6-induced STAT3 activation.
P50
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P50
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American chemist
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Donna Huryn
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Donna Huryn
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Donna Huryn
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Donna Huryn
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Donna Huryn
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