F. Schoenen

发表

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

Tudor I. Oprea, Jennifer E. Golden, Joshua A. Bittker, 2015, Cell.

Isotope or mass encoding of combinatorial libraries.

H. M. Geysen, F. Schoenen, C. Wagner, 1996, Chemistry & biology.

Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays

Alicia M. Hanson, Noreena L. Sweeney, S. Mukherjee, 2012, Nucleic acids research.

Optimization of potent hepatitis C virus NS3 helicase inhibitors isolated from the yellow dyes thioflavine S and primuline.

Jeffrey Aubé, Kelin Li, Alicia M. Hanson, 2012, Journal of medicinal chemistry.

Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.

J. Veal, F. Schoenen, J. Stafford, 1995, Journal of medicinal chemistry.

Hepatitis C Virus NS3 Helicase Inhibitor Discovery

Alicia M. Hanson, Noreena L. Sweeney, Craig A. Belon, 2013 .

Molecular and functional analysis of intragenic SMN1 mutations in patients with spinal muscular atrophy

B. Wirth, F. Schoenen, U. Fischer, 2005, Human mutation.

Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-α

M. Lambert, W. Rocque, S. Jin, 1997, Nature.

The zinc finger protein ZNF297B interacts with BDP1, a subunit of TFIIIB

B. Wirth, F. Schoenen, 2006, Biological chemistry.

Structural features and biochemical properties of TNF-α converting enzyme (TACE)

W. Rocque, S. Jin, M. Milla, 1997, Journal of Neuroimmunology.

Ebselen Inhibits Hepatitis C Virus NS3 Helicase Binding to Nucleic Acid and Prevents Viral Replication

Chad E. Schroeder, Alicia M. Hanson, Noreena L. Sweeney, 2014, ACS chemical biology.

Evaluating p97 Inhibitor Analogues for Potency against p97–p37 and p97–Npl4–Ufd1 Complexes

Henry J. Lin, T. Chou, F. Schoenen, 2016, ChemMedChem.

High level expression of functional human IgMs in human PER.C6® cells

Gene Lee, F. Schoenen, L. Ilag, 2009, mAbs.

A New Glucocerebrosidase Chaperone Reduces α-Synuclein and Glycolipid Levels in iPSC-Derived Dopaminergic Neurons from Patients with Gaucher Disease and Parkinsonism

Zayd M. Khaliq, Wei Zheng, J. Marugan, 2016, The Journal of Neuroscience.

Threading the Needle: Small-Molecule Targeting of a Xenobiotic Receptor to Ablate Escherichia coli Polysaccharide Capsule Expression Without Altering Antibiotic Resistance.

Carlos C. Goller, F. Schoenen, P. Seed, 2016, The Journal of infectious diseases.

Table 1, Listing of all Assays and AIDs for this project

Susanne Heynen-Genel, Shenghua Shi, Thomas D.Y. Chung, 2010 .

Synthesis and crystallographic analysis of a bicyclic core related to the esperamicin/calichemicin aglycones

S. Schreiber, J. Clardy, F. Schoenen, 1989 .

Effect of C-2 substitution on the stability of non-traditional cephalosporins in mouse plasma

C. Nathan, M. Zimmerman, J. Aubé, 2019, The Journal of Antibiotics.

Ionic immobilization, diversification, and release: application to the generation of a library of methionine aminopeptidase inhibitors.

G. Georg, G. Lushington, Benjamin Neuenswander, 2008, Journal of combinatorial chemistry.

Novel compound C150 inhibits pancreatic cancer through induction of ER stress and proteosome assembly

Qi Chen, Ping-Tzu Chen, F. Schoenen, 2022, Frontiers in Oncology.

Identification of Potent and Selective Inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PfM18AAP) of Human Malaria via High-Throughput Screening

J. Dalton, T. Spicer, P. Ghosh, 2014, Journal of biomolecular screening.

Autophagy activation by novel inducers prevents BECN2-mediated drug tolerance to cannabinoids

J. Marugan, Weiran Zhang, Congcong He, 2016, Autophagy.

Transannular Diels-Alder route to systems related to dynemicin A

S. Schreiber, J. Clardy, F. Schoenen, 1990 .

Discovery, SAR, and Biological Evaluation of Non-inhibitory Chaperones of Glucocerebrosidase

Noel Southall, Wei Zheng, J. Marugan, 2013 .

Structural features and biochemical properties of TNF-alpha converting enzyme (TACE).

W. Rocque, M. Milla, F. Schoenen, 1997, Journal of neuroimmunology.

Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.

L. Bohn, Lei Zhou, K. Lovell, 2015, Bioorganic & medicinal chemistry.

Repurposing p97 inhibitors for chemical modulation of the bacterial ClpB–DnaK bichaperone system

B. Geisbrecht, M. Zółkiewski, F. Schoenen, 2020, The Journal of biological chemistry.

Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis.

M. Ferrer, Noel Southall, A. Jadhav, 2022, Journal of medicinal chemistry.

Solution-Phase Parallel Synthesis of a Library of ? 2 -Pyrazolines

G. Lushington, Benjamin Neuenswander, J. Aubé, 2007 .

N‐Phenylbenzamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore

T. Chung, M. Hedrick, Benjamin Neuenswander, 2016, ChemMedChem.

DNAJA1- and conformational mutant p53-dependent inhibition of cancer cell migration by a novel compound identified through a virtual screen

T. Iwakuma, A. Parrales, A. Kaida, 2022, Cell Death Discovery.

Fluorescent primuline derivatives inhibit hepatitis C virus NS3-catalyzed RNA unwinding, peptide hydrolysis and viral replicase formation.

Alicia M. Hanson, Noreena L. Sweeney, S. Mukherjee, 2012, Antiviral research.

Regulation of tumour necrosis factor-α processing by a metalloproteinase inhibitor

R. Bast, B. Champion, F. Schoenen, 1994, Nature.

Simultaneously Targeting the NS3 Protease and Helicase Activities for More Effective Hepatitis C Virus Therapy.

Akbar Ali, Kelin Li, Alicia M. Hanson, 2015, ACS chemical biology.

Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis

C. Nathan, M. Zimmerman, J. Aubé, 2016, Journal of medicinal chemistry.

The dioxanone-to-dihydropyran Claisen rearrangement. Synthesis of C(7)-C(13) fragments of erythronolides A and B

F. Schoenen, M. Nair, S. D. Burke, 1987 .

Skeletal diversification via heteroatom linkage control: preparation of bicyclic and spirocyclic scaffolds from N-substituted homopropargyl alcohols.

J. Douglas, F. Schoenen, V. Day, 2013, The Journal of organic chemistry.

Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.

M. Ferrer, Noel Southall, Shanshan He, 2017, Journal of medicinal chemistry.

An enolate claisen route to c-pyranosides : Development and application to an ionophore synthon

F. Schoenen, D. Armistead, S. D. Burke, 1986 .

A Small Molecule Inhibitor of the MITF Molecular Pathway

Patrick W. Faloon, Carrie M. Mosher, S. Schreiber, 2014 .

Polysubstituted dihydropyrans via the enolate Claisen rearrangement. A stereocontrolled route to C-pyranosides

F. Schoenen, D. Armistead, S. D. Burke, 1984 .

The ester enolate claisen rearrangement. Synthesis of A C(1)C(6) erythronolide fragment

F. Schoenen, S. D. Burke, C. Murtiashaw, 1986 .

One-step synthesis of oxazoline and dihydrooxazine libraries.

G. Lushington, Benjamin Neuenswander, J. Aubé, 2007, Journal of combinatorial chemistry.

Effect of C-2 substitution on the stability of non-traditional cephalosporins in mouse plasma

C. Nathan, M. Zimmerman, J. Aubé, 2019, The Journal of Antibiotics.

Metarrestin, a perinucleolar compartment inhibitor, effectively suppresses metastasis

K. Nagashima, M. Ferrer, A. Shilatifard, 2018, Science Translational Medicine.

Benzothiazole and Pyrrolone Flavivirus Inhibitors Targeting the Viral Helicase.

Alicia M. Hanson, Noreena L. Sweeney, B. Geiss, 2015, ACS infectious diseases.

Three-component synthesis of 1,4-diazepin-5-ones and the construction of gamma-turn-like peptidomimetic libraries.

Jeffrey Aubé, Frank Schoenen, Benjamin Neuenswander, 2008, Journal of combinatorial chemistry.

Helicase-catalyzed ATP Hydrolysis Stimulate Hepatitis C Virus NS 3 Primuline Derivatives That Mimic RNA to Enzymology :

Noreena L. Sweeney, S. Mukherjee, F. Schoenen, 2013 .

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

M. Caron, T. Chung, M. Hedrick, 2012, ACS chemical neuroscience.

Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-α

M. Lambert, W. Rocque, S. Jin, 1997, Nature.

Discovery, Synthesis, and Optimization of Diarylisoxazole‐3‐carboxamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore

T. Chung, Benjamin Neuenswander, J. Aubé, 2015, ChemMedChem.

Small Molecules Targeting the Mitochondrial Permeability Transition

M. Jackson, T. Chung, D. Bourdette, 2015 .

Targeting p97 to Disrupt Protein Homeostasis in Cancer

F. Schoenen, Trisha Home, S. Weir, 2016, Front. Oncol..

Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways

Steven J Brown, R. Deshaies, T. Chou, 2011, Proceedings of the National Academy of Sciences.

VCP inhibitors induce endoplasmic reticulum stress, cause cell cycle arrest, trigger caspase‐mediated cell death and synergistically kill ovarian cancer cells in combination with Salubrinal

J. Chien, F. Schoenen, P. Bastola, 2016, Molecular oncology.

Functional cooperativity of p97 and histone deacetylase 6 in mediating DNA repair in mantle cell lymphoma cells

R. Jensen, S. Anant, D. Subramaniam, 2019, Leukemia.

Primuline Derivatives That Mimic RNA to Stimulate Hepatitis C Virus NS3 Helicase-catalyzed ATP Hydrolysis*

Noreena L. Sweeney, S. Mukherjee, F. Schoenen, 2013, The Journal of Biological Chemistry.

Novel Compound C150 Inhibits Pancreatic Cancer Cell Epithelial-to-Mesenchymal Transition and Tumor Growth in Mice

F. Schoenen, Ping Chen, S. Weir, 2021, Frontiers in Oncology.

Lifting the Mask: Identification of New Small Molecule Inhibitors of Uropathogenic Escherichia coli Group 2 Capsule Biogenesis

Brooks E. Maki, Nichole A. Tower, Carlos C. Goller, 2014, PloS one.

Evaluating p97 Inhibitor Analogues for Their Domain Selectivity and Potency against the p97–p47 Complex

Henry J. Lin, T. Chou, F. Schoenen, 2015, ChemMedChem.

Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D1 and D2 ATPase domains.

Henry J. Lin, M. Walters, M. Arkin, 2014, Journal of molecular biology.

Structure–Activity Relationship Study Reveals ML240 and ML241 as Potent and Selective Inhibitors of p97 ATPase

R. Deshaies, T. Chou, F. Schoenen, 2013, ChemMedChem.

Deficiency of the splicing factor Sfrs10 results in early embryonic lethality in mice and has no impact on full-length SMN/Smn splicing.

B. Wirth, M. Riessland, F. Schoenen, 2010, Human molecular genetics.

Evidence for a modifying pathway in SMA discordant families: reduced SMN level decreases the amount of its interacting partners and Htra2-beta1

Y. Hofmann, B. Wirth, K. Zerres, 2003, Human Genetics.

One-pot, three-component, domino Heck-aza-Michael approach to libraries of functionalized 1,1-dioxido-1,2-benzisothiazoline-3-acetic acids.

Kelly A. Volp, G. Lushington, Benjamin Neuenswander, 2009, Journal of combinatorial chemistry.

Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.

F. Schoenen, J. Stafford, M. A. Leesnitzer, 1995, Journal of medicinal chemistry.

Activity-Based Protein Profiling Reveals That Cephalosporins Selectively Active on Non-replicating Mycobacterium tuberculosis Bind Multiple Protein Families and Spare Peptidoglycan Transpeptidases

J. Sacchettini, C. Nathan, J. Aubé, 2020, Frontiers in Microbiology.

Benzylmorpholine Analogs as Selective Inhibitors of Lung Cytochrome P450 2A13 for the Chemoprevention of Lung Cancer in Tobacco Users

J. Aubé, F. Schoenen, E. Scott, 2013, Pharmaceutical Research.

Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.

T. Chung, E. Sergienko, B. Blagg, 2015, ACS combinatorial science.

Selective, reversible inhibitors of the AAA ATPase p97

Patrick Porubsky, Jeffrey Aubé, Kevin J. Frankowski, 2013 .

A guide to drug discovery: Combinatorial compound libraries for drug discovery: an ongoing challenge

H. Mario Geysen, David Wagner, Frank Schoenen, 2003, Nature Reviews Drug Discovery.

Revisiting the β-Lactams for Tuberculosis Therapy with a Compound-Compound Synthetic Lethality Approach

W. Bishai, Chunhong Mao, J. Aubé, 2019, Antimicrobial Agents and Chemotherapy.

Synthesis of N-alkyl-octahydroisoquinolin-1-one-8-carboxamide libraries using a tandem Diels-Alder/acylation sequence.

Benjamin Neuenswander, D. Fowler, J. Aubé, 2007, Journal of combinatorial chemistry.

Specific Inhibition of p 97 / VCP ATPase and Kinetic Analysis Demonstrate Interaction between D 1 and D 2 ATPase domains

Henry J. Lin, M. Walters, M. Arkin, 2014 .

Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.

Thomas C. Coombs, D. Auld, M. Shen, 2013, Bioorganic & medicinal chemistry letters.

High-Throughput Screening, Discovery, and Optimization To Develop a Benzofuran Class of Hepatitis C Virus Inhibitors.

M. Ferrer, Noel Southall, Shanshan He, 2015, ACS combinatorial science.

Discovery, Synthesis, and Optimization of Diarylisoxazole‐3‐carboxamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore

T. Chung, Benjamin Neuenswander, J. Aubé, 2015, ChemMedChem.

Structure-activity relationships involving the catechol subunit of rolipram

F. Schoenen, J. Stafford, P. Domanico, 1994 .